DC Chemicals · Product datasheet

CGK733 — Datasheet

CAT. NO. DC7101

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ParameterValue
Chemical NameDiphenyl acetamidotrichloroethyl fluoronitrophenyl thiourea
CAS No.905973-89-9
Synonyms2,2-DIPHENYL-N-(2,2,2-TRICHLORO-1-[3-(4-FLUORO-3-NITROPHENYL)THIOUREIDO]ETHYL)ACETAMIDE;CGK 733;2,2-diphenyl-N-[2,2,2-trichloro-1-[(4-fluoro-3-nitrophenyl)carbamothioylamino]ethyl]acetamide;ATM;ATR Kinase Inhibitor;CGK-733;CGK733;2,2-Diphenyl-N-(2,2,2-trichloro-1-(3-(4-fluoro-3-nitrophenyl)thioureido)ethyl)acetamide;Diphenyl acetamidotrichloroethyl fluoronitrophenyl thiourea;2,2-diphenyl-N-(2,2,2-trichloro-1-{[(4-fluoro-3-nitrophenyl)carbamothioyl]amino}ethyl)acetamide;L3DGZ99QY
FormulaC23H18Cl3FN4O3S
M.Wt555.8364
SMILESClC(C([H])(N([H])C(N([H])C1C([H])=C([H])C(=C(C=1[H])[N+](=O)[O-])F)=S)N([H])C(C([H])(C1C([H])=C([H])C([H])=C([H])C=1[H])C1C([H])=C([H])C([H])=C([H])C=1[H])=O)(Cl)Cl
Purity>98%
Storage2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological Activity

CGK733 is a potent ATM/ATR inhibitor, used for the research of cancer.

In Vitro

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[1]. 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[2]. CGK733 (10 μM) results in 1.6-fold increase in ATM reporter activity in HEK-293 cells[3].

In Vivo

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[3].

References & source

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.

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