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MC180295
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
MC180295图片
CAS NO:2237942-08-2
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议

产品名称
(rel)-MC180295
产品介绍
MC180295 ((rel)-MC180295) 是一种有效、选择性的CDK9-Cyclin T1抑制剂,IC50值为 5 nM,对其选择性至少是对其他 CDK 激酶 22 倍。MC180295 ((rel)-MC180295) 同时抑制 GSK-3α 和 GSK-3β。MC180295 具有的抗肿瘤活性。
生物活性

MC180295 ((rel)-MC180295) is a potent and selectiveCDK9-Cyclin T1inhibitor, with anIC50of 5 nM, at least 22-fold more selective forCDK9over other CDKs. MC180295 also inhibitsGSK-3αandGSK-3β. MC180295 ((rel)-MC180295) has potent anti-tumor effect[1].

IC50& Target[1]

CDK9- Cyclin T1

5 nM (IC50)

CDK1-Cyclin B

138 nM (IC50)

cdk2-cyclin A

233 nM (IC50)

cdk2-cyclin E

367 nM (IC50)

CDK3-Cyclin E

399 nM (IC50)

CDK4-Cyclin D

112 nM (IC50)

cdk5-p35

159 nM (IC50)

cdk5-p25

186 nM (IC50)

cdk6-cyclin D3

712 nM (IC50)

CDK7-CycH/MAT1

555 nM (IC50)

体外研究
(In Vitro)

MC180295 is a potent and selective CDK9-Cyclin T1 inhibitor, with an IC50of 5 nM, at least 22-fold more selective for CDK9 over other CDKs, such as CDK1-Cyclin B (IC50, 138 nM), CDK2-Cyclin A (IC50, 233 nM), CDK2-Cyclin E (IC50, 367 nM), CDK3-Cyclin E (IC50, 399 nM), CDK4-Cyclin D (IC50, 112 nM), CDK5-P35 (IC50, 159 nM), CDK5-P25 (IC50, 186 nM), CDK6-Cyclin D3 (IC50, 712 nM), and CDK7-CycH/MAT1 (IC50, 555 nM). MC180295 also inhibits GSK-3α and GSK-3β[1].
MC180295 (500 nM) reactivates epigenetically silenced genes by targeting CDK9 without affecting DNA methylation[1].
MC180295 (0.1 μM) inhibits the proliferation in cancer cells[1].

体内研究
(In Vivo)

MC180295 (20 mg/kg, i.p., qod) inhibits significant anti-tumor activity in mice bearing SW48 cells, shows no inhibitory activity against human T cell growth in vivo[1].

分子量

358.41

性状

Solid

Formula

C17H18N4O3S

CAS 号

2237942-08-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

溶解性数据
In Vitro: 

DMSO : 100 mg/mL(279.01 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.7901 mL13.9505 mL27.9010 mL
5 mM0.5580 mL2.7901 mL5.5802 mL
10 mM0.2790 mL1.3951 mL2.7901 mL
*

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℃, 6 months; -20℃, 1 month (stored under nitrogen)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。