BRK inhibitor P21d hydrochloride

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BRK inhibitor P21d hydrochloride 

BRK inhibitor P21d hydrochloride 是一种有效的乳腺肿瘤激酶 ( BRK/PTK6) 抑制剂，IC50 为 30 nM。BRK inhibitor P21d hydrochloride 抑制 p-SAM68，IC50 为 52 nM。BRK inhibitor P21d hydrochloride 可用于评估 BRK 抑制剂在异种移植乳腺肿瘤模型中的体内活性。

BRK inhibitor P21d hydrochloride

BRK inhibitor P21d hydrochloride Chemical Structure

CAS No. : 2250025-98-8

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生物活性

BRK inhibitor P21d hydrochloride is a potent breast tumor kinase (BRK/PTK6) inhibitor with an IC50 of 30 nM. BRK inhibitor P21d hydrochloride inhibits p-SAM68 with an IC50 of 52 nM. BRK inhibitor P21d hydrochloride can be used to evaluate the in vivo activity of BRK inhibitors in xenograft breast tumor models[1].

IC50 & Target

IC50: 30 nM (BRK), 52 nM (p-SAM68), >20 μM (Aurora B), >20 μM (Lck)[1]
体外研究
(In Vitro)

BRK inhibitor P21d hydrochloride (compound 21d) inhibits Aurora B (IC50>20 μM) and Lck (IC50>20 μM)[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

BRK inhibitor P21d hydrochloride (compound 21d) has much better permeability (CACO-2:314 nm/s) and PK profile (rat, po, 10 mpk, AUC0–6h=31.1 μM•h,C6h=3.5 μM)[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

483.93

Formula

C23H23ClFN7O2
CAS 号

2250025-98-8
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Hongbo Zeng, et al. Discovery of Novel imidazo[1,2-a]pyrazin-8-amines as Brk/PTK6 Inhibitors. Bioorg Med Chem Lett. 2011 Oct 1;21(19):5870-5.

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