CCT129202

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。

CCT129202  纯度: 98.24%

CCT129202 是极光激酶 (aurora) 抑制剂,对极光激酶 A,B,C 的 IC50 值分别为42,198 和227 nM。

CCT129202

CCT129202 Chemical Structure

CAS No. : 942947-93-5

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5 mg ¥950 In-stock
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50 mg ¥5200 In-stock
100 mg ¥9350 In-stock
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生物活性

CCT129202 is an aurora kinase inhibitor with IC50s of 42, 198, and 227 nM for aurora A, B and C, respectively.

IC50 & Target[1]

Aurora A

42 nM (IC50)

Aurora B

198 nM (IC50)

Aurora C

227 nM (IC50)

体外研究
(In Vitro)

CCT129202 causes the accumulation of human tumor cells with z4N DNA content, leading to apoptosis. CCT129202 is found to induce apoptosis with GI50 values that ranges between 0.08 and 1.7 μM. CCT120202-treated human tumor cells shows a delay in mitosis, abrogation of nocodazole-induced mitotic arrest, and spindle defects. CCT129202 Causes p21Up-regulation, Rb Hypophosphorylation, and H2F-DependentTK1Down-regulation[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)

Growth of HCT116 xenografts in nude mice is inhibited after i.p. administration of CCT129202. p21, the cyclin-dependent kinase inhibitor, is induced by CCT129202. Up-regulation of p21 by CCT129202 in HCT116 cells led to Rb hypophosphorylation and E2F inhibition, contributing to a decrease in thymidine kinase 1 transcription[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

497.02

Formula

C23H25ClN8OS

CAS 号

942947-93-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 1 mg/mL (2.01 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0120 mL 10.0600 mL 20.1199 mL
5 mM
10 mM

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

参考文献
  • [1]. Chan F, et al. Mechanism of action of the Aurora kinase inhibitor CCT129202 and in vivo quantification of biological activity. Mol Cancer Ther. 2007 Dec;6(12 Pt 1):3147-57.

Cell Assay
[1]

The effects of CCT129202 on cell proliferation are analyzed with the MTT assay. Cells are plated in 96-well plates at 2,500 per well and are treated with a range of 0 to 50 μM of CCT129202 for 72 h. The absorbance is measured at 570 nm[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.

Animal Administration
[1]

Mice: For efficacy studies, human HCT116 colon carcinoma xenografts are established in female mice. CCT129202 is dissolved in DMSO and injected i.p in vehicle, which comprises 10% DMSO, 5% Tween 20, and 85% sterile saline at 0.1 mL/10 g body weight. Dosing with CCT129202 commenced when tumors are well established (f5 mm mean diameter); control animals receive an equivalent volume of vehicle. Mouse body weights and condition are monitored throughout the study. Tumors are measured thrice weekly[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.

参考文献
  • [1]. Chan F, et al. Mechanism of action of the Aurora kinase inhibitor CCT129202 and in vivo quantification of biological activity. Mol Cancer Ther. 2007 Dec;6(12 Pt 1):3147-57.

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