产品
编 号:F646691
分子式:C19H20N2O6S
分子量:404.44
产品类型
结构图
CAS No: 1346169-92-3
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产品详情
生物活性:
MPT0B392, an orally active quinoline derivative, induces c-Jun N-terminal kinase (JNK) activation, leading to apoptosis. MPT0B392 inhibits tubulin polymerization and triggers induction of the mitotic arrest, followed by mitochondrial membrane potential loss and caspases cleavage by activation of JNK and ultimately leads to apoptosis. MPT0B392 is demonstrated to be a novel microtubule-depolymerizing agent and enhances the cytotoxicity of sirolimus in sirolimus-resistant acute leukemic cells and the multidrug resistant cell line.
体内研究:
The effects of MPT0B392 (oral gavage; 50 mg/kg or 100 mg/kg for 12 or 14 days) shows relative potent anti-leukemia activity in a vivo xenograft model.Animal Model:Severe combined immunodeficient (SCID) mice
Dosage:50 mg/kg or 100 mg/kg
Administration:Oral gavage; 12 or 14 days
Result:Resulted in significant tumor growth delay (83.3%) and tumor volume inhibition without loss of body weight.
体外研究:
MPT0B392 (B392) (0.001-0.1 μM; 24 and 48 hours) inhibits the cell viability of HL60, MOLT-4, and CCRF-CEM cells with IC50s of 0.02 μM, 0.03 μM and 0.02 μM, respectively.MPT0B392 (0.1 μM; 48 hours) induces apoptosis in HL60 cancer cells.MPT0B392 (0.1 μM for 6-48 hours; 0.01-0.1 μM for 24 and 48 hours) triggers cells arrest in the G2/M phase, followed by accumulation in subG1 phase in a concentration and time-dependent manner.MPT0B392 (0.1 μM; 48 hours) increases the phosphorylation of Bcl-2, Mcl-1S and decreases in Mcl-1L.