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所有产品 PDGFR抑制剂(36) PDGFR拮抗剂(1) 新PDGFR产品

产品目录	产品描述	文献引用	实验数据
S1040	Sorafenib Tosylate Sorafenib Tosylate是一种酪氨酸激酶(VEGFR和PDGFR)和RAF/MEK/ERK级联抑制剂，同时作用于Raf-1，^wtBRAF和^V599EBRAF，IC50分别为6 nM， 22 nM和38 nM。	Cancer Lett, 2019, 454:14-25 J Exp Clin Cancer Res, 2019, 38(1):204 Am J Cancer Res, 2019, 9(5):906-926	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.
S1026	Imatinib Mesylate (STI571) Imatinib Mesylate (STI571)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。	Eur J Pharmacol, 2019, 17:172559 Cancer Invest, 2019, 37(2):99-112 Cell Metab, 2018, 28(6):817-832	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.
S1042	Sunitinib Malate Sunitinib 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。	FASEB J, 2019, 33(1):1347-1359 Theranostics, 2018, 8(1):141-155 J Lipid Res, 2018, 59(11):2188-2201	Sunitinib decreases FLT-3 and RET phosphor ylation but increases ERK phosphorylation in a time-dependent manner. H295R and SW13 cells were treated with sunitinib (10 nM) for various time points as indi-cated. Cell lysates were prepared and phospho-FLT-3, RET, and ERK levels were monitored by Western Blot-ting. Re-probing against FLT-3, RET, and ERK was done to ensure equal protein loading.
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。	Nat Commun, 2019, 10(1):2701 Cell Rep, 2019, 26(1):65-78 Front Oncol, 2019, 9:103	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.
S1005	Axitinib Axitinib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。	Lab Chip, 2019, 19(12):2071-2080 J Cell Physiol, 2019, 10.1002/jcp.28810 Assay Drug Dev Technol, 2019, 17(4):167-177	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.
S6526^New	SKLB 610 SKLB-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。
S8780^New	AZD3229 AZD3229是一种有效的泛KIT mutant抑制剂，在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)。
S8757^New	Ripretinib (DCC-2618) DCC-2618是一种具有口服活性的KIT和PDGFR-alpha抑制剂，对WT KIT、V654A KIT、T670I KIT、D816H KIT和D816V KIT的IC50分别为4 nM、8 nM、18 nM、5 nM和14 nM。
S2475	Imatinib (STI571) Imatinib (STI571)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。	Haematologica, 2019, 10.3324/haematol.2019.215939 Mol Cancer Ther, 2019, 18(6):1137-1148 Cancer Manag Res, 2019, 11:5197-5208	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.
S1010	Nintedanib (BIBF 1120) Nintedanib (BIBF 1120) 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。	J Clin Med, 2019, 8(3) J Cancer, 2019, 10(4):1004-1012 PLoS Negl Trop Dis, 2019, 13(3):e0006959	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
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。	J Pharm Sci, 2019, 108(3):1272-1283 Clin Exp Hypertens, 2018, 40(6):524-533 J Cell Physiol, 2016, 231(10):2286-302	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).
S1018	Dovitinib (TKI-258, CHIR-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。	Exp Dermatol, 2019, 10.1111/exd.14010 Amino Acids, 2016, 48(7):1591-9 Mol Cells, 2016, 39(5):389-94	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.
S1003	Linifanib (ABT-869) Linifanib (ABT-869)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。Phase 3。	Leuk Res, 2019, 78:12-20 Sci Rep, 2016, 6:31589 Sci Rep, 2016, 6:29382	(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.
S2730	Crenolanib (CP-868596) Crenolanib (CP-868596)是一种有效的，选择性PDGFRα/β抑制剂，在CHO细胞中K_d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。	Nature, 2019, 572(7769):335-340 Br J Cancer, 2019, 121(2):139-149 Blood, 2018, 132(1):67-77.	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.
S1064	Masitinib (AB1010) Masitinib (AB1010)是一种新型的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。	Mol Cell Endocrinol, 2018, 470:75-83 Hepatology, 2016, 64(2):488-500 Biosens Bioelectron, 2016, 77:149-56	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.
S1207	Tivozanib (AV-951) Tivozanib (AV-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。	Biol Open, 2018, 7(6) Arch Biochem Biophys, 2016, 607:37-43 J Med Chem, 2015,	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.
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具有相似的抑制活性，对VEGFR选择性比PDGFR和Ret高10倍。Phase 3。	Cell Stem Cell, 2019, 25(1):69-86 Int J Cardiol, 2015, 183C:221-231 J Ocul Pharmacol Ther, 2015, 31(1):25-31	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.
S1244	Amuvatinib (MP-470) Amuvatinib (MP-470)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。Phase 2。	Oncotarget, 2016, 7(15):19620-30 J Pathol, 2015, 237(1):14-24 Cancer Res, 2014, 74(20):5878-90	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.
S1470	Orantinib (TSU-68, SU6668) Orantinib (TSU-68, SU6668)有效作用于PDGFR自磷酸化，无细胞试验中K_i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。	Cell Physiol Biochem, 2017, 41(6):2350-2362 Cell Calcium, 2016, 60(1):1-12 Proc Natl Acad Sci USA, 2014, 111(44):E4706-15	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.
S1536	CP-673451 CP-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。	Cancers (Basel), 2018, 10(9) J Neurotrauma, 2018, 35(22):2718-2735 J Med Invest, 2017, 64(3.4):262-265	Pharmacological inhibition of PDGFR-β by cp673451 significantly attenuated the mRNA expression of BCL2A1 (E) and SERPINE (F) in ASCs.
S1363	Ki8751 Ki8751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。	Wound Repair Regen, 2019, 27(4):324-334 Cancer Lett, 2017, 385:12-20 Cellular Signalling, 2016, 19;28(6):652-662	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.
S2231	Telatinib Telatinib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。	Cell Stem Cell, 2019, 24(4):654-669 Clin Cancer Res, 2018, 24(11):2678-2687 Biochem Pharmacol, 2014, 89(1):52-61
S2622	PP121 PP121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。	Biochem Biophys Res Commun, 2015, 465(1):137-44 Tumour Biol, 2014, 35(9):8659-64 Int J Clin Exp Pathol, 2013, 6(10):2082-91	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.
S3012	Pazopanib Pazopanib是一种新型多靶点的VEGFR1，VEGFR2，VEGFR3，PDGFR，FGFR，c-Kit 和 c-Fms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。	Clin Cancer Res, 2018, 24(2):460-473 Arch Toxicol, 2018, 92(4):1435-1451 Cancer Res, 2017, 77(11):2927-2937	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).
S2769	Dovitinib (TKI-258) Dilactic Acid Dovitinib (TKI-258) Dilactic Acid 是一种多靶点的RTK抑制剂，作用于III型(FLT3/c-Kit)最有效，IC50为1 nM/2 nM，也有效作用于IV型(FGFR1/3)和V型(VEGFR1-4)RTKs，IC50为8-13 nM，对InsR， EGFR， c-Met， EphA2， Tie2， IGFR1和HER2作用效果稍弱。Phase 4。	Elife, 2017, 10.7554/eLife.25946 Transl Oncol, 2017, 10(3):357-366 Cancer Lett, 2016, 380(1):163-173	In vitro assays on CUX1-FGFR1-expressing Ba/F3 cells. a. IL-3 deprivation of Ba/F3 cells transduced with CUX1-FGFR1 resulted in transformation to growth factor independent growth. The mean growth ±SEM of three separate measurements over four consecutive days is presented. b. The dose-response curves of CUX1-FGFR1-transduced Ba/F3 cells, treated with TKI258 and PKC412 for 48 hours in the absence or presence of IL-3 (2 ng/ml) are presented. Points represent the average results of two experiments done in triplicate plotted with the curve-fitting GraphPad Prism 5 software; bars, SD. The calculated IC50 for each inhibitor is indicated. c. Western blot analyses of CUX1-FGFR1-transformed Ba/F3 cells after treatment with PKC412 and TKI258. Phosphorylation of CUX1-FGFR1 and its downstream effectors STAT5 and RPS6K decreased with increasing inhibitor concentrations. Expression of total CUX1-FGFR1, STAT5 and RPS6K remained unaffected. d. Effect of PKC412 and TKI258 on apoptosis of CUX1-FGFR1-expressing Ba/F3 cells after treatment for 48 hours. The percentage of apoptotic plus necrotic CUX1-FGFR1-transduced Ba/F3 cells is indicated.
S2774	MK-2461 MK-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。	Mol Cell Biochem, 2018, 449(1-2):1-8	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.
S8024	Tyrphostin AG 1296 Tyrphostin AG 1296是一种PDGFR抑制剂，IC50为0.3-0.5 μM，对EGFR没有抑制活性。	J Cell Physiol, 2018, 233(3):2067-2074 Cardiovasc Res, 2017, 113(3):310-320 Onco Targets Ther, 2014, 7:425-32	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).
S2895	Tyrphostin 9 Tyrphostin 9 是第一个EGFR抑制剂，IC50为460 μM，作用于PDGFR更有效，IC50为0.5μM。
S7765	Dovitinib (TKI258) Lactate Dovitinib (TKI258) 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。	Urol Oncol, 2018, 36(8):365 Eur J Haematol, 2017, 99(5):442-448 Amino Acids, 2016, 48(7):1591-9	(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.
S5272	Toceranib phosphate Toceranib phosphate, 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.
S4018	Sennoside B Sennoside 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。
S7781	Sunitinib Sunitinib 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。	EBioMedicine, 2019, 39:255-264 Biochem Pharmacol, 2019, 164:94-105 Leuk Res, 2019, 78:12-20	Sunitinib decreases FLT-3 and RET phosphor ylation but increases ERK phosphorylation in a time-dependent manner. H295R and SW13 cells were treated with sunitinib (10 nM) for various time points as indi-cated. Cell lysates were prepared and phospho-FLT-3, RET, and ERK levels were monitored by Western Blot-ting. Re-probing against FLT-3, RET, and ERK was done to ensure equal protein loading.
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突变（KIT D816V）的抑制剂（IC50=0.5 nM）。	Mol Pharm, 2019, 16(7):3040-3052
S7003	AZD2932 AZD2932 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。
S5234	Nintedanib Ethanesulfonate Salt Nintedanib 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.
S5077	Regorafenib Monohydrate Regorafenib 瑞戈非尼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、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。
S4736	Trapidil Trapidil是PDGF的拮抗剂，可以抑制生成PDGF的神经胶质瘤细胞的增殖。

产品目录	产品描述	文献引用	实验数据
S1040	Sorafenib Tosylate Sorafenib Tosylate是一种酪氨酸激酶(VEGFR和PDGFR)和RAF/MEK/ERK级联抑制剂，同时作用于Raf-1，^wtBRAF和^V599EBRAF，IC50分别为6 nM， 22 nM和38 nM。	Cancer Lett,2019, 454:14-25 J Exp Clin Cancer Res,2019, 38(1):204 Am J Cancer Res,2019, 9(5):906-926	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.
S1026	Imatinib Mesylate (STI571) Imatinib Mesylate (STI571)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。	Eur J Pharmacol,2019, 17:172559 Cancer Invest,2019, 37(2):99-112 Cell Metab,2018, 28(6):817-832	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.
S1042	Sunitinib Malate Sunitinib 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。	FASEB J,2019, 33(1):1347-1359 Theranostics,2018, 8(1):141-155 J Lipid Res,2018, 59(11):2188-2201	Sunitinib decreases FLT-3 and RET phosphor ylation but increases ERK phosphorylation in a time-dependent manner. H295R and SW13 cells were treated with sunitinib (10 nM) for various time points as indi-cated. Cell lysates were prepared and phospho-FLT-3, RET, and ERK levels were monitored by Western Blot-ting. Re-probing against FLT-3, RET, and ERK was done to ensure equal protein loading.
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。	Nat Commun,2019, 10(1):2701 Cell Rep,2019, 26(1):65-78 Front Oncol,2019, 9:103	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.
S1005	Axitinib Axitinib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。	Lab Chip,2019, 19(12):2071-2080 J Cell Physiol,2019, 10.1002/jcp.28810 Assay Drug Dev Technol,2019, 17(4):167-177	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.
S6526^New	SKLB 610 SKLB-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。
S8780^New	AZD3229 AZD3229是一种有效的泛KIT mutant抑制剂，在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)。
S8757^New	Ripretinib (DCC-2618) DCC-2618是一种具有口服活性的KIT和PDGFR-alpha抑制剂，对WT KIT、V654A KIT、T670I KIT、D816H KIT和D816V KIT的IC50分别为4 nM、8 nM、18 nM、5 nM和14 nM。
S2475	Imatinib (STI571) Imatinib (STI571)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。	Haematologica,2019, 10.3324/haematol.2019.215939 Mol Cancer Ther,2019, 18(6):1137-1148 Cancer Manag Res,2019, 11:5197-5208	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.
S1010	Nintedanib (BIBF 1120) Nintedanib (BIBF 1120) 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。	J Clin Med,2019, 8(3) J Cancer,2019, 10(4):1004-1012 PLoS Negl Trop Dis,2019, 13(3):e0006959	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
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。	J Pharm Sci,2019, 108(3):1272-1283 Clin Exp Hypertens,2018, 40(6):524-533 J Cell Physiol,2016, 231(10):2286-302	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).
S1018	Dovitinib (TKI-258, CHIR-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。	Exp Dermatol,2019, 10.1111/exd.14010 Amino Acids,2016, 48(7):1591-9 Mol Cells,2016, 39(5):389-94	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.
S1003	Linifanib (ABT-869) Linifanib (ABT-869)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。Phase 3。	Leuk Res,2019, 78:12-20 Sci Rep,2016, 6:31589 Sci Rep,2016, 6:29382	(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.
S2730	Crenolanib (CP-868596) Crenolanib (CP-868596)是一种有效的，选择性PDGFRα/β抑制剂，在CHO细胞中K_d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。	Nature,2019, 572(7769):335-340 Br J Cancer,2019, 121(2):139-149 Blood,2018, 132(1):67-77.	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.
S1064	Masitinib (AB1010) Masitinib (AB1010)是一种新型的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。	Mol Cell Endocrinol,2018, 470:75-83 Hepatology,2016, 64(2):488-500 Biosens Bioelectron,2016, 77:149-56	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.
S1207	Tivozanib (AV-951) Tivozanib (AV-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。	Biol Open,2018, 7(6) Arch Biochem Biophys,2016, 607:37-43 J Med Chem,2015,	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.
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具有相似的抑制活性，对VEGFR选择性比PDGFR和Ret高10倍。Phase 3。	Cell Stem Cell,2019, 25(1):69-86 Int J Cardiol,2015, 183C:221-231 J Ocul Pharmacol Ther,2015, 31(1):25-31	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.
S1244	Amuvatinib (MP-470) Amuvatinib (MP-470)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。Phase 2。	Oncotarget,2016, 7(15):19620-30 J Pathol,2015, 237(1):14-24 Cancer Res,2014, 74(20):5878-90	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.
S1470	Orantinib (TSU-68, SU6668) Orantinib (TSU-68, SU6668)有效作用于PDGFR自磷酸化，无细胞试验中K_i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。	Cell Physiol Biochem,2017, 41(6):2350-2362 Cell Calcium,2016, 60(1):1-12 Proc Natl Acad Sci USA,2014, 111(44):E4706-15	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.
S1536	CP-673451 CP-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。	Cancers (Basel),2018, 10(9) J Neurotrauma,2018, 35(22):2718-2735 J Med Invest,2017, 64(3.4):262-265	Pharmacological inhibition of PDGFR-β by cp673451 significantly attenuated the mRNA expression of BCL2A1 (E) and SERPINE (F) in ASCs.
S1363	Ki8751 Ki8751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。	Wound Repair Regen,2019, 27(4):324-334 Cancer Lett,2017, 385:12-20 Cellular Signalling,2016, 19;28(6):652-662	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.
S2231	Telatinib Telatinib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。	Cell Stem Cell,2019, 24(4):654-669 Clin Cancer Res,2018, 24(11):2678-2687 Biochem Pharmacol,2014, 89(1):52-61
S2622	PP121 PP121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。	Biochem Biophys Res Commun,2015, 465(1):137-44 Tumour Biol,2014, 35(9):8659-64 Int J Clin Exp Pathol,2013, 6(10):2082-91	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.
S3012	Pazopanib Pazopanib是一种新型多靶点的VEGFR1，VEGFR2，VEGFR3，PDGFR，FGFR，c-Kit 和 c-Fms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。	Clin Cancer Res,2018, 24(2):460-473 Arch Toxicol,2018, 92(4):1435-1451 Cancer Res,2017, 77(11):2927-2937	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).
S2769	Dovitinib (TKI-258) Dilactic Acid Dovitinib (TKI-258) Dilactic Acid 是一种多靶点的RTK抑制剂，作用于III型(FLT3/c-Kit)最有效，IC50为1 nM/2 nM，也有效作用于IV型(FGFR1/3)和V型(VEGFR1-4)RTKs，IC50为8-13 nM，对InsR， EGFR， c-Met， EphA2， Tie2， IGFR1和HER2作用效果稍弱。Phase 4。	Elife,2017, 10.7554/eLife.25946 Transl Oncol,2017, 10(3):357-366 Cancer Lett,2016, 380(1):163-173	In vitro assays on CUX1-FGFR1-expressing Ba/F3 cells. a. IL-3 deprivation of Ba/F3 cells transduced with CUX1-FGFR1 resulted in transformation to growth factor independent growth. The mean growth ±SEM of three separate measurements over four consecutive days is presented. b. The dose-response curves of CUX1-FGFR1-transduced Ba/F3 cells, treated with TKI258 and PKC412 for 48 hours in the absence or presence of IL-3 (2 ng/ml) are presented. Points represent the average results of two experiments done in triplicate plotted with the curve-fitting GraphPad Prism 5 software; bars, SD. The calculated IC50 for each inhibitor is indicated. c. Western blot analyses of CUX1-FGFR1-transformed Ba/F3 cells after treatment with PKC412 and TKI258. Phosphorylation of CUX1-FGFR1 and its downstream effectors STAT5 and RPS6K decreased with increasing inhibitor concentrations. Expression of total CUX1-FGFR1, STAT5 and RPS6K remained unaffected. d. Effect of PKC412 and TKI258 on apoptosis of CUX1-FGFR1-expressing Ba/F3 cells after treatment for 48 hours. The percentage of apoptotic plus necrotic CUX1-FGFR1-transduced Ba/F3 cells is indicated.
S2774	MK-2461 MK-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。	Mol Cell Biochem,2018, 449(1-2):1-8	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.
S8024	Tyrphostin AG 1296 Tyrphostin AG 1296是一种PDGFR抑制剂，IC50为0.3-0.5 μM，对EGFR没有抑制活性。	J Cell Physiol,2018, 233(3):2067-2074 Cardiovasc Res,2017, 113(3):310-320 Onco Targets Ther,2014, 7:425-32	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).
S2895	Tyrphostin 9 Tyrphostin 9 是第一个EGFR抑制剂，IC50为460 μM，作用于PDGFR更有效，IC50为0.5μM。
S7765	Dovitinib (TKI258) Lactate Dovitinib (TKI258) 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。	Urol Oncol,2018, 36(8):365 Eur J Haematol,2017, 99(5):442-448 Amino Acids,2016, 48(7):1591-9	(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.
S5272	Toceranib phosphate Toceranib phosphate, 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.
S4018	Sennoside B Sennoside 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。
S7781	Sunitinib Sunitinib 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。	EBioMedicine,2019, 39:255-264 Biochem Pharmacol,2019, 164:94-105 Leuk Res,2019, 78:12-20	Sunitinib decreases FLT-3 and RET phosphor ylation but increases ERK phosphorylation in a time-dependent manner. H295R and SW13 cells were treated with sunitinib (10 nM) for various time points as indi-cated. Cell lysates were prepared and phospho-FLT-3, RET, and ERK levels were monitored by Western Blot-ting. Re-probing against FLT-3, RET, and ERK was done to ensure equal protein loading.
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突变（KIT D816V）的抑制剂（IC50=0.5 nM）。	Mol Pharm,2019, 16(7):3040-3052
S7003	AZD2932 AZD2932 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。
S5234	Nintedanib Ethanesulfonate Salt Nintedanib 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.
S5077	Regorafenib Monohydrate Regorafenib 瑞戈非尼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、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。