产品
编 号:F035433
分子式:C29H40N8O3S
分子量:580.74
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
50mg
询价
询价
100mg
询价
询价
结构图
联系客服
产品详情
生物活性:
ASP3026 is a selective and orally active inhibitor of anaplastic lymphoma kinase (ALK). ASP3026 is a selective and oral active anaplastic lymphoma kinase (ALK) inhibitor with a IC50 value of 3.5 nM. ASP3026 can inhibit the phosphorylation of IGF-1R, STAT3, AKT and JNK proteins, and induce the cleavage of caspase 3 and PARP. It also inhibited ROS and ACK. ASP3026 can be used in anti-tumor research.

体内研究:
ASP3026 (30 mg/kg daily for 10 weeks, p.o.) 抑制小鼠体内 NPM-ALK+ ALCL 肿瘤细胞生长。ASP3026 (10 mg/kg daily for 5 days, p.o.) 可增强紫杉醇 Paclitaxel (HY-B0015) 和培美曲塞 Pemetrexed (HY-10820) 的抗肿瘤活性,单独使用时可诱导非小细胞肺癌模型小鼠肿瘤消退并延长生存期,且不影响非小细胞肺癌模型小鼠的体重。Animal Model:Female C.B-17 SCID mice of systemic xenograft lymphoma model
Dosage:30 mg/kg daily for 10 weeks
Administration:p.o.
Result:Mice in the ASP3026-interrupted group developed recurrent lymphoma, were subsequently treated with ASP3026 and survived until the end of the study.

体外研究:
ASP3026 (0.1-2.5 μM, 24-72 h) 降低 NPM-ALK+ ALCL 细胞的活力、增殖和集落形成,并诱导细胞凋亡。ASP3026 (0.1-2.5 μM, 24-72 h) 显著降低转染对 Crizotinib (HY-50878) 耐药的 NPM-ALK 突变体的 293T 细胞的增殖,并下调这些突变体的酪氨酸磷酸化。ASP3026 (1-4 μg/ml, 48 h) 可以抑制红细胞在能量耗尽和氧化应激后的细胞膜崩溃,并由此抵消自杀性红细胞死亡和随后贫血的发展。ASP3026 (100 nM, 1000 nM, 5 days) 以 ATP 竞争性方式抑制 ALK 活性,其抑制谱与 ALK/MET 双重抑制剂 Crizotinib (HY-50878) 不同。
产品资料