CCT244747 is a potent, orally bioavailable and highly selective CHK1 inhibitor, with an IC 50 of 7.7 nM; CCT244747 also abrogates G2 checkpoint with an IC 50 of 29 nM. In Vitro CCT244747 poorly inhibits CHK2 (IC 50 >10 μM) and CDK1 (IC 50 >10 μM). CCT244747 has potent activities against CHK1, RSK1, RSK2, AMPK, BRSK1, IRAK1,and TrkA, with >80% inhibition. CCT244747 (10 μM) exhibits In Vivo CCT244747 (100 mg/kg po, qd7d) significantly reduces tumor burden in human tumor xenografts. CCT244747 (100-300 mg/kg, po) inhibits gemcitabine-induced pS296 CHK1 for up to 24 h in HT29 colon tumor xenografts . CCT244747 (75 mg/kg, p.o.) in combination with gemcitabine has potent antitumor effects in HT29 colon tumor xenografts and Calu6 human lung cancer xenografts. CCT244747 (150 mg/kg p.o.) also shows antitumor activities with irinotecan in SW620 human colon tumor xenografts. CCT244747 (100 mg/kg, p.o.) exhibits radiosensitization activity in Cal27 xenografts. MCE has not independently confirmed the accuracy of these methods. They are for reference only. IC50& Target:Chk1 7.7 nM (IC 50 )
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CCT244747
CAS number：1404095-34-6(DMSO) molecular formula：C20H24N8O2
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| Chinese alias | - | ||
| English alias | - | ||
| CAS number | 1404095-34-6(DMSO) | molecular formula | C20H24N8O2 |
| molecular weight | 408.47 g/mol | Exact mass | 10mM in DMSO |
| PSA | - | logp | - |
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