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].

上海金畔生物科技有限公司 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].

上海金畔生物科技有限公司 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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