BDP5290

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BDP5290

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1817698-21-7

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。

生物活性

BDP5290 is a potent inhibitor of bothROCKandMRCKwithIC₅₀s of 5 nM, 50 nM, 10 nM and 100 nM forROCK1,ROCK2,MRCKαandMRCKβ, respectively.

IC₅₀& Target^[1]

ROCK1

5 nM (IC₅₀)

ROCK2

50 nM (IC₅₀)

MRCKα

10 nM (IC₅₀)

MRCKβ

100 nM (IC₅₀)

体外研究
(In Vitro)

The K_iof BDP5290 for MRCKα is 10 nM, which is slightly more than the K_iof 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 EC₅₀ >10 μM. Wound closure is inhibited by >60% at 1 μM BDP5290, a concentration that has no effect on cell viability^[2].

分子量

371.82

性状

Solid

Formula

C₁₇H₁₈ClN₇O

CAS 号

1817698-21-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 12.5 mg/mL(33.62 mM;Need ultrasonic)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	2.6895 mL	13.4474 mL	26.8947 mL
5 mM	0.5379 mL	2.6895 mL	5.3789 mL
10 mM	0.2689 mL	1.3447 mL	2.6895 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。