CGK733CAS号: 905973-89-9分子式: C23H18Cl3FN4O3S分子量: 555.84描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)
产品描述 | |
描述 |
CGK 733是一种有效的ATM/ATR选择性抑制剂,IC50约为200 nM。 |
纯度 |
>98%
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储存/保存方法 |
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
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基本信息 | |
别名 |
CGK-733; CGK 733
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外观 |
Pale yellow solid
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可溶性/溶解性 |
DMSO : 100 mg/mL (179.9 mM)
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生物活性 | |
靶点 |
ATM_ATR
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In vitro(体外研究) |
CGK733 (4.2 ng/μL-12.5 ng/μL) enhances taxol-induced cytotoxicity in HBV-positive HCC cells. CGK733 (4.2 ng/μL) accelerates the formation of multinucleated cells and promotes the exit of mitosis in taxol-treated HBV-positive HCC cells. CGK733 (10 μM) causes the loss of cyclin D1 through the ubiquitin-dependent proteasomal degradation pathway in MCF-7 and T47D breast cancer cell lines. CGK733 (0.6-40 μM) shows inhibitory activities against proliferation of LnCap prostate cancer cells, HCT116 colon cancer cells, MCF-7 and T47D estrogen receptor positive breast cancer cells, and MDA-MB436 ER negative breast cancer cells. Moreover, CGK733 inhibits proliferation of non-transformed mouse BALB/c 3T3 embryonic fibroblast cells. In addition, CGK733 (10 μM) inhibits MCF-7 proliferation, and the effect can not be suppressed by pan-caspase inhibition. CGK733 (10 μM) results in 1.6-fold increase in ATM reporter activity in HEK-293 cells.
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In vivo(体内研究) |
CGK733 (25 mg/kg, i.p.) increases the ATM reporter activity (reports inactivation of ATM kinase activity) compared to control mice, with 2.4-fold, 3.1-fold, and 1.3-fold changes at 1, 4, and 8 hours, respectively.
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分子结构图