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NVP-BHG 712

NVP-BHG 712用途

NVP-BHG712是EphB4抑制剂,ED50为25 nM,对c-Raf,c-Src和c-Abl的IC50分别为0.395 μM,1.266 μM和1.667 μM。

NVP-BHG 712名称

[ CAS 号 ]:
940310-85-0

[ 中文名 ]:
4-甲基-3-[[1-甲基-6-(3-吡啶基)-1H-吡唑并[3,4-d]嘧啶-4-基]氨基]-N-[3-(三氟甲基)苯基]苯甲酰胺

[ 英文名 ]:
NVP-BHG712

[英文别名 ]:

NVP-BHG712
cc-540
S2202_Selleck

NVP-BHG 712生物活性

[ 描述 ]:

NVP-BHG712是EphB4抑制剂,ED50为25 nM,对c-Raf,c-Src和c-Abl的IC50分别为0.395 μM,1.266 μM和1.667 μM。

[ 相关类别 ]:

信号通路 >> 蛋白酪氨酸激酶 >> 艾弗林受体

研究领域 >> 癌症

[参考文献]

[1]. Martiny-Baron G, et al. The small molecule specific EphB4 kinase inhibitor NVP-BHG712 inhibits VEGF driven angiogenesis. Angiogenesis. 2010 Sep;13(3):259-67.

[相关活性小分子]

N-[4-[(4-乙基-1-哌嗪基)甲基]-3-(三氟甲基)苯基]-4-甲基-3-[[[5-(2-噻吩基)-3-吡啶基]羰基]氨基]苯甲酰胺 | 特伐替尼 | 1-[1-[(2-氨基吡啶-4-基)甲基]-1H-吲哚-4-基]-3-(5-溴-2-甲氧基苯基)脲

NVP-BHG 712物理化学性质

[ 密度 ]:
1.4±0.1 g/cm3

[ 分子式 ]:
C₂₆H₂₀F₃N₇O

[ 分子量 ]:
503.478

[ 精确质量 ]:
503.168152

[ PSA ]:
101.11000

[ LogP ]:
4.05

[ 外观性状 ]:
white to beige

[ 折射率 ]:
1.666

[ 储存条件 ]:
?20°C

[ 水溶解性 ]:
DMSO: >15mg/mL

NVP-BHG 712安全信息

[ 符号 ]:

GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H301

[ 警示性声明 ]:
P301 + P310

[ 危害码 (欧洲) ]:
T

[ 风险声明 (欧洲) ]:
25

[ 安全声明 (欧洲) ]:
45

[ 危险品运输编码 ]:
UN 2811 6.1 / PGIII

NVP-BHG 712文献

EphB4 forward signalling regulates lymphatic valve development.

Nat. Commun. 6 , 6625, (2015)

Bidirectional signalling is regarded as a notable hallmark of the Eph-ephrin signalling system: Eph-dependent forward signalling in Eph-expressing cells and ephrin-dependent reverse signalling in Ephr...

EPHB4 Protein Expression in Vascular Smooth Muscle Cells Regulates Their Contractility, and EPHB4 Deletion Leads to Hypotension in Mice.

J. Biol. Chem. 290 , 14235-44, (2015)

EPH kinases are the largest family of receptor tyrosine kinases, and their ligands, ephrins (EFNs), are also cell surface molecules. This work presents evidence that EPHB4 on vascular smooth muscle ce...

Effect of EPH-ephrin signaling on the growth of human leukemia cells.

Anticancer Res. 34(6) , 2913-8, (2014)

Signaling induced by binding of erythropoietin-producing hepatoma-amplified sequence (EPH) receptors to their cell-surface ephrin ligands is implicated in hematopoiesis and growth of various cancer ce...

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