CGK 733

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

CGK 733 是一种有效的选择性 ATM/ATR 抑制剂，IC50 约为 200 nM。

CGK 733 is a potent and selective inhibitor of ATM/ATR with IC50 of ~200 nM.

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.

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.

ATM/ATR Kinase Inhibitor

Cell Cycle/DNA Damage

ATM/ATR

ATM| ATR

Cancer

——

905973-89-9

555.84

C23H18Cl3FN4O3S

>98% (HPLC)

DMSO: 100 mg/mL (179.9 mM)

O=C(NC(NC(NC1=CC=C(F)C([N+]([O-])=O)=C1)=S)C(Cl)(Cl)Cl)C(C2=CC=CC=C2)C3=CC=CC=C3

2,2-diphenyl-N-(2,2,2-trichloro-1-(3-(4-fluoro-3-nitrophenyl)thioureido)ethyl)acetamide

(-20℃)

With Ice Pack

≥ 2 years