产品
编 号:F099443
分子式:C21H22N4O4
分子量:394.42
产品类型
结构图
CAS No: 1259484-97-3
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产品详情
生物活性:
SKI-178 is a potent sphingosine kinase-1 (SphK1) and SphK2 inhibitor. SKI-178 is cytotoxic at IC50 concentrations ranging from 1.8 to 0.1 μM in both agent sensitive and multi-agent resistant cancer cell lines (i.e., MTR3, NCI-ADR and HL60/VCR cells). SKI-178 induces apoptosis in a CDK1-dependent manner in human acute myeloid leukemia cell lines.
体内研究:
SKI-178 (20 mg/kg;异氟醚麻醉下眼眶后注射) 抑制 MLL-AF9 模型中的白血病进展。Animal Model:MLL-AF9 mouse model (leukemic mice)
Dosage:20 mg/kg
Administration:Retro-orbital injection under isoflurane anesthesia; three times per week for 1 and 3 weeks
Result:White blood cell (WBC) counts decreased from their initial 104 cells/μL levels and continued to decline after 3 weeks of treatment until they reached normal levels (~4×103 cells/μL).
体外研究:
SKI-178 (5 μM;24 小时) 诱导的凋亡细胞死亡与延长的 Bcl-2 磷酸化相关。