ALK-IN-26

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

ALK-IN-26 (compound 4a) 是 ALK 抑制剂，对 ALK 酪氨酸激酶的 IC50 值为7.0 μM。ALK-IN-26 有良好的药代动力学特性和血脑屏障通透性。ALK-IN-26 能够引起细胞凋亡、自噬和坏死。ALK-IN-26 能够用于胶质母细胞瘤研究。

ALK-IN-26 is an ALK inhibitor with IC50 value of 7.0 μM for ALK tyrosine kinase. ALK-IN-26 has good pharmacokinetic properties and blood-brain barrier (BBB) permeability. ALK-IN-26 can induce apoptosis, autophagy and necrosis. ALK-IN-26 can be used in glioblastoma studies.

Apoptosis AnalysisCell Line:GL261 Concentration:0.5 μM, 1.0 μM, 2.0 μM Incubation Time:24 h, 48 h, 72 h Result:Induced apoptosis of glioblastoma in a concentration- and time-dependent manner, and caused the cells (24.5%) entered the S phase but barely proceeded to the G2/M phase when treated with 1 μM for 72 h.Cell Viability AssayCell Line:GL216, U87MG, HelaConcentration:0.5 μM, 1.0 μM, 2.0 μM, 5 μM, 10 μM for GL216 and U87MG cells 5 μM, 10 μM, 20 μM, 40 μM, 80 μM, 160 μM for Hela cells Incubation Time:24 h, 48h, 72h Result:Inhibited the activity of GL216 cells with the inhibition rate of cells at 80% when incubated with 2 μM for 72 h and inhibited U87MG cells viability with a dose- and time-dependent manner, while showed limited inhibition on Hela cells, even at 160 μM, the inhibition rate is less than 50%. Can inhibit the activity of ALK tyrosine kinase with a dose-dependent manner.Cell Autophagy Assay Cell Line:GL261 Concentration:0.5 μM, 1.0 μM, 2.0 μM Incubation Time:24 h Result: Induced autophagy death in glioblastoma cells.

Animal Model:Male C57BL/6J miceDosage:5 mg/kgAdministration:Intravenous injection (i.v.), Single dose Result:Could be rapidly absorbed (Tmax = 0.58 h) with an acceptable half-life (T1/2 = 3.55 h) and bioavailability (F = 38.4%).Animal Model:Male C57BL/6J mice Dosage:20mg/kg Administration:Intraperitoneal injection (i.p.), Single doseResult:Could enter the body at concentrations up to 2.7μmol/kg (after 2 h administration at 20 mg/kg) andpenetrate the blood-brain barrier.

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Angiogenesis

ALK

ALK

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2447607-85-2

405.51

C24H23NO3S

>98% (HPLC)

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O=S(=O)(C1=CC=C(C=C1)C)N2C=C(C=3C=CC=CC32)CC=4C=C(C(O)=C(C4)C)C

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(-20℃)

With Ice Pack

≥ 2 years