产品
编 号:F598801
分子式:C29H30F2N4O2
分子量:504.57
产品类型
结构图
CAS No: 847928-32-9
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产品详情
生物活性:
1G244 is a potent DPP8/9 inhibitor with IC50s of 12 nM and 84 nM, respectively. 1G244 does not inhibit DPPIV and DPPII. 1G244 induces apoptosis in multiple myeloma cells and has anti-myeloma effects.
体内研究:
1G244 (30 mg/kg;皮下注射;每周一次;持续 3 周;NOG 雌性小鼠) 明显抑制了小鼠异种移植肿瘤模型中 MM.1S 细胞的皮下生长。Animal Model:NOD/Shi-scid IL-2Rγnull (NOG) female mice (6-7 weeks; 19-21?g) injected with MM.1?S cells
Dosage:30 mg/kg
Administration:Subcutaneous injection; once-a-week; for 3 weeks
Result:Apparently suppressed the subcutaneous growth of MM.1?S cells in murine xenograft model.
体外研究:
1G244 (0-100 μM;72 小时;Delta47、U266、KMS-5、RPMI8226 或 MM.1 S 细胞) 剂量依赖性地降低了五种多发性骨髓瘤细胞系的活细胞数。 1G244 (50 μM;0-48 小时;MM.1 S 细胞) 诱导细胞凋亡,因为检测到 caspase-3 和 PARP 的裂解形式。