TC-A 2317 hydrochloride

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CAS NO:

1245907-03-2

包装与价格：

包装	价格(元)
100mg	电议
250mg	电议
500mg	电议

产品介绍

TC-A 2317 hydrochloride 是一种口服活性的极光 A 激酶 (Aurora A kinase) 抑制剂 (K_i=1.2 nM)。TC-A 2317 hydrochloride 对 Aurora B 激酶 (K_i=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。

生物活性

TC-A 2317 hydrochloride is an orally activeAurora Akinaseinhibitor (K_i=1.2 nM). TC-A 2317 hydrochloride exhibits excellent selectivity toAurora Bkinase (K_i=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 IC₅₀of 115 nM^[1].

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; C_maxvalue is 4930 nM (T_max=1.2 h) and serum concentration after 24 h is 52 nM (T_1/2=3.3 h) at 30 mg/kg po in rats^[1].

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.