c-Kit
Catalog No. | Inhibitor Name | c-Kit | Other |
---|---|---|---|
A10290 | Dasatinib | *** | Abl,Src |
A10468 | Imatinib Mesylate | ** | PDGFR,v-Abl |
A10996 | Cabozantinib | *** | VEGFR2/KDR,c-Met,VEGFR3/FLT4 |
A10103 | Axitinib | **** | VEGFR1/FLT1,VEGFR2/Flk1,VEGFR2/KDR |
A10699 | Pazopanib HCl | * | VEGFR1,VEGFR2,VEGFR3 |
A11411 | Dovitinib | **** | FLT3,FGFR1,VEGFR3/FLT4 |
A10967 | Vatalanib 2HCl | * | VEGFR2/KDR,VEGFR1/FLT1,VEGFR2/Flk1 |
A10558 | Masitinib | * | Lyn B,PDGFRα,PDGFRβ |
A10101 | Tivozanib | ** | VEGFR2,VEGFR3,EphB2 |
A10610 | Amuvatinib | *** | PDGFRα (V561D),FLT3 (D835Y) |
A10608 | Motesanib Diphosphate | *** | VEGFR1,VEGFR2,VEGFR2/Flk1 |
A10679 | OSI-930 | ** | FLT1,KDR,CSF-1R |
A10502 | Ki8751 | ** | VEGFR2,PDGFRα,FGFR2 |
A10903 | Telatinib | **** | VEGFR3,VEGFR2,PDGFRα |
A11518 | Pazopanib | * | VEGFR1,VEGFR2,VEGFR3 |
A10198 | Dovitinib Dilactic Acid | **** | FLT3,FGFR1,VEGFR3/FLT4 |
A16320 | Dasatinib Monohydrate | *** | Abl ,Src |
A14156 | AZD2932 | *** | PDGFRβ,Flt3,VEGFR-2 |
A10880 | Sunitinib Malate | FLT3,PDGFRβ,VEGFR2 | |
A15062 | DCC-2618 | *** | PDGFRα, PDGFRβ |
A15519 | PLX647 | *** | Fms |
A15520 | Pexidartinib (PLX3397) | *** | CSF-1R, Flt-3 |
Notes:
1.Hover mouse over " " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.
-
Regorafenib Hydrochloride
Catalog No. A11546 VEGFR1/2/3/PDGFRβ/Kit/RET/Raf-1 inhibitorRegorafenib Hydrochloride is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively. 了解更多 -
CHMFL-ABL/KIT-155
Catalog No. A12421 ABL/c-KIT dual kinase inhibitorCHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155; compound 34) is a highly potent and orally active type II ABL/c-KIT dual kinase inhibitor. 了解更多 -
c-Kit-IN-2
Catalog No. A18440 c-KIT inhibitorc-Kit-IN-2 is a c-KIT inhibitor with an IC50 of 82 nM, shows superior antiproliferative activities against all the three GIST cell lines, GIST882, GIST430, and GIST48, with GI50s of 3, 1, and 2 nM, respectively. 了解更多 -
CHMFL-KIT-033
Catalog No. A18476 c-KIT T670I mutant inhibitorCHMFL-KIT-033 is a potent and selective inhibitor of c-KIT T670I mutant for gastrointestinal stromal tumors (GISTs), with an IC50 of 0.045 μM. 了解更多 -
AC710 Mesylate
Catalog No. A16246 FLT3/KIT/PDGFRα/PDGFRβ 抑制剂AC710 Mesylate是一种有效的选择性PDGFR家族激酶抑制剂,对于FLT3/KIT/PDGFRα/PDGFRβ的Kd值分别为0.6 nM/1.0 nM/1.3 nM/1.0 nM。 了解更多 -
AC710
Catalog No. A15933 -
Pexidartinib (PLX3397)
Catalog No. A15520 CSF1/Kit/FLT3 抑制剂Pexidartinib (PLX3397)是KIT,CSF1R和FLT3的小分子酪氨酸激酶(RTK)抑制剂,具有潜在的抗肿瘤活性。 了解更多 -
Masitinib mesylate
Catalog No. A15152 KIT/PDGFR 抑制剂Masitinib mesylate是Kit和PDGFRα/β的新型抑制剂,IC50为200 nM和540 nM/800 nM,对ABL和c-Fms的抑制作用较弱。 了解更多 -
Ki 20227
Catalog No. A11472 -
Pazopanib (GW-786034)
Catalog No. A11518 VEGFR 抑制剂Pazopanib (GW-786034)是VEGFR-1,VEGFR-2,VEGFR-3,PDGFR-a/β和c-kit的有效且选择性的多靶点酪氨酸激酶抑制剂,可阻止肿瘤生长并抑制血管生成。 了解更多 -
Sunitinib Malate
Catalog No. A10880 RTK inhibitorSunitinib Malate是一种多靶点RTK抑制剂,作用于VEGFR2 (Flk-1)和 PDGFRβ,也会抑制c-Kit的活性。用于治疗肾细胞癌(RCC)和伊马替尼耐药的胃肠道间质瘤(GIST)。 了解更多 -
Pazopanib HCl (GW786034)
Catalog No. A10699 VEGFR/PDGFR/FGFR 抑制剂Pazopanib HCl (GW786034)是VEGFR-1,VEGFR-2,VEGFR-3,PDGFR-a/β和c-kit的有效且选择性的多靶点酪氨酸激酶抑制剂,可阻止肿瘤生长并抑制血管生成。 了解更多 -
Regorafenib (BAY 73-4506)
Catalog No. A10250 VEGFR 抑制剂Regorafenib (BAY 73-4506)是一种多激酶抑制剂,IC50为17、40和69 nM c-KIT,VEGFR2,B-Raf。Regorafenib(BAY 73-4506)是一种针对肿瘤及其脉管系统的口服生物利用型多激酶抑制剂。 了解更多 -
Imatinib (Gleevec)
Catalog No. A10259 PDGFR 抑制剂Imatinib (Gleevec)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。 了解更多 -
XL184 free base (Cabozantinib)
Catalog No. A10996 VEGFR 抑制剂XL184 free base (Cabozantinib)是设计用来抑制多种受体酪氨酸激酶(特别是MET和VEGFR2)的小分子。 了解更多 -
Imatinib Mesylate
Catalog No. A10468 Bcr-Abl 抑制剂Imatinib mesylate是一种选择性酪氨酸激酶抑制剂,通过抑制KIT信号转导途径,在治疗胃肠间质瘤中诱导了持续的客观反应。 了解更多 -
Dasatinib (BMS-354825)
Catalog No. A10290 Abl-Src 抑制剂Dasatinib (BMS-354825)是一种口服多BCR/ABL和Src家族酪氨酸激酶抑制剂。Dasatinib (BMS-354825)的主要靶标是BCR/ABL,Src,c-Kit,ephrin受体和其他几种酪氨酸激酶,但不是erbB激酶,例如EGFR或Her2。 了解更多 -
Masitinib ( AB1010)
Catalog No. A10558 -
Dovitinib (TKI-258)
Catalog No. A11411 RTK 抑制剂Dovitinib是一种小分子多靶点酪氨酸激酶抑制剂,可抑制通过ZNF198-FGFR1或BCR-FGFR1转化为IL3独立性的Ba / F3细胞,IC50值分别为150 nM和90 nM。 了解更多 -
Tivozanib (AV-951)
Catalog No. A10101 VEGFR 抑制剂Tivozanib (AV-951)是一种口服VEGF受体酪氨酸激酶抑制剂,旨在抑制所有三种VEGF受体。 了解更多 -
AZD3229 Tosylate
Catalog No. A16867 -
Flumatinib
Catalog No. A16258 multi-kinase 抑制剂Flumatinib是一种多激酶抑制剂,对c-Abl,PDGFRbeta和c-Kit的IC50值分别为1.2 nM,307.6 nM和2662 nM。 了解更多 -
MP470 (MP-470, Amuvatinib)
Catalog No. A10610 -
PLX647
Catalog No. A15519 -
AST 487
Catalog No. A15003 -
Regorafenib monohydrate
Catalog No. A15218 Tyrosine kinase 抑制剂Regorafenib monohydrate是VEGFR1/VEGFR2/VEGFR3/PDGFRβ/Kit/RET和Raf-1的多靶点抑制剂,IC50分别为13 nM/4.2 nM/46 nM/22 nM/7 nM/1.5 nM和2.5 nM。 了解更多 -
N-Desethyl Sunitinib
Catalog No. A15182 VEGFR/PDGFRβ/KIT 抑制剂N-Desethyl Sunitinib是舒尼替尼的主要药理活性代谢产物,是有效的,ATP竞争性VEGFR,PDGFRβ和KIT抑制剂(VEGFR -1,-2,-3的Ki值为2、9、17、8和4 nM。分别为PDGFRβ和KIT)。 了解更多 -
Vatalanib (PTK787) 2HCl
Catalog No. A10967 VEGFR 抑制剂Vatalanib (PTK787) 2HCl是一种小分子蛋白激酶抑制剂,可抑制抑制所有已知VEGF受体以及血小板衍生的生长因子受体β和c-kit的血管生成,但对VEGFR-2的选择性最高。 了解更多 -
Flumatinib mesylate
Catalog No. A13530 c-Abl/c-Kit/PDGRFβ 抑制剂Flumatinib mesylate以时间和剂量依赖性的方式降低U266细胞中C-MYC,HIF-1a和VEGF的表达,因此甲磺酸氟马替尼可能成为MM治疗的新药。 了解更多 -
Toceranib (PHA 291639, SU 11654)
Catalog No. A11581 c-Kit, PDGFR, VEGFR 抑制剂Toceranib (PHA 291639,SU 11654)是一种激酶抑制剂,通过抑制KIT,血管内皮生长因子受体2和PDGFRβ同时具有抗肿瘤和抗血管生成活性。 了解更多 -
Telatinib (BAY 57-9352)
Catalog No. A10903 VEGFR-2 抑制剂Telatinib (BAY 57-9352)是一种口服的血管内皮生长因子受体2和3(VEGFR2/3)和血小板衍生的生长因子受体β酪氨酸激酶的小分子抑制剂,IC50分别为6 nM/4 nM,1 nM和15 nM。 了解更多 -
Dovitinib Dilactic acid (TKI258 Dilactic acid)
Catalog No. A10198 RTK 抑制剂Dovitinib是一种小分子多靶点酪氨酸激酶抑制剂,可抑制通过ZNF198-FGFR1或BCR-FGFR1转化为IL3独立性的Ba / F3细胞,IC50值分别为150 nM和90 nM。 了解更多 -
Motesanib Diphosphate (AMG-706)
Catalog No. A10608 VEGFR 抑制剂Motesanib也称为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。 了解更多