TC-A 2317 hydrochloride

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

TC-A 2317 hydrochloride 

TC-A 2317 hydrochloride 是一种口服活性的极光 A 激酶 (Aurora A kinase) 抑制剂 (Ki=1.2 nM)。TC-A 2317 hydrochloride 对 Aurora B 激酶 (Ki=101 nM) 和其他 60 种激酶具有优异的选择性，具有良好的细胞通透性和良好的 PK 特性。TC-A 2317 hydrochloride 具有抗肿瘤活性。

TC-A 2317 hydrochloride

TC-A 2317 hydrochloride Chemical Structure

CAS No. : 1245907-03-2

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

TC-A 2317 hydrochloride is an orally active Aurora A kinase inhibitor (Ki=1.2 nM). TC-A 2317 hydrochloride exhibits excellent selectivity to Aurora B kinase (Ki=101 nM) and other 60 kinases, good cell permeability and good PK profile. Antitumor activity[1].

IC50 & Target[1]

Aurora A

1.2 nM (Ki)

Aurora B

101 nM (Ki)

体外研究
(In Vitro)

TC-A 2317 hydrochloride (Compound 6) inhibits proliferation of HCT116 cells with an IC50 of 115 nM[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)

TC-A 2317 hydrochloride is effective in antitumor mice model without decrease of body weight[1].
TC-A 2317 hydrochloride shows good PK profile; Cmax value is 4930 nM (Tmax=1.2 h) and serum concentration after 24 h is 52 nM (T1/2=3.3 h) at 30 mg/kg po in rats[1].

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

Animal Model: HCT-116 Xenograft mice mode[1]
Dosage: P.o.; daily for 14 days
Administration: 30 mg/kg
Result: Growth of tumor was inhibited by 59% after 14 days.

分子量

392.93

Formula

C19H29ClN6O
CAS 号

1245907-03-2
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]. Ando R, et al. 3-Cyano-6-(5-methyl-3-pyrazoloamino)pyridines: selective Aurora A kinase inhibitors. Bioorg Med Chem Lett. 2010;20(15):4709-4711.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务