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CCT241736

CAS No. : 1402709-93-6

MCE 国际站：CCT241736

产品活性：CCT241736 是一种有效的，可口服的 FLT3 和 Aurora kinase 双重抑制剂，能够有效抑制 Aurora-A (K_d，7.5 nM；IC₅₀，38 nM)，Aurora-B (K_d，48 nM)，FLT3 (K_d，6.2 nM)，以及 FLT3 突变体 FLT3-ITD (K_d，38 nM) 和 FLT3(D835Y) (K_d，14 nM) 的活性。

研究领域：Protein Tyrosine Kinase/RTK  |  Epigenetics  |  Cell Cycle/DNA Damage

作用靶点：FLT3  |  Aurora Kinase

In Vitro: CCT241736 (Compound 27e) is a potent and orally bioavailable dual FLT3 and Aurora kinase inhibitor, which inhibits Aurora kinases (Aurora-A K_d, 7.5 nM, IC₅₀, 38 nM, Aurora-B K_d, 48 nM), FLT3 kinase (K_d, 6.2 nM), and FLT3 mutants including FLT3-ITD (K_d, 38 nM) and FLT3(D835Y) (K_d, 14 nM). CCT241736 exhibits antiproliferative activity in a range of human tumor cell lines, such as HCT116 human colon carcinoma (GI₅₀, 0.300 μM), the human FLT3-ITD positive AML cell lines MOLM-13 (GI₅₀, 0.104 μM) and MV4-11 (GI₅₀, 0.291 μM). CCT241736 also inhibits both the autophosphorylation of Aurora-A at T288 (a biomarker for Aurora-A inhibition: IC₅₀, 0.030 μM) and histone H3 phosphorylation at S10 (a biomarker for Aurora-B inhibition: IC₅₀, 0.148 μM), consistent with potent cellular activity versus both Aurora-A and -B. CCT241736 suppresses Aurora-A in MOLM-13 cells with concomitant inhibition of FLT3 signaling.

In Vivo: CCT241736 (50, 100 mg/kg, b.i.d, p.o.) dose-dependently suppresses the growth of MV4-11 human tumor xenografts, and completely abolishes the tumors at 100 mg/kg via p.o. administration twice a day.

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