MK-2461 is a potent and multi-targeted inhibitor for c-Met with IC50 of 0.4-2.5 nM, also inhibits FGFR1/2/3, KDR, TrkA/B, and Flt4 with IC50 of 65/39/50 nM, 44 nM, 46/61 nM, and 78 nM respectively.
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产品名称 | PDGFR ↓ ↑ | PDGFRα ↓ ↑ | PDGFRβ ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Tyrphostin A9 |
+
PDGFR, IC50: 0.5 μM |
EGFR | 98% | ||||||||||||||||
Tyrphostin AG1296 | 99%+ | ||||||||||||||||||
Motesanib Diphosphate |
++
PDGFR, IC50: 84 nM |
98% | |||||||||||||||||
Pazopanib |
++
PDGFR, IC50: 84 nM |
99% | |||||||||||||||||
Imatinib |
+
PDGFR, IC50: 100 nM |
c-Kit | 98% | ||||||||||||||||
Imatinib Mesylate |
+
PDGFR, IC50: 100 nM |
c-Kit | 99% | ||||||||||||||||
Sennoside B | ✔ | 99%+ | |||||||||||||||||
PP121 |
++++
PDGFR, IC50: 2 nM |
mTOR,VEGFR | 99%+ | ||||||||||||||||
Crenolanib |
++++
PDGFRα, Kd: 2.1 nM |
++++
PDGFRβ, Kd: 3.2 nM |
99%+ | ||||||||||||||||
Masitinib |
+
PDGFRα, IC50: 540 nM |
+
PDGFRβ, IC50: 800 nM |
99%+ | ||||||||||||||||
Ki8751 |
++
PDGFRα, IC50: 67 nM |
c-Kit | 98+% | ||||||||||||||||
Tivozanib |
++
PDGFRα, IC50: 40 nM |
++
PDGFRβ, IC50: 49 nM |
99%+ | ||||||||||||||||
Ponatinib |
++++
PDGFRα, IC50: 1.1 nM |
98% | |||||||||||||||||
Amuvatinib |
++
PDGFRα (V561D), IC50: 40 nM |
99%+ | |||||||||||||||||
Axitinib |
+++
PDGFRα, IC50: 5.0 nM |
++++
PDGFRβ, IC50: 1.6 nM |
98% | ||||||||||||||||
CP-673451 |
+++
PDGFRα, IC50: 10 nM |
++++
PDGFRβ, IC50: 1 nM |
99%+ | ||||||||||||||||
Telatinib |
+++
PDGFRα, IC50: 15 nM |
c-Kit | 99%+ | ||||||||||||||||
Nintedanib |
++
PDGFRα, IC50: 59 nM |
++
PDGFRβ, IC50: 65 nM |
99+% | ||||||||||||||||
Avapritinib |
++++
PDGFRα (D842V), IC50: 0.5 nM |
99%+ | |||||||||||||||||
MK-2461 |
+++
PDGFRβ, IC50: 22 nM |
98%+ | |||||||||||||||||
Lactate |
+++
PDGFRβ, IC50: 27 nM |
c-Kit,FLT3 | 85% | ||||||||||||||||
Linifanib |
++
PDGFRβ, IC50: 66 nM |
99%+ | |||||||||||||||||
AZD2932 |
+++
PDGFRβ, IC50: 4 nM |
c-Kit | 98% | ||||||||||||||||
Dovitinib |
+++
PDGFRβ, IC50: 27 nM |
c-Kit,FLT3 | 99%+ | ||||||||||||||||
Sorafenib |
++
mPDGFRβ, IC50: 57 nM PDGFRβ, IC50: 57 nM |
99% | |||||||||||||||||
Sunitinib |
++++
PDGFRβ , IC50: 2 nM |
FLT3 | 98% | ||||||||||||||||
Orantinib |
+++
PDGFRβ, Ki: 8 nM |
99%+ | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
产品名称 | FGFR ↓ ↑ | FGFR1 ↓ ↑ | FGFR2 ↓ ↑ | FGFR3 ↓ ↑ | FGFR4 ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Tyrphostin AG1296 |
+
FGFR (Swiss 3T3), IC50: 12.3 μM |
PDGFR | 99%+ | ||||||||||||||||
Pazopanib |
+
FGFR, IC50: 140 nM |
99% | |||||||||||||||||
Erdafitinib | ✔ | RET | 99%+ | ||||||||||||||||
Gambogenic acid | ✔ | 98+% | |||||||||||||||||
Sulfatinib |
+++
FGFR1, IC50: 15 nM |
99+% | |||||||||||||||||
Nintedanib esylate |
+
FGFR1, IC50: 69 nM |
++
FGFR2, IC50: 37 nM |
+
FGFR3, IC50: 108 nM |
98% | |||||||||||||||
Zoligratinib |
+++
FGFR1, IC50: 9.3 nM |
+++
FGFR2, IC50: 7.6 nM |
++
FGFR3, IC50: 22 nM |
+
FGFR4, IC50: 290 nM |
99%+ | ||||||||||||||
MK-2461 |
+
FGFR1, IC50: 65 nM |
++
FGFR2, IC50: 39 nM |
++
FGFR3, IC50: 50 nM |
98%+ | |||||||||||||||
SU 5402 |
++
FGFR1, IC50: 30 nM |
98% | |||||||||||||||||
Brivanib |
+
FGFR1, IC50: 148 nM |
99%+ | |||||||||||||||||
Lucitanib |
++
FGFR1, IC50: 17.5 nM |
+
FGFR2, IC50: 82.5 nM |
99%+ | ||||||||||||||||
Ponatinib |
++++
FGFR1, IC50: 2.2 nM |
98% | |||||||||||||||||
PD-166866 |
+
FGFR1, IC50: 52.4 nM |
98% | |||||||||||||||||
Narazaciclib |
++
FGFR1, IC50: 26 nM |
RET | 99%+ | ||||||||||||||||
Lactate |
+++
FGFR1, IC50: 8 nM |
+++
FGFR3, IC50: 9 nM |
c-Kit,FLT3 | 85% | |||||||||||||||
Lenvatinib mesylate |
++
FGFR1, IC50: 46 nM |
c-RET | 99% | ||||||||||||||||
LY2874455 |
++++
FGFR1, IC50: 2.8 nM |
++++
FGFR2, IC50: 2.6 nM |
+++
FGFR3, IC50: 6.4 nM |
+++
FGFR4, IC50: 6 nM |
99%+ | ||||||||||||||
FIIN-2 |
+++
FGFR1, IC50: 3.09 nM |
+++
FGFR2, IC50: 4.3 nM |
++
FGFR3, IC50: 27 nM |
++
FGFR4, IC50: 45.3 nM |
98% | ||||||||||||||
FIIN-3 |
+++
FGFR1, IC50: 13.1 nM |
++
FGFR2, IC50: 21 nM |
++
FGFR3, IC50: 31.4 nM |
++
FGFR4, IC50: 35.3 nM |
98% | ||||||||||||||
Infigratinib |
++++
FGFR1, IC50: 0.9 nM |
++++
FGFR2, IC50: 1.4 nM |
++++
FGFR3, IC50: 1.0 nM FGFR3 (K650E), IC50: 4.9 nM |
+
FGFR4, IC50: 60 nM |
99%+ | ||||||||||||||
Danusertib |
++
FGFR1, IC50: 47 nM |
RET | 99%+ | ||||||||||||||||
R1530 |
++
FGFR1, IC50: 28 nM |
98% | |||||||||||||||||
ENMD-2076 |
+
FGFR1, IC50: 92.7 nM |
+
FGFR2, IC50: 70.8 nM |
RET,FLT3 | 98% | |||||||||||||||
Dovitinib |
+++
FGFR1, IC50: 8 nM |
+++
FGFR3, IC50: 9 nM |
c-Kit,FLT3 | 99%+ | |||||||||||||||
Sorafenib |
+
FGFR1, IC50: 580 nM |
99% | |||||||||||||||||
SSR128129E |
+
FGFR1, IC50: 1.9 μM |
99%+ | |||||||||||||||||
AZD-4547 |
++++
FGFR1, IC50: 0.2 nM |
++++
FGFR2, IC50: 2.5 nM |
++++
FGFR3, IC50: 1.8 nM |
98% | |||||||||||||||
Lenvatinib |
++
FGFR1, IC50: 46 nM |
RET | 98% | ||||||||||||||||
PD173074 |
++
FGFR1, IC50: ~25 nM |
99%+ | |||||||||||||||||
S49076 |
++
FGFR1, IC50: 18 nM |
+++
FGFR2, IC50: 17 nM |
+++
FGFR3, IC50: 15 nM |
98% | |||||||||||||||
Futibatinib |
++++
FGFR1, IC50: 1.8 nM |
++++
FGFR2, IC50: 1.4 nM |
++++
FGFR3, IC50: 1.6 nM |
+++
FGFR4, IC50: 3.7 nM |
99%+ | ||||||||||||||
Ferulic Acid |
+
FGFR1, IC50: 3.78 μM |
+
FGFR2, IC50: 12.5 μM |
98% | ||||||||||||||||
Nintedanib |
+
FGFR1, IC50: 69 nM |
++
FGFR2, IC50: 37 nM |
+
FGFR3, IC50: 108 nM |
+
FGFR4, IC50: 610 nM |
99+% | ||||||||||||||
ASP5878 |
++++
FGFR1, IC50: 0.47 nM |
++++
FGFR2, IC50: 0.6 nM |
++++
FGFR3, IC50: 0.74 nM |
+++
FGFR4, IC50: 3.5 nM |
98% | ||||||||||||||
PRN1371 |
++++
FGFR1, IC50: 0.6 nM |
++++
FGFR2, IC50: 1.3 nM |
+++
FGFR3, IC50: 4.1 nM |
++
FGFR4, IC50: 19.3 nM |
99% | ||||||||||||||
Derazantinib |
+++
FGFR1, IC50: 4.5 nM |
++++
FGFR2, IC50: 1.8 nM |
+++
FGFR3, IC50: 4.5 nM |
++
FGFR4, IC50: 34 nM |
RET | 99%+ | |||||||||||||
ODM-203 |
+++
FGFR1, IC50: 11 nM |
+++
FGFR2, IC50: 16 nM |
+++
FGFR3, IC50: 6 nM |
++
FGFR4, IC50: 35 nM |
99%+ | ||||||||||||||
Pemigatinib |
++++
FGFR1, IC50: 0.4 nM |
++++
FGFR2, IC50: 0.5 nM |
++++
FGFR3, IC50: 1.2 nM |
++
FGFR4, IC50: 30 nM |
99%+ | ||||||||||||||
SKLB 610 | ✔ | PDGFR | 99%+ | ||||||||||||||||
Alofanib | ✔ | 99%+ | |||||||||||||||||
Lirafugratinib | ✔ | 98% | |||||||||||||||||
Masitinib mesylate | ✔ | FAK | 99%+ | ||||||||||||||||
BLU9931 |
+
FGFR3, IC50: 150 nM |
+++
FGFR4, IC50: 3 nM |
99%+ | ||||||||||||||||
BO-264 | ✔ | 99%+ | |||||||||||||||||
Fisogatinib |
+++
FGFR4, IC50: 5 nM |
99%+ | |||||||||||||||||
H3B-6527 |
++++
FGFR4, IC50: <1.2 nM |
99%+ | |||||||||||||||||
Roblitinib |
++++
FGFR4, IC50: 1.9 nM |
99%+ | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
靶点 |
|
描述 | MK-2461 is a potent, multi-targeted inhibitor for c-Met (WT/mutants) with IC50 of 0.4-2.5 nM, less potent to Ron, Flt1 and with 8- to 30-fold greater selectivity of c-Met targets versus FGFR1, FGFR2, FGFR3, PDGFRβ, KDR, Flt3, Flt4, TrkA, and TrkB. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.02mL 0.40mL 0.20mL |
10.09mL 2.02mL 1.01mL |
20.18mL 4.04mL 2.02mL |
CAS号 | 917879-39-1 |
分子式 | C24H25N5O5S |
分子量 | 495.551 |
别名 | |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,Store in freezer, under -20°C |
溶解度 |
DMSO: 30 mg/mL(60.54 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |