TC-A 2317 hydrochloride

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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

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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.

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