产品
编 号:F488634
分子式:C21H17ClFN3OS
分子量:413.9
产品类型
结构图
CAS No: 869185-85-3
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产品详情
生物活性:
Adezmapimod (SB 203580) hydrochloride is a selective and ATP-competitive p38 MAPK inhibitor with IC50s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. Adezmapimod hydrochloride inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. Adezmapimod hydrochloride is an autophagy and mitophagy activator.
体内研究:
Adezmapimod hydrochloride (5 mg/kg/day; 连续16天每天腹膜内注射; 雌性无胸腺 Nu/Nu 小鼠) 处理与平行处理的 p38TM 肿瘤相比,p38WT 肿瘤的肿瘤负荷明显更小。Animal Model:Six-week-old female atymic Nu/Nu mice CAL27 p38WT and p38TM tumors
Dosage:5 mg/kg/day
Administration:Intra peritoneal injected daily for 16 consecutive days
Result:After 2 weeks treatment, CAL27 p38WT tumors were significantly smaller; CAL27 p38TM tumors were not affected by the p38 inhibitor (n=10).?
体外研究:
Adezmapimod hydrochloride (用 0-30 μM 预孵育 1 小时并在 20 ng/mL IL-2 存在下培养 24 小时) 可防止 IL-2 诱导的原代人 T 细胞、鼠 CT6 T 细胞或 BAF 增殖 F7 B 细胞的 IC50 为 3-5 μM。 Adezmapimod hydrochloride 阻断 PKB 磷酸化 (IC50 3-5 μM)。Adezmapimod hydrochloride 在 CT6 和活化的人 T 细胞以及 IL-2 反应性 BA/F3 F7 B 细胞中以剂量依赖性方式抑制 Ser473 的磷酸化。