产品
编 号:F226249
分子式:C10H13N5O5
分子量:283.24
产品类型
结构图
CAS No: 1818-71-9
联系客服
产品详情
生物活性:
Crotonoside is isolated from Chinese medicinal herb, Croton. Crotonoside inhibits FLT3 and HDAC3/6, exhibits selective inhibition in acute myeloid leukemia (AML) cells. Crotonoside could be a promising new lead compound for the research of AML.
体内研究:
Crotonoside(intraperitoneal and intravenous injection; 70 mg/kg, 35 mg/kg; once daily) induces a significant antitumor activity and inhibited xenograft tumor progress as compared to treatment with vehicle.Animal Model: NOD-SCID mice with MV4-11 cells
Dosage:70 mg/kg, 35 mg/kg
Administration:Intraperitoneal and intravenous injection; 70 mg/kg, 35 mg/kg; once daily
Result:Produced significant AML tumor inhibition rates of 93.5% at 70 mg/kg.
体外研究:
Crotonoside (0-200 μM;) selectively inhibits the viability of AML cell line MV4-11, MOLM-13 (with FLT3-ITD mutant) and KG-1 (without FLT3-ITD mutant) in a dose-dependent manner with an IC50 of 11.6 μM, 12.7 μM and 17.2 μM, respectively.Crotonoside (0-100μM; 7 hours) inhibits the phosphorylation of FLT3 Erk1/2, Akt/mTOR and STAT5 is strongly inhibited by crotonoside at higher concentration of 12.5 μM in a concentration-dependent manner.Crotonoside (0-100 μM; 12 hours) exhibits a dose-dependent increase in the percentage of G0/G1 phase and a dose-dependent decrease in the percentage of G2/M and S phases cells. Crotonoside (0-100 μM; 24 hours) leads to concentration-dependent changes in the number of apoptotic MV4-11 cells, results in a dose-dependent decrease in the level of pro-caspase-3 and a dose-dependent increase in the level of the cleaved caspase-3 fragments.