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MK-2461 {[allProObj[0].p_purity_real_show]}

货号:A683250

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.

MK-2461 化学结构 CAS号:917879-39-1
MK-2461 化学结构
CAS号:917879-39-1
MK-2461 3D分子结构
CAS号:917879-39-1
MK-2461 化学结构 CAS号:917879-39-1
MK-2461 3D分子结构 CAS号:917879-39-1
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MK-2461 纯度/质量文件 产品仅供科研

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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。

MK-2461 生物活性

靶点
  • PDGFRβ

    PDGFRβ, IC50:22 nM

  • FGFR2

    FGFR2, IC50:39 nM

  • FGFR3

    FGFR3, IC50:50 nM

  • FGFR1

    FGFR1, IC50:65 nM

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.

MK-2461 参考文献

[1]Pan BS, Chan GK, et al. MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor. Cancer Res. 2010 Feb 15;70(4):1524-33.

[2]Park YW, Cummings RT, et al. Homogeneous proximity tyrosine kinase assays: scintillation proximity assay versus homogeneous time-resolved fluorescence. Anal Biochem. 1999 Apr 10;269(1):94-104.

MK-2461 实验方案

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

MK-2461 技术信息

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
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