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编 号:F174222
分子式:C16H16F3N7O
分子量:379.34
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10mM*1mL in DMSO
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5mg
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10mg
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25mg
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50mg
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100mg
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生物活性:
CCT245737 (SRA737) is an orally active and seletive Chk1 inhibitor, with an IC50 of 1.3 nM.

体内研究:
CCT245737 (150 mg/kg p.o.) inhibits tumor growth in combination with LY 188011 (100 mg/kg iv) in HT29 colon cancer xenografts. CCT245737 (300 mg/kg, p.o.) also inhibits the LY 188011 (60 mg/kg iv) induced pSer296 CHK1 autophosphorylation at 24 h in SW620 human colon cancer xenografts. CCT245737 (150 mg/kg, p.o) alone significantly inhibits tumor growth in an Eμ-Myc mouse model of human B-cell lymphocytic leukemia.

体外研究:
CCT245737 (10 μM) shows >80% inhibition of a panel of 124 kinases, including ERK8, PKD1, RSK2 and RSK1 with IC50s of 130, 298, 361 and 362 nM. CCT245737 abrogates an VP-16-induced G2 checkpoint in HT29, SW620, MiaPaCa-2, and Calu6 cell lines, with IC50s ranging from 30 to 220 nM.
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