化学性质:
规格 | 10mM (in 1mL DMSO) 5mg 10mg 50mg 200mg |
CAS | 1097917-15-1 |
别名 | ASP 3026;ASP-3026 |
化学名 | 2-N-[2-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl]-4-N-(2-propan-2-ylsulfonylphenyl)-1,3,5-triazine-2,4-diamine |
分子式 | C29H40N8O3S |
分子量 | 580.74 |
溶解度 | ≥ 14.5 mg/mL in DMSO, ≥ 4.9 mg/mL in EtOH with ultrasonic and warming |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
产品描述:
ASP3026 is a selective inhibitor of ALK with IC50 value of 3.5 nM [1].
ASP3026 is a potent ALK inhibitor and has a different selectivity with the reported ALK inhibitor crizotinib. When tested with a panel of 86 tyrosine kinases, ASP3026 showed the highest selectivity for ALK, ROS and ACK kinases. In NCI-H2228 NSCLC cells expressing EML4-ALK, five-day treatment of ASP3026 resulted in a cell growth inhibition with IC50 value of 64.8 nM. ASP3026 also inhibited the viability of NPM-ALK+ ALCL cells with IC50 values of 0.4, 0.75, 1 and 2.5 μM in SU-DHL-1, SUP-M2, SR-786 and Karpas 299 cells, respectively [2, 3].
In mouse model with NCI-H2228 subcutaneous xenograft, oral administration of ASP3026 caused significant reduction of phosphorylated ALK and tumor growth. 30 mg/kg/d ASP3026 for 2 weeks induced tumor regression by 78%. In mice injected with Karpas 299 cells, ASP3026 treatment caused remarkable lymphoma regression [2, 3].
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