Bioactivity | 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[1]. |
Invitro | ALK-IN-26 (0.5-2 μM, 24 h) 在 GL216 细胞中能够抑制 ALK 的活性[1]。ALK-IN-26 (0.5-10 μM, 24-72 h) 在 GL216、U87MG、Hela 细胞中能够抑制 GL216、U87MG 的活性,对 Hela 细胞活性的抑制有限[1]。ALK-IN-26 (0.5-2 μM, 24 h) 在 GL216 细胞中能够降低 mTOR 蛋白水平的表达[1]。ALK-IN-26 (0.5-2 μM, 24 h) 在 GL261 和 U87MG 细胞中显著降低 p-ERK1/2 蛋白水平、增强 p-JNK水平,对 p-AKT 和 p-STAT3 蛋白水平几乎不影响[1]。ALK-IN-26 (0.5-2 μM, 24 h) 在GL261 细胞中能够诱导细胞自噬[1]。ALK-IN-26 (0.5 μM-2 μM, 24-72 h) 在 GL261 细胞中升高了 cleaved-PARP (c-PARP) 和cleaved-caspase-3 (c-caspase 3) 蛋白水平[1]。ALK-IN-26 (0.5 μM-2 μM, 24-72 h) 在GL261 细胞中引起凋亡[1]。 0 --> ALK-IN-26 相关抗体: Apoptosis Analysis[1] Cell Line: |
In Vivo | ALK-IN-26 (5 mg/kg, i.v., 单剂量) 在雄性 C57BL6/J 小鼠中有药代动力学特性[1]。ALK-IN-26 (20 mg/kg, i.p., 单剂量) 在雄性 C57BL6/J 小鼠中能够穿透血脑屏障[1]。 Animal Model: |
Name | ALK-IN-26 |
CAS | 2447607-85-2 |
Formula | C24H23NO3S |
Molar Mass | 405.51 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Feng L, et al. Synthesis and Bioevaluation of 3-(Arylmethylene) indole Derivatives: Discovery of a Novel ALK Modulator with Antiglioblastoma Activities[J]. Journal of Medicinal Chemistry, 2023. |