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1817698-21-7

中文名稱 BDP5290
英文名稱 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 結(jié)構(gòu)式 1817698-21-7 結(jié)構(gòu)式

基本信息

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

物理化學(xué)性質(zhì)

沸點584.0±50.0 °C(Predicted)
密度1.56±0.1 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度DMSO : 12.5 mg/mL (33.62 mM)
酸度系數(shù)(pKa)10.83±0.50(Predicted)
形態(tài)Solid
顏色White to off-white

常見問題列表

生物活性
BDP5290 是 ROCK 和 MRCK 的有效抑制劑，對于 ROCK1，ROCK2，MRCKα 和 MRCKβ 的 IC50 值分別為 5 nM，50 nM，10 nM 和 100 nM。
靶點

ROCK1

5 nM (IC 50 )

ROCK2

50 nM (IC 50 )

MRCKα

10 nM (IC 50 )

MRCKβ

100 nM (IC 50 )

體外研究

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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