PDGFR
特异性亚型抑制剂
PDGFR产品
目录号 | 产品描述 | 文献引用 | 实验数据 |
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S1040 |
Sorafenib (BAY 43-9006) tosylateSorafenib (BAY 43-9006) tosylate是Raf-1和B-Raf的多重激酶抑制剂,无细胞试验中IC50分别为6 nM和22 nM。Sorafenib 还可抑制VEGFR-2、VEGFR-3、PDGFR-β、Flt-3和c-KIT,对应的IC50值分别为90 nM、20 nM、57 nM、59 nM和68 nM。Sorafenib Tosylate 可诱导autophagy、apoptosis并激活ferroptosis,并具有抗肿瘤活性。 |
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Inhibition of breast cancer cell growth using sorafenib. MCF-7 breast cancer cells were treated with increasing concentrations of sorafenib for 5 days. Cell number was measured using a colorimetric growth assay (crystal violet stain) and expressed relative to DMSO treated control cells. |
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S1026 |
Imatinib (STI571) MesylateImatinib Mesylate (STI571, CGP-57148B)是一种口服生物有效的Imatinib甲磺酸盐,是一种多靶点抑制剂,作用于v-Abl,c-Kit和PDGFR,在无细胞和细胞试验中,IC50分别为0.6 μM,0.1 μM 和0.1 μM。Imatinib Mesylate (STI571) 可诱导自噬。 |
![]() ![]() THOC5 phospho-Y225 levels were assessed in the populations shown by flow cytometry following 24 h treatment with 5 μM imatinib, 150 nM dasatinib or 5 μM nilotinib. Results are displayed as mean fluorescence intensity (n= 4) ±s.e.m. |
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S1042 |
Sunitinib (SU11248) malateSunitinib (SU11248) malate是一种多靶点RTK抑制剂,作用于VEGFR2 (Flk-1)和 PDGFRβ,在无细胞试验中IC50分别为80 nM 和2 nM,也会抑制c-Kit的活性。Sunitinib Malate 可有效地抑制 Ire1α 的自身磷酸化。Sunitinib Malate 可增加 death receptor 和 线粒体依赖的凋亡 mitochondrial-dependent apoptosis。 |
![]() ![]() Autophagy inhibition blocks the antiproliferative effects of sunitinib and sorafenib but not AZD6244. Medullary thyroid cancer–1.1 (MTC-1.1) and TT cells were transfected transiently with scrambled or autophagy protein 5 (Atg-5) small inter fering RNA. After transfection, cells with and without Atg-5 knockdown were exposed to sunitinib (50 nM), sorafenib (10 nM), and AZD6244 (30 nM) for 48 hours. Treated cells were subjected to a 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium proliferation assay. Similar experiments were repeated 3 times. Histograms represent the relative percent of OD490 nM absorbance. The asterisk indicates significance versus scrambled small inter fering RNA–treated control ( P < .05). All data are relative multiples of expression compared to untreated cells. The data are representative of 3 experiments and are expressed as the mean ± the standard error. |
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S1490 |
Ponatinib (AP24534)Ponatinib (AP24534)是一种新型有效的多靶点抑制剂,在无细胞试验中作用于Abl,PDGFRα,VEGFR2,FGFR1和Src,IC50分别为0.37 nM,1.1 nM,1.5 nM,2.2 nM和5.4 nM。Ponatinib (AP24534)可抑制自噬。 |
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RCH-ACV cells were treated with ponatinib(50 nM), PCI-32765(50 nM), or BMS-599626(500 nM) over a time course, and whole-cell extracts were subjected to immunoblot analysis for total or phospho-AKT. |
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S1005 |
Axitinib (AG 013736)Axitinib (AG 013736)是一种多靶点抑制剂,作用于 VEGFR1,VEGFR2,VEGFR3,PDGFRβ和c-Kit,在猪主动脉内皮细胞中IC50分别为0.1 nM,0.2 nM,0.1-0.3 nM,1.6 nM和1.7 nM。 |
![]() ![]() Secondary assay development. The invasive potential of MDA-MB-231 spheroids was measured using modified Boyden chambers coated with Matrigel™. Invading cells were fixed, stained with DAPI, and quantified by fluorescence microscopy using 5 random fields per filter insert in triplicate. U0126, PF2341066, axitinib, and PKC412 inhibited the invasive potential of MDA-MB-231 spheroids by ~90% as compared to untreated spheroids (UT). ***p ≤ 0.001. IGF1R and dasatinib displayed no statistical difference as compared to UT MDA-MB-231 spheroids. |
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S9973New |
Flumatinib (HH-GV-678)Flumatinib (HH-GV-678) 是一种新型 Bcr-Abl 抑制剂,对 c-Abl、PDGFRβ 和 c-Kit 的 IC50 值分别为 1.2 nM、307.6 nM 和 665.5 nM。 |
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E0050New |
Seralutinib (GB002)Seralutinib (PK10571, GB002) 是一种新型 PDGFR 激酶抑制剂,在酶测定中对 PDGFRα 和 PDGFRβ 的 IC50 分别为 8 nM 和 10 nM。 |
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S2475 |
Imatinib (STI571)Imatinib (STI571, CGP057148B, ST-1571)是一种多靶点酪氨酸激酶抑制剂,抑制v-Abl、c-Kit和PDGFR的IC50分别为0.6,0.1和0.1 μM。Imatinib (STI571) 可诱导自噬。 |
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Inhibition of thymidine (a and b) and cytarabine (c and d) uptake with imatinib. K562 cells (a and c) and MEG-01 cells (b and d) were incubated at 37 ◦C for 15 min with imatinib transport buffer, and then incubated with 0.5 Ci of [3H] thymidine or [3H] cytarabine for an additional 5 min in presence of imatinib. Cells were then washed 3 times, lysed and radioactivity associated to cell pellets was quantified. DMSO, dimethylsulfoxide; DPD, dipyridamole. |
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S1111 |
Foretinib (GSK1363089)Foretinib (GSK1363089, EXEL-2880, XL-880, GSK089) 是一种ATP竞争性的HGFR和VEGFR抑制剂,对Met (c-Met)和KDR作用最强,在无细胞试验中IC50分别为0.4 nM和0.9 nM。对Ron, Flt-1/3/4, Kit (c-Kit), PDGFRα/β和Tie-2作用效果稍弱,对FGFR1和EGFR几乎没有抑制活性。Phase 2。 |
![]() ![]() c-MET/RON inhibitors restore sensitivity to lapatinib in SK-BR-3-LR cells. Cell growth was determined using the sulforhodamine B assay. The concentration used was 0.1 uM for crizotinib, MGCD-265, XL880, sunitinib, dasatinib, and TAE-684I. The phosphorylation of HER2, AKT and ERK1/2 was determined by Western blotting.
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S1010 |
Nintedanib (BIBF 1120)Nintedanib (BIBF 1120, Intedanib, Vargatef, Ofev) 尼达尼布是一种有效的三重血管激酶抑制剂,作用于VEGFR1/2/3, FGFR1/2/3和PDGFRα/β,在无细胞试验中IC50分别为34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM和59 nM/65 nM。Phase 3。 |
![]() ![]() Effect of BIBF 1120 on the accumulation of doxorubicin (Dox) and rhodamine 123. The accumulations of doxorubicin a, b and rhodamine 123 c, d were measured by flow cytometric analysis as described in "Materials and Methods". The results are presented as fold change in fluorescence intensity relative to control MDR cells. Columns, means of triplicate determinations; bars, SDs. **P<0.01 versus control group |
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S1178 |
Regorafenib (BAY 73-4506)Regorafenib (BAY 73-4506, Fluoro-Sorafenib, Resihance, Stivarga) 是一个多靶点抑制剂,作用于VEGFR1,VEGFR2,VEGFR3,PDGFR-β,Kit (c-Kit),RET (c-RET)和Raf-1,在无细胞试验中IC50分别是13 nM,4.2 nM,46 nM,22 nM,7 nM,1.5 nM和2.5 nM。Regorafenib 可诱导自噬。 |
![]() ![]() Hepatoma cells 24 h after plating were treated with vehicle (DMSO), regorafenib (REGO, 0.5 µM), PDE5 inhibitor (sildenafil, 2 µM); or the drugs in combination. 24 hours after treatment cells were isolated and viability determined by trypan blue (n=3, SEM). *P 0.05
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S1035 |
Pazopanib HCl (GW786034 HCl)Pazopanib HCl (GW786034 HCl)是一种新型多靶点抑制剂,作用于VEGFR1,VEGFR2,VEGFR3,PDGFR,FGFR,c-Kit和c-fms,在无细胞试验中IC50分别是10 nM,30 nM,47 nM,84 nM,74 nM,140 nM和146 nM。Pazopanib 可诱导自噬II型细胞死亡。 |
![]() ![]() Effect of HDIL-2/TKI on apoptosis of RCC cells. Three RCC cell lines treated with different concentrations of Pazopanib and HDIL-2 and incubated for 48 h. Microscopic images show apoptotic materials 48 h following treatment (arrows show the apoptotic materials in the pazopanib-treated cells).
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S1017 |
Cediranib (AZD2171)Cediranib (AZD2171, NSC-732208)是一种高效的VEGFR(KDR)抑制剂,IC50为<1 nM,同时也抑制Flt1/4,IC50为5 nM/≤3 nM,此外对c-Kit和PDGFRβ也具有相似的抑制活性,对VEGFR的选择性比PDGFR-α, CSF-1R和Flt3分别高36倍, 110倍 和1000倍以上。Cediranib (AZD2171)可诱导自噬小体累积。Phase 3。 |
![]() ![]() Western blots of EZH2 expression in A549, HCC461, and HCC4006 cells upon treatment with different doses of VEGFR-2-inhibitor AZD2171 (0, 5 and 10 nM). AZD2171 decreased the expression of EZH2 in HCC4006 and HCC461 cells expressing VEGFR-2 in a dose-dependent manner but did not do so in A549 cells lacking expression of VEGFR-2.
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S1018 |
Dovitinib (TKI-258)Dovitinib (TKI-258, CHIR-258)是一种多靶点的RTK抑制剂,在无细胞试验中对III型(FLT3/c-Kit)作用最强,IC50为1 nM/2 nM,同时也作用于IV类(FGFR1/3)和V类(VEGFR1-4) RTKs,IC50为8-13 nM,但对InsR,EGFR,c-Met,EphA2,Tie2,IGF-1R和HER2作用较弱。Phase 4。 |
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Orthotopic xenografts of HNSCC cell lines (A) SCC-1 and (B) OSC-19 were treated with dovitinib (20 mg/kg/day). In addition, the OSC-19 xenografts were treated with +/ radiation therapy. Marker, mean for triplicate; bars, SE. Statistical significance by unpaired t-test, p < 0.05. |
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S1003 |
Linifanib (ABT-869)Linifanib (ABT-869, AL39324, RG3635)是一种新型有效的ATP竞争性VEGFR/PDGFR抑制剂,作用于KDR,CSF-1R,Flt-1/3和PDGFRβ,其IC50分别为4 nM,3 nM,3 nM/4 nM和66 nM,对突变激酶依赖性癌细胞(即FLT3)最有效。Linifanib (ABT-869) 可诱导自噬和凋亡。Phase 3。 |
![]() ![]() (B and C) KMCH-1 cells were plated alone (monoculture) or together with PDGF-BB-secreting LX-2 cells (co-culture) in a transwell insert co-culture system (KMCH-1 cells in the bottom wells and LX-2 cells in the inserts; 1:1 ratio) for 2 days. Cells were treated as indicated with vehicle, rhTRAIL (10 ng/ml for 6 h on day 2), rhTRAIL plus imatinib [rhTRAIL:10 ng/ml for 6 h on day 2; Imatinib: 5 μmol/L for 24 h (day2)], or rhTRAIL plus linifanib [rhTRAIL: 10 ng/ml for 6 h on day 2; Linifanib:0.5 μmol/L for 24 h (day2)]. After rhTRAIL treatment for 6 h,KMCH-1 cells were analysed for apoptotic nuclear morphology by DAPI-staining (B) and for DNA fragmentation by transferasemediated dUTP nick end labelling assay (C) with quantification of apoptotic nuclei by fluorescence microscopy. |
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S2730 |
Crenolanib (CP-868596)Crenolanib (CP-868596, ARO 002)是一种有效的,选择性PDGFRα/β抑制剂,在CHO细胞中Kd为2.1 nM/3.2 nM,也能有效抑制FLT3,对D842V突变型敏感对V561D突变型不敏感,作用于PDGFR比作用于c-Kit,VEGFR-2,TIE-2,FGFR-2,EGFR,erbB2,和Src的选择性高100倍以上。Crenolanib可辅助诱导线粒体自噬。 |
![]() ![]() Western blot analysis using 4G10 and anti-FLT3 antibody after immunoprecipitation with anti-FLT3 antibody and Western blot analysis of phospho-ERK (pERK) and ERK performed on whole cell lysates from HB119 and Molm14 cells. Cells were exposed to 100 nM crenolanib for 60 min.
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S1064 |
Masitinib (AB1010)Masitinib (AB1010)是一种新型的Kit (c-Kit)和PDGFRα/β抑制剂,IC50分别为200 nM和540 nM/800 nM,但对ABL和c-Fms抑制作用较弱。Phase 3。 |
![]() ![]() H&E stained histology slides of A), C), and E) control implants and B), D), and F) drug-loaded implants for 14, 21 and 28 day time points respectively. Location of the implants is denoted by the asterisk ‘*’. Scale bar: 200 μm.
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S1207 |
Tivozanib (AV-951)Tivozanib (AV-951, KRN-951)是一种有效的,选择性VEGFR抑制剂,作用于VEGFR1/2/3时,IC50分别为0.21 nM/0.16 nM/0.24 nM,也抑制PDGFR和c-Kit,作用于FGFR-1, Flt3, c-Met EGFR和IGF-1R活性较弱。Phase 3。 |
![]() ![]() On-chip angiogenesis assay. Fluorescence imaging of Tg(fli1a:EGFP) embryos at 64 hpf. Transgenic embryos were arrayed and immobilized at 16 hpf and continuously perfused with E3 media containing vehicle control (dimethyl sulfoxide) or selected small-molecule antiangiogenic drugs (Sunitinib and Tivozanib). Right panel: microscopic visualization of patterns of ISV. White arrows: normal ISV growth; blue arrows: partial ISV growth inhibition; and red arrows; complete ISV growth inhibition.
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S1032 |
Motesanib Diphosphate (AMG-706)Motesanib Diphosphate (AMG-706)是一种有效的ATP竞争性的VEGFR1/2/3抑制剂,IC50分别为2 nM/3 nM/6 nM;对Kit (c-Kit)具有相似的抑制活性,对VEGFR选择性比PDGFR和Ret高10倍。Phase 3。 |
![]() ![]() Immunofluorescence staining of choroidal neovascularization (CNV) lesions 14 days after laser photocoagulation. Choroidal flat mounts were fluorescently labeled with F-actin-specific marker phalloidin (green channel), endothelial cell marker CD34 (red channel), and nuclear marker DAPI (blue channel). CNV lesions in topical vehicle-treated eye (A, C, E and G) and topical motesanib-treated eye (B, D, F and H). The scale bar represents 100 um.
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S1244 |
Amuvatinib (MP-470)Amuvatinib (MP-470, HPK 56) 是一种有效的,作用于c-Kit、PDGFα和Flt3的多靶点抑制剂,IC50分别为10 nM、40 nM和81 nM。Amuvatinib 可抑制c-MET和c-RET。Amuvatinib 还具有DNA修复蛋白Rad51抑制剂及抗肿瘤的活性。Phase 2。 |
![]() ![]() Inactivation of AXL by MP470 reverses epithelial to mesenchymal transition. Immunoblot analyses of lysates from TGFβ/TNFα- treated MCF10A cells treated with varying amounts of MP470 for 72 hours.
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S1164 |
Lenvatinib (E7080)Lenvatinib (E7080)是一种多靶点抑制剂,无细胞试验中,作用于VEGFR2(KDR)/VEGFR3(Flt-4)最有效,IC50为4 nM/5.2 nM,对VEGFR1/Flt-1作用效果稍弱,作用于VEGFR2/3比作用于FGFR1, PDGFRα/β选择性高10倍左右。Lenvatinib (E7080) 也是FGFR1-4、PDGFR、Kit (c-Kit)和RET (c-RET)的抑制剂,并具有强效的抗肿瘤活性。Phase 3。 |
![]() ![]() Dot Plot Distribution of Live, Preapoptotic and Apoptotic Cells after Administration of DuP-697 and E7080 Combination.
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S1470 |
Orantinib (SU6668)Orantinib (TSU-68, SU6668)有效作用于PDGFR自磷酸化,无细胞试验中Ki为8 nM,也强效抑制Flk-1和FGFR1反式磷酸化,对IGF-1R,Met, Src,Lck,Zap70,Abl和CDK2几乎没有抑制活性;对EGFR没有抑制作用。Phase 3。 |
![]() ![]() Effect of select kinase inhibitors on DF508-CFTR maturation analyzed by immunoblotting. 293MSR-GT cells stably expressing DF508-CFTR were treated with 15 uM kinase inhibitors or 0.3% DMSO (vehicle control), as indicated, grown at 37°C for 48 h, and the appearance of the mature protein, band C, monitored by immunoblotting with anti-CFTR antibodies. Band B represents the immature protein. DMSO represents vehicle- alone control, 27°C represents temperature rescue of F508-CFTR at 27°C, 37°C represents untreated DF508-CFTR control, and WT represents WT-CFTR. Top panels depict the anti-CFTR immunoblot and bottom panels depict actin (loading) control. ** represents cellular toxicity. |
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S1181 |
ENMD-2076ENMD-2076 选择性地作用于 Aurora A 和 Flt3,IC50分别为14 nM和1.86 nM,作用于Aurora A比作用于Aurora B选择性高25倍,对RET、SRC、NTRK1/TRKA、CSF1R/FMS、VEGFR2/KDR、FGFR和PDGFRα作用效果稍弱。ENMD-2076 可抑制各种人类实体瘤和造血癌细胞系的生长,其IC50值为0.025至0.7μM,可诱导凋亡和G2/M期停滞。Phase 2。 |
![]() ![]() Breast cancer cells line MDA-MB-231 were treated with the indicated concentrations of ENMD-2076.
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S1536 |
CP-673451CP-673451是一种选择性的PDGFRα/β抑制剂,无细胞试验中IC50为10 nM/1 nM,比作用于其他血管生成受体选择性高450倍以上,具有抗血管生成和抗肿瘤活性。 |
![]() ![]() Pharmacological inhibition of PDGFR-β by cp673451 significantly attenuated the mRNA expression of BCL2A1 (E) and SERPINE (F) in ASCs.
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S1363 |
Ki8751Ki8751是一种有效的,选择性的VEGFR2抑制剂,IC50为0.9 nM,作用于VEGFR2比作用于c-Kit, PDGFRα和FGFR-2选择性高40倍以上,对EGFR, HGFR和InsR没有抑制活性。 |
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Effect of select kinase inhibitors on DF508-CFTR maturation analyzed by immunoblotting. 293MSR-GT cells stably expressing DF508-CFTR were treated with 15 uM kinase inhibitors or 0.3% DMSO (vehicle control), as indicated, grown at 37 °C for 48 h, and the appearance of the mature protein, band C, monitored by immunoblotting with anti-CFTR antibodies. Band B represents the immature protein. DMSO represents vehicle-alone control, 27 °C represents temperature rescue of F508-CFTR at 27 °C, 37 °C represents untreated DF508-CFTR control, and WT represents WT-CFTR. Top panels depict the anti-CFTR immunoblot and bottom panels depict actin (loading) control. ** represents cellular toxicity. |
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S2231 |
TelatinibTelatinib (BAY 57-9352) 是一种有效的VEGFR2/3, c-Kit和PDGFRα抑制剂,IC50分别为6 nM/4 nM, 1 nM和15 nM。Phase 2。 |
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S2622 |
PP121PP121是一种作用于PDGFR, Hck, mTOR, VEGFR2, Src和Abl的多靶点抑制剂,IC50分别为2 nM, 8 nM, 10 nM, 12 nM, 14 nM和18 nM,也抑制DNA-PK,IC50为60 nM。 |
![]() ![]() PP121 induces apoptosis in ATC cells. CAL62 cells were treated with PP121 at the indicated concentrations for 48 h, followed by PI staining. The nuclei were stained with Hoechst and analyzed using a fluorescent microscope. The representative images are shown.
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S3012 |
PazopanibPazopanib (GW786034) 是一种新型多靶点的VEGFR1,VEGFR2,VEGFR3,PDGFR,FGFR,c-Kit 和 c-Fms/CSF1R抑制剂,无细胞试验中IC50分别为10 nM,30 nM,47 nM,84 nM,74 nM,140 nM 和 146 nM。Pazopanib 可诱导 cathepsin B 的活化和自噬。 |
![]() ![]() Three RCC cell lines treated with different concentrations of TKI and HDIL-2 and incubated for 48 h. Microscopic images show apoptotic materials 48 h following treatment (arrows show the apoptotic materials in the pazopanib-treated cells).
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S7397 |
Sorafenib (BAY 43-9006)Sorafenib (BAY 43-9006, NSC-724772)是Raf-1和B-Raf的多重激酶抑制剂,无细胞试验中IC50分别为6 nM和22 nM。Sorafenib 还可抑制VEGFR-2、VEGFR-3、PDGFR-β、Flt-3和c-KIT,对应的IC50值分别为90 nM、20 nM、57 nM、59 nM和68 nM。Sorafenib 可诱导autophagy、apoptosis并激活ferroptosis,Sorafenib 具有抗肿瘤活性。 |
![]() ![]() Involvement of EV linc-VLDLR in tumor cell responses to chemotherapy. Cells were incubated with sorafenib, camptothecin, or doxorubicin. EVs were obtained after 24 hours, and qRT-PCR was performed for linc-VLDLR. The bars represent the mean ?SEM of the increase in cell viability from 3 independent studies. *, P < 0.05.
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S2774 |
MK-2461MK-2461是一种有效的,多靶点抑制剂,作用于c-Met(WT/mutants),IC50为0.4-2.5 nM,对Ron,和Flt1作用效果稍弱;作用于c-Met比作用于FGFR1, FGFR2, FGFR3, PDGFRβ, KDR, Flt3, Flt4, TrkA和TrkB选择性高8到30倍。Phase 1/2。 |
![]() ![]() Both V-H cells and V-J cells are treated with MK-2461, XL-184 or ABT-869, respectively. (i-k) Western blot analysis of sFlt-1 expression after incubation with three VEGF-A receptor inhibitors or in the control.
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S8024 |
Tyrphostin AG 1296Tyrphostin AG 1296 是一种PDGFR抑制剂,IC50为0.3-0.5 μM,对EGFR没有抑制活性。Tyrphostin AG1296 在抑制Swiss 3T3细胞中抑制 FGFR 和 c-Kit 的IC50值为12.3 μM和1.8 μM。Tyrphostin AG1296 可在A375R细胞中诱导剧烈的凋亡。 |
![]() ![]() After inoculation with KAT4 cells, administration of compounds including MK-2206 (100 mg/kg), tyrphostin AG 1296 (100 mg/kg), or a combination of MK-2206 (100 mg/kg) and tyrphostin AG 1296 (100 mg/kg) was performed. The combination of MK-2206 and tyrphostin AG 1296 induced significant apoptosis of KAT4 tumor cells in vivo measured by the terminal deoxynucleotidyl transferase dUTP nick end labeling assay (green), and nuclei were stained with Hoechst (blue). |
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S8015 |
Agerafenib (RXDX-105)Agerafenib (RXDX-105, CEP-32496) 是一种高度有效的BRAF(V600E/WT)和c-Raf抑制剂,Kd为14 nM/36 nM和39 nM,适度有效作用于Abl-1, c-Kit, RET (c-RET), PDGFRβ和VEGFR2,对MEK-1, MEK-2, ERK-1和ERK-2具有微弱的亲和力。Phase 1/2。 |
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S2895 |
Tyrphostin 9Tyrphostin 9 (SF 6847, RG-50872) 是第一个EGFR抑制剂,IC50为460 μM,作用于PDGFR更有效,IC50为0.5μM。 |
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S0504 |
SU14813SU14813 (SU 014813)是一种多受体 tyrosine kinase 的抑制剂,对于 VEGFR2、VEGFR1、PDGFRβ 和 Kit (c-Kit) 的IC50值分别为50 nM,2 nM,4 nM和15 nM。SU14813 具有强大的抗血管生成和抗肿瘤活性。 |
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S7667 |
SU5402SU5402是一种有效的多靶点受体激酶抑制剂,对VEGFR2,FGFR1,和PDGF-Rβ的IC50分别为20 nM,30 nM,和510 nM。 |
![]() ![]() Four FGFR inhibitors, namely PD-173074 (PD-74), PD-166866 (PD-66), SU5402 (SU54) and NVP-BGJ398 (BG-98), inhibit A673, SKNMC, POE, RDES and SKES Ewing cell growth in vitro in a dose-dependent manner, whereas normal cells (IMR90 fibroblasts) remained unaffected. PD-74 proved to be most effective in four out of five Ewing sarcoma cell lines tested. Cells were grown in 10% FBS conditions and cell proliferation was measured after 72 h using a Resazurin assay.
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S8721 |
PDGFR inhibitor 1PDGFR inhibitor 1是一种具有口服活性的Kit (c-Kit)和PDGFR抑制剂,具有潜在的抗肿瘤活性。它还能抑制好几种其他激酶,包括VEGFR2、TIE2、PDGFR-beta和CSF1R,因此进而抑制肿瘤细胞的生长。 |
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S7688 |
Ki20227Ki20227 是一种口服活性的 c-Fms tyrosine kinase(CSF1R) 的高选择性抑制剂,对 c-Fms、vascular endothelial growth factor receptor-2 (KDR/VEGFR-2)、stem cell factor receptor (c-Kit) 和 platelet-derived growth factor receptor beta (PDGFRβ) 的IC50值为2 nM、12 nM、451 nM和217 nM。 |
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S7765 |
Dovitinib (TKI258) LactateDovitinib (TKI258, CHIR258) Lactate是Dovitinib的乳酸盐,Dovitinib是一种多靶点的PTK抑制剂,主要对第III类(FLT3/c-Kit)发挥作用,IC50为1 nM/2 nM,对第IV 类(FGFR1/3)和第V 类(VEGFR1-4) RTKs也有效,IC50为8-13 nM,对InsR,EGFR,c-Met,EphA2,Tie2,IGFR1 和HER2作用较差。Phase 4。 |
![]() ![]() (c) Percent survival for the AGS cancer cell line is shown with FGFR2 inhibitors of varying specificity. (d) The KatoIII diffuse gastric cancer cell line was treated with FGFR2 inhibitors of varying specificity. The Y-axis depicts percent survival versus the X-axis with log concentrations. In all panels, error bars represent standard error of the mean. The difference in percent cell survival between KatoIII and AGS cells was statistically significant (P <0.05) at the three highest concentrations of all drugs, except Brivanib which was only significant at the highest concentration. |
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S5272 |
Toceranib phosphateToceranib phosphate (Palladia, SU11654), the phosphate salt of toceranib, is a selective inhibitor of the tyrosine kinase activity of several members of the split kinase RTK family, including Flk-1/KDR, PDGFR, and Kit with Ki values of 6 nM and 5 nM for Flk-1/KDR and PDGFRβ, respectively. |
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S5240 |
Lenvatinib (E7080) MesylateLenvatinib Mesylate (E7080)是一种合成、具有口服活性的 tyrosine kinase 的抑制剂,可抑制血管内皮生长因子受体(VEGFR1-3),成纤维细胞生长因子受体(FGFR1-4),血小板衍生生长因子受体(PDGFRα),干细胞因子受体(Kit (c-Kit)),并在转染过程中重新排列(RET (c-RET))。甲磺酸来伐替尼具有潜在的抗肿瘤活性。 |
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S4947 |
Regorafenib HydrochlorideRegorafenib (Stivarga, BAY 73-4506) Hydrochloride 是一种多靶点抑制剂,对 VEGFR1、Murine VEGFR2/3、PDGFRβ、Kit (c-Kit)、RET (c-RET) 和 Raf-1 的IC50值分别为13 nM、4.2 nM/46 nM、22 nM、7 nM、1.5 nM和2.5 nM。 |
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S4018 |
Sennoside BSennoside B,一种从大黄根茎中分离得到的刺激性泻药,抑制PDGF刺激的细胞增殖。 |
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S8401 |
Erdafitinib (JNJ-42756493)Erdafitinib (JNJ-42756493)是有效的、具有选择性和口服生物活性的泛成纤维细胞生长因子受体FGFR抑制剂,具有潜在的抗肿瘤活性。Erdafitinib 也能结合RET (c-RET)、CSF-1R、PDGFR-α/PDGFR-β、FLT4、Kit (c-Kit)和VEGFR-2并可诱导细胞凋亡。 |
![]() ![]() E, Continuous ERK phosphorylation in FGFR inhibitor resistant cells under 24-hour treatment with 1 μmol/L BGJ398 assessed by immunoblotting. FGFR inhibitors: AZD4547, BGJ398, and JNJ-42756493 |
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S6526 |
SKLB 610SKLB-610是一种多靶点的酪氨酸激酶 (tyrosine kinases)抑制剂。它对VEGFR2的抑制作用最为有效,是FGFR2和PDGFR的弱抑制剂。 |
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S7781 |
Sunitinib (SU11248)Sunitinib (SU11248) 是一种多靶点 RTK 抑制剂,以VEGFR2(Flk-1)和PDGFRβ为靶点,IC50为80 nM 和 2 nM,对c-Kit也有抑制作用。Sunitinib 还是 IRE1α 的自磷酸化活性的剂量依赖性抑制剂。 舒尼替尼可诱导自噬和细胞凋亡。 |
![]() ![]() Autophagy inhibition blocks the antiproliferative effects of sunitinib and sorafenib but not AZD6244. Medullary thyroid cancer–1.1 (MTC-1.1) and TT cells were transfected transiently with scrambled or autophagy protein 5 (Atg-5) small inter fering RNA. After transfection, cells with and without Atg-5 knockdown were exposed to sunitinib (50 nM), sorafenib (10 nM), and AZD6244 (30 nM) for 48 hours. Treated cells were subjected to a 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium proliferation assay. Similar experiments were repeated 3 times. Histograms represent the relative percent of OD490 nM absorbance. The asterisk indicates significance versus scrambled small inter fering RNA–treated control ( P < .05). All data are relative multiples of expression compared to untreated cells. The data are representative of 3 experiments and are expressed as the mean ± the standard error. |
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S6843 |
X-82 (Vorolanib)X-82 (Vorolanib, CM082)是一种口服的 vascular endothelial growth factor receptor (VEGFR) 和 platelet-derived growth factor receptor (PDGFR) 的多激酶双重抑制剂,并具有抗血管生成和抗肿瘤的活性。 |
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S8757 |
Ripretinib (DCC-2618)DCC-2618是一种具有口服活性的Kit (c-Kit)和PDGFR-alpha抑制剂,对WT Kit (c-Kit)、V654A Kit (c-Kit)、T670I Kit (c-Kit)、D816H Kit (c-Kit)和D816V Kit (c-Kit)的IC50分别为4 nM、8 nM、18 nM、5 nM和14 nM。 |
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S8780 |
AZD3229AZD3229是一种有效的泛Kit (c-Kit) mutant抑制剂,在Kit (c-Kit)突变体所驱动的Ba/F3细胞系中,GI50为1-50 nM。它还能抑制PDGFR突变体 (Tel-PDGFRα, Tel-PDGFRβ, V561D/D842V)。 |
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S8161 |
ON123300ON123300是有效的多靶点激酶抑制剂,对CDK4, Ark5/NUAK1, PDGFRβ, FGFR1, RET (c-RET), Fyn的IC50分别为3.9 nM, 5 nM, 26 nM, 26 nM, 9.2 nM和11nM。 |
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S8553 |
Avapritinib (BLU-285)Avapritinib (BLU-285)是一种小分子激酶抑制剂,可有效抑制PDGFRα D842V突变体的活性、在细胞背景下抑制PDGFRα D842V自我磷酸化(IC50=30 nM);同时也是Kit (c-Kit)突变(Kit (c-Kit) D816V)的抑制剂(IC50=0.5 nM)。 |
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S7003 |
AZD2932AZD2932 是一种有效的多靶点蛋白酪氨酸激酶抑制剂,对VEGFR-2,PDGFRβ,Flt-3,和 c-Kit 的 IC50 分别为 8 nM,4 nM,7 nM,和 9 nM。 |
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S5234 |
Nintedanib Ethanesulfonate SaltNintedanib (Intedanib, BIBF 1120) is a small molecule tyrosine-kinase inhibitor with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β, respectively. |
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S5077 |
Regorafenib (BAY-734506) MonohydrateRegorafenib (BAY-734506, Fluoro-sorafenib, Resihance, Stivarga) Monohydrate 是一种新型口服的多重激酶抑制剂,对VEGFR1、小鼠VEGFR2、小鼠VEGFR3、PDGFR-β、Kit (c-Kit)、RET (c-RET)、RAF-1、B-RAF和B-RAF(V600E)的IC50分别为13, 4.2, 46, 22, 7, 1.5, 2.5, 28, 19 nM。 |
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S4736 |
TrapidilTrapidil (Rocornal, Trapymin, Avantrin, Trapymine) 是PDGF的拮抗剂,可以抑制生成PDGF的神经胶质瘤细胞的增殖。 |
目录号 | 产品描述 | 文献引用 | 实验数据 |
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S1040 |
Sorafenib (BAY 43-9006) tosylateSorafenib (BAY 43-9006) tosylate是Raf-1和B-Raf的多重激酶抑制剂,无细胞试验中IC50分别为6 nM和22 nM。Sorafenib 还可抑制VEGFR-2、VEGFR-3、PDGFR-β、Flt-3和c-KIT,对应的IC50值分别为90 nM、20 nM、57 nM、59 nM和68 nM。Sorafenib Tosylate 可诱导autophagy、apoptosis并激活ferroptosis,并具有抗肿瘤活性。 |
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Inhibition of breast cancer cell growth using sorafenib. MCF-7 breast cancer cells were treated with increasing concentrations of sorafenib for 5 days. Cell number was measured using a colorimetric growth assay (crystal violet stain) and expressed relative to DMSO treated control cells. |
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S1026 |
Imatinib (STI571) MesylateImatinib Mesylate (STI571, CGP-57148B)是一种口服生物有效的Imatinib甲磺酸盐,是一种多靶点抑制剂,作用于v-Abl,c-Kit和PDGFR,在无细胞和细胞试验中,IC50分别为0.6 μM,0.1 μM 和0.1 μM。Imatinib Mesylate (STI571) 可诱导自噬。 |
![]() ![]() THOC5 phospho-Y225 levels were assessed in the populations shown by flow cytometry following 24 h treatment with 5 μM imatinib, 150 nM dasatinib or 5 μM nilotinib. Results are displayed as mean fluorescence intensity (n= 4) ±s.e.m. |
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S1042 |
Sunitinib (SU11248) malateSunitinib (SU11248) malate是一种多靶点RTK抑制剂,作用于VEGFR2 (Flk-1)和 PDGFRβ,在无细胞试验中IC50分别为80 nM 和2 nM,也会抑制c-Kit的活性。Sunitinib Malate 可有效地抑制 Ire1α 的自身磷酸化。Sunitinib Malate 可增加 death receptor 和 线粒体依赖的凋亡 mitochondrial-dependent apoptosis。 |
![]() ![]() Autophagy inhibition blocks the antiproliferative effects of sunitinib and sorafenib but not AZD6244. Medullary thyroid cancer–1.1 (MTC-1.1) and TT cells were transfected transiently with scrambled or autophagy protein 5 (Atg-5) small inter fering RNA. After transfection, cells with and without Atg-5 knockdown were exposed to sunitinib (50 nM), sorafenib (10 nM), and AZD6244 (30 nM) for 48 hours. Treated cells were subjected to a 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium proliferation assay. Similar experiments were repeated 3 times. Histograms represent the relative percent of OD490 nM absorbance. The asterisk indicates significance versus scrambled small inter fering RNA–treated control ( P < .05). All data are relative multiples of expression compared to untreated cells. The data are representative of 3 experiments and are expressed as the mean ± the standard error. |
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S1490 |
Ponatinib (AP24534)Ponatinib (AP24534)是一种新型有效的多靶点抑制剂,在无细胞试验中作用于Abl,PDGFRα,VEGFR2,FGFR1和Src,IC50分别为0.37 nM,1.1 nM,1.5 nM,2.2 nM和5.4 nM。Ponatinib (AP24534)可抑制自噬。 |
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RCH-ACV cells were treated with ponatinib(50 nM), PCI-32765(50 nM), or BMS-599626(500 nM) over a time course, and whole-cell extracts were subjected to immunoblot analysis for total or phospho-AKT. |
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S1005 |
Axitinib (AG 013736)Axitinib (AG 013736)是一种多靶点抑制剂,作用于 VEGFR1,VEGFR2,VEGFR3,PDGFRβ和c-Kit,在猪主动脉内皮细胞中IC50分别为0.1 nM,0.2 nM,0.1-0.3 nM,1.6 nM和1.7 nM。 |
![]() ![]() Secondary assay development. The invasive potential of MDA-MB-231 spheroids was measured using modified Boyden chambers coated with Matrigel™. Invading cells were fixed, stained with DAPI, and quantified by fluorescence microscopy using 5 random fields per filter insert in triplicate. U0126, PF2341066, axitinib, and PKC412 inhibited the invasive potential of MDA-MB-231 spheroids by ~90% as compared to untreated spheroids (UT). ***p ≤ 0.001. IGF1R and dasatinib displayed no statistical difference as compared to UT MDA-MB-231 spheroids. |
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S9973New |
Flumatinib (HH-GV-678)Flumatinib (HH-GV-678) 是一种新型 Bcr-Abl 抑制剂,对 c-Abl、PDGFRβ 和 c-Kit 的 IC50 值分别为 1.2 nM、307.6 nM 和 665.5 nM。 |
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E0050New |
Seralutinib (GB002)Seralutinib (PK10571, GB002) 是一种新型 PDGFR 激酶抑制剂,在酶测定中对 PDGFRα 和 PDGFRβ 的 IC50 分别为 8 nM 和 10 nM。 |
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S2475 |
Imatinib (STI571)Imatinib (STI571, CGP057148B, ST-1571)是一种多靶点酪氨酸激酶抑制剂,抑制v-Abl、c-Kit和PDGFR的IC50分别为0.6,0.1和0.1 μM。Imatinib (STI571) 可诱导自噬。 |
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Inhibition of thymidine (a and b) and cytarabine (c and d) uptake with imatinib. K562 cells (a and c) and MEG-01 cells (b and d) were incubated at 37 ◦C for 15 min with imatinib transport buffer, and then incubated with 0.5 Ci of [3H] thymidine or [3H] cytarabine for an additional 5 min in presence of imatinib. Cells were then washed 3 times, lysed and radioactivity associated to cell pellets was quantified. DMSO, dimethylsulfoxide; DPD, dipyridamole. |
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S1111 |
Foretinib (GSK1363089)Foretinib (GSK1363089, EXEL-2880, XL-880, GSK089) 是一种ATP竞争性的HGFR和VEGFR抑制剂,对Met (c-Met)和KDR作用最强,在无细胞试验中IC50分别为0.4 nM和0.9 nM。对Ron, Flt-1/3/4, Kit (c-Kit), PDGFRα/β和Tie-2作用效果稍弱,对FGFR1和EGFR几乎没有抑制活性。Phase 2。 |
![]() ![]() c-MET/RON inhibitors restore sensitivity to lapatinib in SK-BR-3-LR cells. Cell growth was determined using the sulforhodamine B assay. The concentration used was 0.1 uM for crizotinib, MGCD-265, XL880, sunitinib, dasatinib, and TAE-684I. The phosphorylation of HER2, AKT and ERK1/2 was determined by Western blotting.
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S1010 |
Nintedanib (BIBF 1120)Nintedanib (BIBF 1120, Intedanib, Vargatef, Ofev) 尼达尼布是一种有效的三重血管激酶抑制剂,作用于VEGFR1/2/3, FGFR1/2/3和PDGFRα/β,在无细胞试验中IC50分别为34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM和59 nM/65 nM。Phase 3。 |
![]() ![]() Effect of BIBF 1120 on the accumulation of doxorubicin (Dox) and rhodamine 123. The accumulations of doxorubicin a, b and rhodamine 123 c, d were measured by flow cytometric analysis as described in "Materials and Methods". The results are presented as fold change in fluorescence intensity relative to control MDR cells. Columns, means of triplicate determinations; bars, SDs. **P<0.01 versus control group |
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S1178 |
Regorafenib (BAY 73-4506)Regorafenib (BAY 73-4506, Fluoro-Sorafenib, Resihance, Stivarga) 是一个多靶点抑制剂,作用于VEGFR1,VEGFR2,VEGFR3,PDGFR-β,Kit (c-Kit),RET (c-RET)和Raf-1,在无细胞试验中IC50分别是13 nM,4.2 nM,46 nM,22 nM,7 nM,1.5 nM和2.5 nM。Regorafenib 可诱导自噬。 |
![]() ![]() Hepatoma cells 24 h after plating were treated with vehicle (DMSO), regorafenib (REGO, 0.5 µM), PDE5 inhibitor (sildenafil, 2 µM); or the drugs in combination. 24 hours after treatment cells were isolated and viability determined by trypan blue (n=3, SEM). *P 0.05
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S1035 |
Pazopanib HCl (GW786034 HCl)Pazopanib HCl (GW786034 HCl)是一种新型多靶点抑制剂,作用于VEGFR1,VEGFR2,VEGFR3,PDGFR,FGFR,c-Kit和c-fms,在无细胞试验中IC50分别是10 nM,30 nM,47 nM,84 nM,74 nM,140 nM和146 nM。Pazopanib 可诱导自噬II型细胞死亡。 |
![]() ![]() Effect of HDIL-2/TKI on apoptosis of RCC cells. Three RCC cell lines treated with different concentrations of Pazopanib and HDIL-2 and incubated for 48 h. Microscopic images show apoptotic materials 48 h following treatment (arrows show the apoptotic materials in the pazopanib-treated cells).
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S1017 |
Cediranib (AZD2171)Cediranib (AZD2171, NSC-732208)是一种高效的VEGFR(KDR)抑制剂,IC50为<1 nM,同时也抑制Flt1/4,IC50为5 nM/≤3 nM,此外对c-Kit和PDGFRβ也具有相似的抑制活性,对VEGFR的选择性比PDGFR-α, CSF-1R和Flt3分别高36倍, 110倍 和1000倍以上。Cediranib (AZD2171)可诱导自噬小体累积。Phase 3。 |
![]() ![]() Western blots of EZH2 expression in A549, HCC461, and HCC4006 cells upon treatment with different doses of VEGFR-2-inhibitor AZD2171 (0, 5 and 10 nM). AZD2171 decreased the expression of EZH2 in HCC4006 and HCC461 cells expressing VEGFR-2 in a dose-dependent manner but did not do so in A549 cells lacking expression of VEGFR-2.
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S1018 |
Dovitinib (TKI-258)Dovitinib (TKI-258, CHIR-258)是一种多靶点的RTK抑制剂,在无细胞试验中对III型(FLT3/c-Kit)作用最强,IC50为1 nM/2 nM,同时也作用于IV类(FGFR1/3)和V类(VEGFR1-4) RTKs,IC50为8-13 nM,但对InsR,EGFR,c-Met,EphA2,Tie2,IGF-1R和HER2作用较弱。Phase 4。 |
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Orthotopic xenografts of HNSCC cell lines (A) SCC-1 and (B) OSC-19 were treated with dovitinib (20 mg/kg/day). In addition, the OSC-19 xenografts were treated with +/ radiation therapy. Marker, mean for triplicate; bars, SE. Statistical significance by unpaired t-test, p < 0.05. |
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S1003 |
Linifanib (ABT-869)Linifanib (ABT-869, AL39324, RG3635)是一种新型有效的ATP竞争性VEGFR/PDGFR抑制剂,作用于KDR,CSF-1R,Flt-1/3和PDGFRβ,其IC50分别为4 nM,3 nM,3 nM/4 nM和66 nM,对突变激酶依赖性癌细胞(即FLT3)最有效。Linifanib (ABT-869) 可诱导自噬和凋亡。Phase 3。 |
![]() ![]() (B and C) KMCH-1 cells were plated alone (monoculture) or together with PDGF-BB-secreting LX-2 cells (co-culture) in a transwell insert co-culture system (KMCH-1 cells in the bottom wells and LX-2 cells in the inserts; 1:1 ratio) for 2 days. Cells were treated as indicated with vehicle, rhTRAIL (10 ng/ml for 6 h on day 2), rhTRAIL plus imatinib [rhTRAIL:10 ng/ml for 6 h on day 2; Imatinib: 5 μmol/L for 24 h (day2)], or rhTRAIL plus linifanib [rhTRAIL: 10 ng/ml for 6 h on day 2; Linifanib:0.5 μmol/L for 24 h (day2)]. After rhTRAIL treatment for 6 h,KMCH-1 cells were analysed for apoptotic nuclear morphology by DAPI-staining (B) and for DNA fragmentation by transferasemediated dUTP nick end labelling assay (C) with quantification of apoptotic nuclei by fluorescence microscopy. |
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S2730 |
Crenolanib (CP-868596)Crenolanib (CP-868596, ARO 002)是一种有效的,选择性PDGFRα/β抑制剂,在CHO细胞中Kd为2.1 nM/3.2 nM,也能有效抑制FLT3,对D842V突变型敏感对V561D突变型不敏感,作用于PDGFR比作用于c-Kit,VEGFR-2,TIE-2,FGFR-2,EGFR,erbB2,和Src的选择性高100倍以上。Crenolanib可辅助诱导线粒体自噬。 |
![]() ![]() Western blot analysis using 4G10 and anti-FLT3 antibody after immunoprecipitation with anti-FLT3 antibody and Western blot analysis of phospho-ERK (pERK) and ERK performed on whole cell lysates from HB119 and Molm14 cells. Cells were exposed to 100 nM crenolanib for 60 min.
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S1064 |
Masitinib (AB1010)Masitinib (AB1010)是一种新型的Kit (c-Kit)和PDGFRα/β抑制剂,IC50分别为200 nM和540 nM/800 nM,但对ABL和c-Fms抑制作用较弱。Phase 3。 |
![]() ![]() H&E stained histology slides of A), C), and E) control implants and B), D), and F) drug-loaded implants for 14, 21 and 28 day time points respectively. Location of the implants is denoted by the asterisk ‘*’. Scale bar: 200 μm.
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S1207 |
Tivozanib (AV-951)Tivozanib (AV-951, KRN-951)是一种有效的,选择性VEGFR抑制剂,作用于VEGFR1/2/3时,IC50分别为0.21 nM/0.16 nM/0.24 nM,也抑制PDGFR和c-Kit,作用于FGFR-1, Flt3, c-Met EGFR和IGF-1R活性较弱。Phase 3。 |
![]() ![]() On-chip angiogenesis assay. Fluorescence imaging of Tg(fli1a:EGFP) embryos at 64 hpf. Transgenic embryos were arrayed and immobilized at 16 hpf and continuously perfused with E3 media containing vehicle control (dimethyl sulfoxide) or selected small-molecule antiangiogenic drugs (Sunitinib and Tivozanib). Right panel: microscopic visualization of patterns of ISV. White arrows: normal ISV growth; blue arrows: partial ISV growth inhibition; and red arrows; complete ISV growth inhibition.
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S1032 |
Motesanib Diphosphate (AMG-706)Motesanib Diphosphate (AMG-706)是一种有效的ATP竞争性的VEGFR1/2/3抑制剂,IC50分别为2 nM/3 nM/6 nM;对Kit (c-Kit)具有相似的抑制活性,对VEGFR选择性比PDGFR和Ret高10倍。Phase 3。 |
![]() ![]() Immunofluorescence staining of choroidal neovascularization (CNV) lesions 14 days after laser photocoagulation. Choroidal flat mounts were fluorescently labeled with F-actin-specific marker phalloidin (green channel), endothelial cell marker CD34 (red channel), and nuclear marker DAPI (blue channel). CNV lesions in topical vehicle-treated eye (A, C, E and G) and topical motesanib-treated eye (B, D, F and H). The scale bar represents 100 um.
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S1244 |
Amuvatinib (MP-470)Amuvatinib (MP-470, HPK 56) 是一种有效的,作用于c-Kit、PDGFα和Flt3的多靶点抑制剂,IC50分别为10 nM、40 nM和81 nM。Amuvatinib 可抑制c-MET和c-RET。Amuvatinib 还具有DNA修复蛋白Rad51抑制剂及抗肿瘤的活性。Phase 2。 |
![]() ![]() Inactivation of AXL by MP470 reverses epithelial to mesenchymal transition. Immunoblot analyses of lysates from TGFβ/TNFα- treated MCF10A cells treated with varying amounts of MP470 for 72 hours.
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S1164 |
Lenvatinib (E7080)Lenvatinib (E7080)是一种多靶点抑制剂,无细胞试验中,作用于VEGFR2(KDR)/VEGFR3(Flt-4)最有效,IC50为4 nM/5.2 nM,对VEGFR1/Flt-1作用效果稍弱,作用于VEGFR2/3比作用于FGFR1, PDGFRα/β选择性高10倍左右。Lenvatinib (E7080) 也是FGFR1-4、PDGFR、Kit (c-Kit)和RET (c-RET)的抑制剂,并具有强效的抗肿瘤活性。Phase 3。 |
![]() ![]() Dot Plot Distribution of Live, Preapoptotic and Apoptotic Cells after Administration of DuP-697 and E7080 Combination.
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S1470 |
Orantinib (SU6668)Orantinib (TSU-68, SU6668)有效作用于PDGFR自磷酸化,无细胞试验中Ki为8 nM,也强效抑制Flk-1和FGFR1反式磷酸化,对IGF-1R,Met, Src,Lck,Zap70,Abl和CDK2几乎没有抑制活性;对EGFR没有抑制作用。Phase 3。 |
![]() ![]() Effect of select kinase inhibitors on DF508-CFTR maturation analyzed by immunoblotting. 293MSR-GT cells stably expressing DF508-CFTR were treated with 15 uM kinase inhibitors or 0.3% DMSO (vehicle control), as indicated, grown at 37°C for 48 h, and the appearance of the mature protein, band C, monitored by immunoblotting with anti-CFTR antibodies. Band B represents the immature protein. DMSO represents vehicle- alone control, 27°C represents temperature rescue of F508-CFTR at 27°C, 37°C represents untreated DF508-CFTR control, and WT represents WT-CFTR. Top panels depict the anti-CFTR immunoblot and bottom panels depict actin (loading) control. ** represents cellular toxicity. |
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S1181 |
ENMD-2076ENMD-2076 选择性地作用于 Aurora A 和 Flt3,IC50分别为14 nM和1.86 nM,作用于Aurora A比作用于Aurora B选择性高25倍,对RET、SRC、NTRK1/TRKA、CSF1R/FMS、VEGFR2/KDR、FGFR和PDGFRα作用效果稍弱。ENMD-2076 可抑制各种人类实体瘤和造血癌细胞系的生长,其IC50值为0.025至0.7μM,可诱导凋亡和G2/M期停滞。Phase 2。 |
![]() ![]() Breast cancer cells line MDA-MB-231 were treated with the indicated concentrations of ENMD-2076.
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S1536 |
CP-673451CP-673451是一种选择性的PDGFRα/β抑制剂,无细胞试验中IC50为10 nM/1 nM,比作用于其他血管生成受体选择性高450倍以上,具有抗血管生成和抗肿瘤活性。 |
![]() ![]() Pharmacological inhibition of PDGFR-β by cp673451 significantly attenuated the mRNA expression of BCL2A1 (E) and SERPINE (F) in ASCs.
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S1363 |
Ki8751Ki8751是一种有效的,选择性的VEGFR2抑制剂,IC50为0.9 nM,作用于VEGFR2比作用于c-Kit, PDGFRα和FGFR-2选择性高40倍以上,对EGFR, HGFR和InsR没有抑制活性。 |
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Effect of select kinase inhibitors on DF508-CFTR maturation analyzed by immunoblotting. 293MSR-GT cells stably expressing DF508-CFTR were treated with 15 uM kinase inhibitors or 0.3% DMSO (vehicle control), as indicated, grown at 37 °C for 48 h, and the appearance of the mature protein, band C, monitored by immunoblotting with anti-CFTR antibodies. Band B represents the immature protein. DMSO represents vehicle-alone control, 27 °C represents temperature rescue of F508-CFTR at 27 °C, 37 °C represents untreated DF508-CFTR control, and WT represents WT-CFTR. Top panels depict the anti-CFTR immunoblot and bottom panels depict actin (loading) control. ** represents cellular toxicity. |
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S2231 |
TelatinibTelatinib (BAY 57-9352) 是一种有效的VEGFR2/3, c-Kit和PDGFRα抑制剂,IC50分别为6 nM/4 nM, 1 nM和15 nM。Phase 2。 |
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S2622 |
PP121PP121是一种作用于PDGFR, Hck, mTOR, VEGFR2, Src和Abl的多靶点抑制剂,IC50分别为2 nM, 8 nM, 10 nM, 12 nM, 14 nM和18 nM,也抑制DNA-PK,IC50为60 nM。 |
![]() ![]() PP121 induces apoptosis in ATC cells. CAL62 cells were treated with PP121 at the indicated concentrations for 48 h, followed by PI staining. The nuclei were stained with Hoechst and analyzed using a fluorescent microscope. The representative images are shown.
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S3012 |
PazopanibPazopanib (GW786034) 是一种新型多靶点的VEGFR1,VEGFR2,VEGFR3,PDGFR,FGFR,c-Kit 和 c-Fms/CSF1R抑制剂,无细胞试验中IC50分别为10 nM,30 nM,47 nM,84 nM,74 nM,140 nM 和 146 nM。Pazopanib 可诱导 cathepsin B 的活化和自噬。 |
![]() ![]() Three RCC cell lines treated with different concentrations of TKI and HDIL-2 and incubated for 48 h. Microscopic images show apoptotic materials 48 h following treatment (arrows show the apoptotic materials in the pazopanib-treated cells).
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S7397 |
Sorafenib (BAY 43-9006)Sorafenib (BAY 43-9006, NSC-724772)是Raf-1和B-Raf的多重激酶抑制剂,无细胞试验中IC50分别为6 nM和22 nM。Sorafenib 还可抑制VEGFR-2、VEGFR-3、PDGFR-β、Flt-3和c-KIT,对应的IC50值分别为90 nM、20 nM、57 nM、59 nM和68 nM。Sorafenib 可诱导autophagy、apoptosis并激活ferroptosis,Sorafenib 具有抗肿瘤活性。 |
![]() ![]() Involvement of EV linc-VLDLR in tumor cell responses to chemotherapy. Cells were incubated with sorafenib, camptothecin, or doxorubicin. EVs were obtained after 24 hours, and qRT-PCR was performed for linc-VLDLR. The bars represent the mean ?SEM of the increase in cell viability from 3 independent studies. *, P < 0.05.
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S2774 |
MK-2461MK-2461是一种有效的,多靶点抑制剂,作用于c-Met(WT/mutants),IC50为0.4-2.5 nM,对Ron,和Flt1作用效果稍弱;作用于c-Met比作用于FGFR1, FGFR2, FGFR3, PDGFRβ, KDR, Flt3, Flt4, TrkA和TrkB选择性高8到30倍。Phase 1/2。 |
![]() ![]() Both V-H cells and V-J cells are treated with MK-2461, XL-184 or ABT-869, respectively. (i-k) Western blot analysis of sFlt-1 expression after incubation with three VEGF-A receptor inhibitors or in the control.
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S8024 |
Tyrphostin AG 1296Tyrphostin AG 1296 是一种PDGFR抑制剂,IC50为0.3-0.5 μM,对EGFR没有抑制活性。Tyrphostin AG1296 在抑制Swiss 3T3细胞中抑制 FGFR 和 c-Kit 的IC50值为12.3 μM和1.8 μM。Tyrphostin AG1296 可在A375R细胞中诱导剧烈的凋亡。 |
![]() ![]() After inoculation with KAT4 cells, administration of compounds including MK-2206 (100 mg/kg), tyrphostin AG 1296 (100 mg/kg), or a combination of MK-2206 (100 mg/kg) and tyrphostin AG 1296 (100 mg/kg) was performed. The combination of MK-2206 and tyrphostin AG 1296 induced significant apoptosis of KAT4 tumor cells in vivo measured by the terminal deoxynucleotidyl transferase dUTP nick end labeling assay (green), and nuclei were stained with Hoechst (blue). |
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S8015 |
Agerafenib (RXDX-105)Agerafenib (RXDX-105, CEP-32496) 是一种高度有效的BRAF(V600E/WT)和c-Raf抑制剂,Kd为14 nM/36 nM和39 nM,适度有效作用于Abl-1, c-Kit, RET (c-RET), PDGFRβ和VEGFR2,对MEK-1, MEK-2, ERK-1和ERK-2具有微弱的亲和力。Phase 1/2。 |
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S2895 |
Tyrphostin 9Tyrphostin 9 (SF 6847, RG-50872) 是第一个EGFR抑制剂,IC50为460 μM,作用于PDGFR更有效,IC50为0.5μM。 |
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S0504 |
SU14813SU14813 (SU 014813)是一种多受体 tyrosine kinase 的抑制剂,对于 VEGFR2、VEGFR1、PDGFRβ 和 Kit (c-Kit) 的IC50值分别为50 nM,2 nM,4 nM和15 nM。SU14813 具有强大的抗血管生成和抗肿瘤活性。 |
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S7667 |
SU5402SU5402是一种有效的多靶点受体激酶抑制剂,对VEGFR2,FGFR1,和PDGF-Rβ的IC50分别为20 nM,30 nM,和510 nM。 |
![]() ![]() Four FGFR inhibitors, namely PD-173074 (PD-74), PD-166866 (PD-66), SU5402 (SU54) and NVP-BGJ398 (BG-98), inhibit A673, SKNMC, POE, RDES and SKES Ewing cell growth in vitro in a dose-dependent manner, whereas normal cells (IMR90 fibroblasts) remained unaffected. PD-74 proved to be most effective in four out of five Ewing sarcoma cell lines tested. Cells were grown in 10% FBS conditions and cell proliferation was measured after 72 h using a Resazurin assay.
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S8721 |
PDGFR inhibitor 1PDGFR inhibitor 1是一种具有口服活性的Kit (c-Kit)和PDGFR抑制剂,具有潜在的抗肿瘤活性。它还能抑制好几种其他激酶,包括VEGFR2、TIE2、PDGFR-beta和CSF1R,因此进而抑制肿瘤细胞的生长。 |
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S7688 |
Ki20227Ki20227 是一种口服活性的 c-Fms tyrosine kinase(CSF1R) 的高选择性抑制剂,对 c-Fms、vascular endothelial growth factor receptor-2 (KDR/VEGFR-2)、stem cell factor receptor (c-Kit) 和 platelet-derived growth factor receptor beta (PDGFRβ) 的IC50值为2 nM、12 nM、451 nM和217 nM。 |
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S7765 |
Dovitinib (TKI258) LactateDovitinib (TKI258, CHIR258) Lactate是Dovitinib的乳酸盐,Dovitinib是一种多靶点的PTK抑制剂,主要对第III类(FLT3/c-Kit)发挥作用,IC50为1 nM/2 nM,对第IV 类(FGFR1/3)和第V 类(VEGFR1-4) RTKs也有效,IC50为8-13 nM,对InsR,EGFR,c-Met,EphA2,Tie2,IGFR1 和HER2作用较差。Phase 4。 |
![]() ![]() (c) Percent survival for the AGS cancer cell line is shown with FGFR2 inhibitors of varying specificity. (d) The KatoIII diffuse gastric cancer cell line was treated with FGFR2 inhibitors of varying specificity. The Y-axis depicts percent survival versus the X-axis with log concentrations. In all panels, error bars represent standard error of the mean. The difference in percent cell survival between KatoIII and AGS cells was statistically significant (P <0.05) at the three highest concentrations of all drugs, except Brivanib which was only significant at the highest concentration. |
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S5272 |
Toceranib phosphateToceranib phosphate (Palladia, SU11654), the phosphate salt of toceranib, is a selective inhibitor of the tyrosine kinase activity of several members of the split kinase RTK family, including Flk-1/KDR, PDGFR, and Kit with Ki values of 6 nM and 5 nM for Flk-1/KDR and PDGFRβ, respectively. |
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S5240 |
Lenvatinib (E7080) MesylateLenvatinib Mesylate (E7080)是一种合成、具有口服活性的 tyrosine kinase 的抑制剂,可抑制血管内皮生长因子受体(VEGFR1-3),成纤维细胞生长因子受体(FGFR1-4),血小板衍生生长因子受体(PDGFRα),干细胞因子受体(Kit (c-Kit)),并在转染过程中重新排列(RET (c-RET))。甲磺酸来伐替尼具有潜在的抗肿瘤活性。 |
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S4947 |
Regorafenib HydrochlorideRegorafenib (Stivarga, BAY 73-4506) Hydrochloride 是一种多靶点抑制剂,对 VEGFR1、Murine VEGFR2/3、PDGFRβ、Kit (c-Kit)、RET (c-RET) 和 Raf-1 的IC50值分别为13 nM、4.2 nM/46 nM、22 nM、7 nM、1.5 nM和2.5 nM。 |
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S4018 |
Sennoside BSennoside B,一种从大黄根茎中分离得到的刺激性泻药,抑制PDGF刺激的细胞增殖。 |
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S8401 |
Erdafitinib (JNJ-42756493)Erdafitinib (JNJ-42756493)是有效的、具有选择性和口服生物活性的泛成纤维细胞生长因子受体FGFR抑制剂,具有潜在的抗肿瘤活性。Erdafitinib 也能结合RET (c-RET)、CSF-1R、PDGFR-α/PDGFR-β、FLT4、Kit (c-Kit)和VEGFR-2并可诱导细胞凋亡。 |
![]() ![]() E, Continuous ERK phosphorylation in FGFR inhibitor resistant cells under 24-hour treatment with 1 μmol/L BGJ398 assessed by immunoblotting. FGFR inhibitors: AZD4547, BGJ398, and JNJ-42756493 |
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S6526 |
SKLB 610SKLB-610是一种多靶点的酪氨酸激酶 (tyrosine kinases)抑制剂。它对VEGFR2的抑制作用最为有效,是FGFR2和PDGFR的弱抑制剂。 |
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S7781 |
Sunitinib (SU11248)Sunitinib (SU11248) 是一种多靶点 RTK 抑制剂,以VEGFR2(Flk-1)和PDGFRβ为靶点,IC50为80 nM 和 2 nM,对c-Kit也有抑制作用。Sunitinib 还是 IRE1α 的自磷酸化活性的剂量依赖性抑制剂。 舒尼替尼可诱导自噬和细胞凋亡。 |
![]() ![]() Autophagy inhibition blocks the antiproliferative effects of sunitinib and sorafenib but not AZD6244. Medullary thyroid cancer–1.1 (MTC-1.1) and TT cells were transfected transiently with scrambled or autophagy protein 5 (Atg-5) small inter fering RNA. After transfection, cells with and without Atg-5 knockdown were exposed to sunitinib (50 nM), sorafenib (10 nM), and AZD6244 (30 nM) for 48 hours. Treated cells were subjected to a 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium proliferation assay. Similar experiments were repeated 3 times. Histograms represent the relative percent of OD490 nM absorbance. The asterisk indicates significance versus scrambled small inter fering RNA–treated control ( P < .05). All data are relative multiples of expression compared to untreated cells. The data are representative of 3 experiments and are expressed as the mean ± the standard error. |
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S6843 |
X-82 (Vorolanib)X-82 (Vorolanib, CM082)是一种口服的 vascular endothelial growth factor receptor (VEGFR) 和 platelet-derived growth factor receptor (PDGFR) 的多激酶双重抑制剂,并具有抗血管生成和抗肿瘤的活性。 |
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S8757 |
Ripretinib (DCC-2618)DCC-2618是一种具有口服活性的Kit (c-Kit)和PDGFR-alpha抑制剂,对WT Kit (c-Kit)、V654A Kit (c-Kit)、T670I Kit (c-Kit)、D816H Kit (c-Kit)和D816V Kit (c-Kit)的IC50分别为4 nM、8 nM、18 nM、5 nM和14 nM。 |
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S8780 |
AZD3229AZD3229是一种有效的泛Kit (c-Kit) mutant抑制剂,在Kit (c-Kit)突变体所驱动的Ba/F3细胞系中,GI50为1-50 nM。它还能抑制PDGFR突变体 (Tel-PDGFRα, Tel-PDGFRβ, V561D/D842V)。 |
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S8161 |
ON123300ON123300是有效的多靶点激酶抑制剂,对CDK4, Ark5/NUAK1, PDGFRβ, FGFR1, RET (c-RET), Fyn的IC50分别为3.9 nM, 5 nM, 26 nM, 26 nM, 9.2 nM和11nM。 |
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S8553 |
Avapritinib (BLU-285)Avapritinib (BLU-285)是一种小分子激酶抑制剂,可有效抑制PDGFRα D842V突变体的活性、在细胞背景下抑制PDGFRα D842V自我磷酸化(IC50=30 nM);同时也是Kit (c-Kit)突变(Kit (c-Kit) D816V)的抑制剂(IC50=0.5 nM)。 |
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S7003 |
AZD2932AZD2932 是一种有效的多靶点蛋白酪氨酸激酶抑制剂,对VEGFR-2,PDGFRβ,Flt-3,和 c-Kit 的 IC50 分别为 8 nM,4 nM,7 nM,和 9 nM。 |
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S5234 |
Nintedanib Ethanesulfonate SaltNintedanib (Intedanib, BIBF 1120) is a small molecule tyrosine-kinase inhibitor with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β, respectively. |
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S5077 |
Regorafenib (BAY-734506) MonohydrateRegorafenib (BAY-734506, Fluoro-sorafenib, Resihance, Stivarga) Monohydrate 是一种新型口服的多重激酶抑制剂,对VEGFR1、小鼠VEGFR2、小鼠VEGFR3、PDGFR-β、Kit (c-Kit)、RET (c-RET)、RAF-1、B-RAF和B-RAF(V600E)的IC50分别为13, 4.2, 46, 22, 7, 1.5, 2.5, 28, 19 nM。 |
目录号 | 产品描述 | 文献引用 | 实验数据 |
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S4736 |
TrapidilTrapidil (Rocornal, Trapymin, Avantrin, Trapymine) 是PDGF的拮抗剂,可以抑制生成PDGF的神经胶质瘤细胞的增殖。 |