FLT3

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抑制剂选择性比较

FLT3产品

所有产品 FLT3抑制剂(26) 新FLT3产品

目录号	产品描述	文献引用	实验数据
S2194	R406 R406是一种有效的Syk抑制剂，无细胞试验中IC50为41 nM，对Syk抑制作用强，但是不抑制Lyn，对Flt3的作用比对Syk低5倍。Phase 1。	Nat Cell Biol, 2019, 21(2):203-213 PLoS Pathog, 2019, 15(8):e1007923 PLoS One, 2019, 14(1):e0210879	Platelets (3 x 10⁸/mL) were preincubated with Y27632 (10 uM), R406 (1 uM), or a combination of Y27632 and R406 for 20 minutes followed by stimulation with oxLDL (50 ug/mL) for 15 seconds and lysis. Samples were then separated by SDS-PAGE and were immunoblotted for phospho-MLCSer19, followed by reprobing for β-tubulin. (Fi) Representative blots. (Fii) Densitometric analysis of 3 independent experiments. *P < .05. Data are presented as mean ± SEM. Experiments were carried out in the presence of apyrase (2 U/mL), indomethacin (10 uM), and EGTA (1 mM).
S1526	Quizartinib (AC220) Quizartinib (AC220)是一种二代FLT3抑制剂，作用于Flt3(ITD/WT)，在MV4-11和 RS4;11细胞中IC50分别为1.1 nM/4.2 nM，作用于Flt3比作用于KIT，PDGFRA，PDGFRB，RET，和CSF-1R选择性高10倍。Phase 3。	Mol Cell Proteomics, 2020, 10.1074/mcp.RA119.001504 Eur J Med Chem, 2020, 193:112232 J Cell Mol Med, 2020, 24(3):2308-2318	Cotreatment with JQ1 and AC220 synergistically induces apoptosis of FLT3-ITD–expressing AML cells. MV4-11 cells were treated with the indicated concentrations of AC220 and/or JQ1 for 24 hours. At the end of treatment, immunoblot analyses were conducted as indicated. The numbers beneath the blots represent densitometry analysis conducted on representative blots.
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。	J Cell Mol Med, 2020, 24(3):2308-2318 Cell, 2019, 36(2):179-193 Cancer Cell, 2019, 36(2):179-193	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.
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.
S1043	Tandutinib (MLN518) Tandutinib (MLN518)是一种有效的FLT3拮抗剂，IC50为0.22 μM，同时也抑制PDGFR和c-Kit，对FLT3作用效果比CSF-1R强15到20倍，比FGFR， EGFR和KDR等强100倍以上。Phase 2。	Cell Rep, 2019, 28(9):2331-2344 J Alzheimers Dis, 2019, 67(3):1089-1106 Cancer Cell, 2018, 34(2):315-330
S1099^New	SKLB4771 (FLT3-IN-1) SKLB4771是一种有效、选择性的人类受体型酪氨酸蛋白激酶FLT3抑制剂，IC50为10 nM。
S6662^New	AST-487 (NVP-AST487) AST-487，一种N,N'-二苯基脲，是Flt3的竞争性抑制剂，ki值为0.12 μM。除FLT3以外，AST487还抑制RET,KDR,c-KIT 和 c-ABL 激酶，IC50值低于1 μM。
S8899^New	FF-10101 FF-10101是一种新型的不可逆的FLT3抑制剂，对FLT3(WT)和 FLT3(D835Y)的ic50分别为0.20 nM 和 0.16 nM。
S2692	TG101209 TG101209是一种选择性的JAK2抑制剂，无细胞试验中IC50为6 nM，对Flt3和RET作用效果稍弱，IC50分别为25 nM和17 nM，作用于JAK2比作用于JAK3选择性高30倍左右，对JAK2V617F和MPLW515L/K突变型敏感。	Nat Commun, 2018, 9(1):3259 Int Immunopharmacol, 2018, 54:354-365 Nat Commun, 2017, 8(1):1130	EGFR-ERCC1 effect on survival. QGP1 cells were transfected with Scrambled, ERCC1, EGFR, or EGFR-ERCC1 siRNA. Following 48 hours of siRNA transfection, Scrambled siRNA and ERCC1 siRNA-transfected cells were treated with 1 umol/L gefitinib or 125 nmol/L NU7026 (DNAPK inhibitor), or both, while EGFR siRNA and EGFR-ERCC1 siRNA-transfected cells were treated with 125 nmol/L of NU7026 1 hour prior 4 Gy IR treatment. Survival of these cells was then assessed 72 hours following IR treatment via MTT assay. The graphs show percentage of survival from 3 independent experiments as compared with untreated control. Bars show SD. Asterisks show statistical significance (,P < 0.05; , P < 0.01; **, P < 0.001; NS, nonsignificant).
S2158	KW-2449 KW-2449是一种多靶点抑制剂，最有效作用于Flt3，IC50为6.6 nM，作用于Flt3， Bcr-Abl和Aurora A适度有效；对PDGFRβ， IGF-1R， EGFR没有抑制效果。Phase 1。	Cell Rep, 2019, 28(9):2331-2344 Cell Chem Biol, 2018, 25(2):224-229 Mol Cancer Res, 2018, 16(10):1556-1567	Western blot analysis of p-histone and histone. 0-10μM KW2449 was added.
S1181	ENMD-2076 ENMD-2076选择性作用于Aurora A和VEGFR(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VEGFR2/KDR和VEGFR3， FGFR1和FGFR2和PDGFRα作用效果稍弱。Phase 2。	J Pediatr Hematol Oncol, 2019, 41(6):e359-e370 Vet Comp Oncol, 2016, 14(1):13-27 PLoS One, 2014, 9(7):e102741	Breast cancer cells line MDA-MB-231 were treated with the indicated concentrations of ENMD-2076.
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。	J Bone Oncol, 2019, 16:100232 Elife, 2017, 10.7554/eLife.25946 Transl Oncol, 2017, 10(3):357-366	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.
S8057	Pacritinib (SB1518) Pacritinib (SB1518)是有效的选择性Janus Kinase 2 (JAK2)和Fms-Like Tyrosine Kinase-3 (FLT3)抑制剂，无细胞试验中IC50分别为23和22 nM。Phase 3。	Exp Cell Res, 2019, 378(1):11-20 Clin Cancer Res, 2016, 22(24):6118-6128	Phosphorylation of the CSF-1R targets indicated was examined by immunoblotting
S8023	TCS 359 TCS 359是一种有效的FLT3抑制剂，IC50为42 nM。	Blood, 2016, 127(23):2890-90
S2018	ENMD-2076 L-(+)-Tartaric acid ENMD-2076 L-(+)-Tartaric acid 是ENMD-2076的酒石酸，选择性作用于Aurora A和VEGFR(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VEGFR2/KDR和VEGFR3， FGFR1和FGFR2和PDGFRα作用效果稍弱。Phase 2。		Breast cancer cells line MDA-MB-231 were treated with the indicated concentrations of ENMD-2076.
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 Genome Biol, 2016, 17:80	(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.
S7576	UNC2025 UNC2025是一种有效且口服生物可利用的双重MER/FLT3抑制剂，IC50分别为0.74 nM 和 0.8 nM，选择性比作用于Axl和 Tyro3大约高20倍。	Pharmacol Res, 2018, 134:166-178 Mol Cancer Ther, 2018, 17(11):2297-2308
S9275	Isoguanosine Isoguanosine 抑制 FLT3 和 HDAC3/6 治疗AML。Isoguanosine 是巴豆（Croton tiglium）种子中天然存在的鸟苷的活性异构体。
S8442	TAK-659 TAK-659是一种有效的、选择性的SYK抑制剂。IC50为3.2 nM。对其他激酶具有选择性，对FLT3也能有效抑制，IC50为4.6 nM。
S8229	Brigatinib (AP26113) Brigatinib (AP26113)是一种有效的、选择性的ALK抑制剂，IC50=0.6 nM；也是ROS1抑制剂，IC50=0.9 nM。它还能以相对较低的效力抑制FLT3、FLT3(D835Y)、EGFR。	Cell Syst, 2019, 8(2):97-108 Clin Cancer Res, 2019, 10.1158/1078-0432.CCR-19-1104 Invest New Drugs, 2019, 10.1007/s10637-019-00802-7	Immunoblotting analysis of H3122 and H3122-CER cells showing that brigatinib did not inhibit EGFR phosphorylation (p-EGFR). Total EGFR (t-EGFR) is also shown. Actin was used as a loading control. The cells were treated with brigatinib for 2 hours.
S7545	G-749 G-749是一种新型有效的FLT3抑制剂，对FLT3(WT),FLT3(D835Y),和Mer的IC50分别为0.4 nM,0.6nM 和 1nM，对其它酪氨酸激酶效果较低。
S7754	Gilteritinib (ASP2215) Gilteritinib(ASP2215)是小分子FLT3/AXL抑制剂，对FLT3和AXL的IC50值为0.29 nM和0.73 nM。其抑制c-KIT的IC50值约为抑制FLT3的800倍。	Clin Cancer Res, 2019, 10.1158/1078-0432.CCR-19-0832
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。
S7818	Pexidartinib (PLX3397) Pexidartinib (PLX3397)是一种口服有效的多靶点CSF-1R，Kit，和 FLT3受体酪氨酸激酶抑制剂，其IC50分别为20 nM, 10 nM 和 160 nM。Pexidartinib (PLX3397) 可以诱导细胞凋亡和坏死，并具有抗肿瘤活性。Phase 3。	J Control Release, 2020, 322:31-41 Stroke, 2020, 51(3):967-974 Neurobiol Dis, 2020, 134:104705	(a) Reduced tumour burden in PLX3397 (PLX) treated mice relative to untreated (NT) (n=6, P=.015; unpaired t-test). Bars represent total tumour volume with number of identified tumours indicated above each bar.
S7119	Go6976 Go6976是一种强效的PKC抑制剂，其对PKC (老鼠大脑), PKCα, and PKCβ1的IC50分别为7.9nM，2.3 nM, 和 6.2 nM 。此外，也是JAK2 和 Flt3的强抑制剂。	Front Pharmacol, 2020, 10:1589 Oncogene, 2019, 38(1):120-139 EBioMedicine, 2019, 40:151-162	Erk5 activation depends on Mek5, classical PKC and Mek1/2. MOVAS cells were serum-starved overnight and then treated for 1 h if not indicated otherwise with inhibitors targeting Jnk (SP600125, 10 μM), p38 (SB203580, 10 μM), Mek1/2 (CI-1040, 3 μM), Jak2 (AG490, 10 μM), Src (SU6656, 0.5 μM), Go6983 (PKC, 1 μM), Gö6976 (classical PKC, 1 μM), proteasomes (MG132, 25 μM), TPA (100 ng/ml for 15 min to activate PKCs or overnight to inhibit) and Mek5 (BIX02189, 1 μM), as well as Ca2 + chelators (EDTA, 2 mM; BAPTA-AM, 10 μM; both with 30 min preincubation), followed by stimulation with 20 ng/ml PDGF-BB for 10 min. Total cell lysates (TCL) were prepared and subjected to SDS-PAGE. Erk5 and PDGFRβ activities were measured by band shift and Tyr857 phosphorylation, respectively, using immunoblotting. Panel E and G show representative immunoblots.
S7533	AMG 925 AMG 925是一种有效的，且口服具有生物活性的双重FLT3/CDK4抑制剂，IC50分别为1 nM 和 3 nM。

目录号	产品描述	文献引用	实验数据
S2194	R406 R406是一种有效的Syk抑制剂，无细胞试验中IC50为41 nM，对Syk抑制作用强，但是不抑制Lyn，对Flt3的作用比对Syk低5倍。Phase 1。	Nat Cell Biol,2019, 21(2):203-213 PLoS Pathog,2019, 15(8):e1007923 PLoS One,2019, 14(1):e0210879	Platelets (3 x 10⁸/mL) were preincubated with Y27632 (10 uM), R406 (1 uM), or a combination of Y27632 and R406 for 20 minutes followed by stimulation with oxLDL (50 ug/mL) for 15 seconds and lysis. Samples were then separated by SDS-PAGE and were immunoblotted for phospho-MLCSer19, followed by reprobing for β-tubulin. (Fi) Representative blots. (Fii) Densitometric analysis of 3 independent experiments. *P < .05. Data are presented as mean ± SEM. Experiments were carried out in the presence of apyrase (2 U/mL), indomethacin (10 uM), and EGTA (1 mM).
S1526	Quizartinib (AC220) Quizartinib (AC220)是一种二代FLT3抑制剂，作用于Flt3(ITD/WT)，在MV4-11和 RS4;11细胞中IC50分别为1.1 nM/4.2 nM，作用于Flt3比作用于KIT，PDGFRA，PDGFRB，RET，和CSF-1R选择性高10倍。Phase 3。	Mol Cell Proteomics,2020, 10.1074/mcp.RA119.001504 Eur J Med Chem,2020, 193:112232 J Cell Mol Med,2020, 24(3):2308-2318	Cotreatment with JQ1 and AC220 synergistically induces apoptosis of FLT3-ITD–expressing AML cells. MV4-11 cells were treated with the indicated concentrations of AC220 and/or JQ1 for 24 hours. At the end of treatment, immunoblot analyses were conducted as indicated. The numbers beneath the blots represent densitometry analysis conducted on representative blots.
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。	J Cell Mol Med,2020, 24(3):2308-2318 Cell,2019, 36(2):179-193 Cancer Cell,2019, 36(2):179-193	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.
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.
S1043	Tandutinib (MLN518) Tandutinib (MLN518)是一种有效的FLT3拮抗剂，IC50为0.22 μM，同时也抑制PDGFR和c-Kit，对FLT3作用效果比CSF-1R强15到20倍，比FGFR， EGFR和KDR等强100倍以上。Phase 2。	Cell Rep,2019, 28(9):2331-2344 J Alzheimers Dis,2019, 67(3):1089-1106 Cancer Cell,2018, 34(2):315-330
S1099^New	SKLB4771 (FLT3-IN-1) SKLB4771是一种有效、选择性的人类受体型酪氨酸蛋白激酶FLT3抑制剂，IC50为10 nM。
S6662^New	AST-487 (NVP-AST487) AST-487，一种N,N'-二苯基脲，是Flt3的竞争性抑制剂，ki值为0.12 μM。除FLT3以外，AST487还抑制RET,KDR,c-KIT 和 c-ABL 激酶，IC50值低于1 μM。
S8899^New	FF-10101 FF-10101是一种新型的不可逆的FLT3抑制剂，对FLT3(WT)和 FLT3(D835Y)的ic50分别为0.20 nM 和 0.16 nM。
S2692	TG101209 TG101209是一种选择性的JAK2抑制剂，无细胞试验中IC50为6 nM，对Flt3和RET作用效果稍弱，IC50分别为25 nM和17 nM，作用于JAK2比作用于JAK3选择性高30倍左右，对JAK2V617F和MPLW515L/K突变型敏感。	Nat Commun,2018, 9(1):3259 Int Immunopharmacol,2018, 54:354-365 Nat Commun,2017, 8(1):1130	EGFR-ERCC1 effect on survival. QGP1 cells were transfected with Scrambled, ERCC1, EGFR, or EGFR-ERCC1 siRNA. Following 48 hours of siRNA transfection, Scrambled siRNA and ERCC1 siRNA-transfected cells were treated with 1 umol/L gefitinib or 125 nmol/L NU7026 (DNAPK inhibitor), or both, while EGFR siRNA and EGFR-ERCC1 siRNA-transfected cells were treated with 125 nmol/L of NU7026 1 hour prior 4 Gy IR treatment. Survival of these cells was then assessed 72 hours following IR treatment via MTT assay. The graphs show percentage of survival from 3 independent experiments as compared with untreated control. Bars show SD. Asterisks show statistical significance (,P < 0.05; , P < 0.01; **, P < 0.001; NS, nonsignificant).
S2158	KW-2449 KW-2449是一种多靶点抑制剂，最有效作用于Flt3，IC50为6.6 nM，作用于Flt3， Bcr-Abl和Aurora A适度有效；对PDGFRβ， IGF-1R， EGFR没有抑制效果。Phase 1。	Cell Rep,2019, 28(9):2331-2344 Cell Chem Biol,2018, 25(2):224-229 Mol Cancer Res,2018, 16(10):1556-1567	Western blot analysis of p-histone and histone. 0-10μM KW2449 was added.
S1181	ENMD-2076 ENMD-2076选择性作用于Aurora A和VEGFR(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VEGFR2/KDR和VEGFR3， FGFR1和FGFR2和PDGFRα作用效果稍弱。Phase 2。	J Pediatr Hematol Oncol,2019, 41(6):e359-e370 Vet Comp Oncol,2016, 14(1):13-27 PLoS One,2014, 9(7):e102741	Breast cancer cells line MDA-MB-231 were treated with the indicated concentrations of ENMD-2076.
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。	J Bone Oncol,2019, 16:100232 Elife,2017, 10.7554/eLife.25946 Transl Oncol,2017, 10(3):357-366	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.
S8057	Pacritinib (SB1518) Pacritinib (SB1518)是有效的选择性Janus Kinase 2 (JAK2)和Fms-Like Tyrosine Kinase-3 (FLT3)抑制剂，无细胞试验中IC50分别为23和22 nM。Phase 3。	Exp Cell Res,2019, 378(1):11-20 Clin Cancer Res,2016, 22(24):6118-6128	Phosphorylation of the CSF-1R targets indicated was examined by immunoblotting
S8023	TCS 359 TCS 359是一种有效的FLT3抑制剂，IC50为42 nM。	Blood,2016, 127(23):2890-90
S2018	ENMD-2076 L-(+)-Tartaric acid ENMD-2076 L-(+)-Tartaric acid 是ENMD-2076的酒石酸，选择性作用于Aurora A和VEGFR(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VEGFR2/KDR和VEGFR3， FGFR1和FGFR2和PDGFRα作用效果稍弱。Phase 2。		Breast cancer cells line MDA-MB-231 were treated with the indicated concentrations of ENMD-2076.
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 Genome Biol,2016, 17:80	(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.
S7576	UNC2025 UNC2025是一种有效且口服生物可利用的双重MER/FLT3抑制剂，IC50分别为0.74 nM 和 0.8 nM，选择性比作用于Axl和 Tyro3大约高20倍。	Pharmacol Res,2018, 134:166-178 Mol Cancer Ther,2018, 17(11):2297-2308
S9275	Isoguanosine Isoguanosine 抑制 FLT3 和 HDAC3/6 治疗AML。Isoguanosine 是巴豆（Croton tiglium）种子中天然存在的鸟苷的活性异构体。
S8442	TAK-659 TAK-659是一种有效的、选择性的SYK抑制剂。IC50为3.2 nM。对其他激酶具有选择性，对FLT3也能有效抑制，IC50为4.6 nM。
S8229	Brigatinib (AP26113) Brigatinib (AP26113)是一种有效的、选择性的ALK抑制剂，IC50=0.6 nM；也是ROS1抑制剂，IC50=0.9 nM。它还能以相对较低的效力抑制FLT3、FLT3(D835Y)、EGFR。	Cell Syst,2019, 8(2):97-108 Clin Cancer Res,2019, 10.1158/1078-0432.CCR-19-1104 Invest New Drugs,2019, 10.1007/s10637-019-00802-7	Immunoblotting analysis of H3122 and H3122-CER cells showing that brigatinib did not inhibit EGFR phosphorylation (p-EGFR). Total EGFR (t-EGFR) is also shown. Actin was used as a loading control. The cells were treated with brigatinib for 2 hours.
S7545	G-749 G-749是一种新型有效的FLT3抑制剂，对FLT3(WT),FLT3(D835Y),和Mer的IC50分别为0.4 nM,0.6nM 和 1nM，对其它酪氨酸激酶效果较低。
S7754	Gilteritinib (ASP2215) Gilteritinib(ASP2215)是小分子FLT3/AXL抑制剂，对FLT3和AXL的IC50值为0.29 nM和0.73 nM。其抑制c-KIT的IC50值约为抑制FLT3的800倍。	Clin Cancer Res,2019, 10.1158/1078-0432.CCR-19-0832
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。
S7818	Pexidartinib (PLX3397) Pexidartinib (PLX3397)是一种口服有效的多靶点CSF-1R，Kit，和 FLT3受体酪氨酸激酶抑制剂，其IC50分别为20 nM, 10 nM 和 160 nM。Pexidartinib (PLX3397) 可以诱导细胞凋亡和坏死，并具有抗肿瘤活性。Phase 3。	J Control Release,2020, 322:31-41 Stroke,2020, 51(3):967-974 Neurobiol Dis,2020, 134:104705	(a) Reduced tumour burden in PLX3397 (PLX) treated mice relative to untreated (NT) (n=6, P=.015; unpaired t-test). Bars represent total tumour volume with number of identified tumours indicated above each bar.
S7119	Go6976 Go6976是一种强效的PKC抑制剂，其对PKC (老鼠大脑), PKCα, and PKCβ1的IC50分别为7.9nM，2.3 nM, 和 6.2 nM 。此外，也是JAK2 和 Flt3的强抑制剂。	Front Pharmacol,2020, 10:1589 Oncogene,2019, 38(1):120-139 EBioMedicine,2019, 40:151-162	Erk5 activation depends on Mek5, classical PKC and Mek1/2. MOVAS cells were serum-starved overnight and then treated for 1 h if not indicated otherwise with inhibitors targeting Jnk (SP600125, 10 μM), p38 (SB203580, 10 μM), Mek1/2 (CI-1040, 3 μM), Jak2 (AG490, 10 μM), Src (SU6656, 0.5 μM), Go6983 (PKC, 1 μM), Gö6976 (classical PKC, 1 μM), proteasomes (MG132, 25 μM), TPA (100 ng/ml for 15 min to activate PKCs or overnight to inhibit) and Mek5 (BIX02189, 1 μM), as well as Ca2 + chelators (EDTA, 2 mM; BAPTA-AM, 10 μM; both with 30 min preincubation), followed by stimulation with 20 ng/ml PDGF-BB for 10 min. Total cell lysates (TCL) were prepared and subjected to SDS-PAGE. Erk5 and PDGFRβ activities were measured by band shift and Tyr857 phosphorylation, respectively, using immunoblotting. Panel E and G show representative immunoblots.
S7533	AMG 925 AMG 925是一种有效的，且口服具有生物活性的双重FLT3/CDK4抑制剂，IC50分别为1 nM 和 3 nM。

研究领域

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FLT3

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研究领域

抑制剂选择性比较

FLT3产品