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。

CCT241736 is a potent and orally bioavailable dual FLT3 and Aurora kinase inhibitor, which inhibits Aurora kinases (Aurora-A K d , 7.5 nM, IC 50 , 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).

Solid

Aurora-A 38 nM (IC50) Aurora-A 7.5 nM (Kd)

CCT241736 (Compound 27e) is a potent and orally bioavailable dual FLT3 and Aurora kinase inhibitor, which inhibits Aurora kinases (Aurora-A Kd, 7.5 nM, IC50, 38 nM, Aurora-B Kd, 48 nM), FLT3 kinase (Kd, 6.2 nM), and FLT3 mutants including FLT3-ITD (Kd, 38 nM) and FLT3(D835Y) (Kd, 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

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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Bavetsias V, et al. Optimization of imidazo[4,5-b]pyridine-based kinase inhibitors: identification of a dual FLT3/Aurora kinase inhibitor as an orally bioavailable preclinical development candidate for the treatment of acute myeloid leukemia. J Med Chem.

In Vitro: DMSO : 75 mg/mL (164.34 mM; Need ultrasonic)配制储备液