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CCT245737

CAS No. : 1489389-18-5

MCE 站：CCT245737

产品活性：CCT245737 是一种可口服的，选择性的 Chk1 抑制剂，IC₅₀ 值为 1.3 nM。

研究领域：Cell Cycle/DNA Damage

作用靶点：Checkpoint Kinase (Chk)

In Vitro: CCT245737 (10 ?M) 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.

In Vivo: 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.

相关产品：Bioactive Compound Library Plus  |  Cell Cycle/DNA Damage Compound Library  |  Kinase Inhibitor Library  |  Anti-Cancer Compound Library  |  Anti-Aging Compound Library  |  Orally Active Compound Library  |  Anti-Blood Cancer Compound Library  |  CCT241533 hydrochloride  |  2OH-BNPP1  |  ANI-7  |  SB-218078  |  Chk1-IN-5  |  CHK1-IN-2

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