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1817698-21-7

中文名称 BDP5290
英文名称 BDP5290
CAS 1817698-21-7
分子式 C17H18ClN7O
分子量 371.82
MOL 文件 1817698-21-7.mol
更新日期 2024/12/03 15:40:36
1817698-21-7 结构式 1817698-21-7 结构式

基本信息

中文别名
ROCK和MRCK抑制剂(BDP5290)
英文别名
BDP5290
BDP5290
BDP-5290
BDP 5290
1H-Pyrazole-3-carboxamide, 4-chloro-1-(4-piperidinyl)-N-[3-(2-pyridinyl)-1H-pyrazol-4-yl]-

物理化学性质

沸点584.0±50.0 °C(Predicted)
密度1.56±0.1 g/cm3(Predicted)
储存条件-20°C储存
溶解度DMSO : 12.5 mg/mL (33.62 mM)
酸度系数(pKa)10.83±0.50(Predicted)
形态Solid
颜色White to off-white
BDP5290价格(试剂级)
报价日期产品编号产品名称CAS号包装价格
2025/05/22HY-12437BDP52901817698-21-71 mg654元
2025/05/22HY-12437BDP52901817698-21-710 mM * 1 mLin DMSO1227元
2025/05/22HY-12437BDP5290
BDP5290
1817698-21-75mg1500元

常见问题列表

生物活性
BDP5290 是 ROCK 和 MRCK 的有效抑制剂,对于 ROCK1,ROCK2,MRCKα 和 MRCKβ 的 IC50 值分别为 5 nM,50 nM,10 nM 和 100 nM。
靶点

ROCK1

5 nM (IC 50 )

ROCK2

50 nM (IC 50 )

MRCKα

10 nM (IC 50 )

MRCKβ

100 nM (IC 50 )

体外研究

The K i of BDP5290 for MRCKα is 10 nM, which is slightly more than the K i of 4 nM for MRCKβ. 3 μM BDP5290 completely inhibits myosin II light chain (MLC) phosphorylation induced by MRCKβ, but not by ROCK1 or ROCK2. At higher concentrations, BDP5290 reduces MLC phosphorylation (pMLC) to undetectable levels. BDP5290 reduces MDA-MB-231 invasion at all tested concentrations starting from 0.1 μM, with virtually complete inhibition at 10 μM. After 24 hours in the presence of BDP5290 cell viability is slightly reduced with an EC 50 >10 μM. Wound closure is inhibited by >60% at 1 μM BDP5290, a concentration that has no effect on cell viability.

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