Name: CHI3L1-IN-3
Brand: TargetMol
SKU: T211934
Rating: 4.5 (1 reviews)

规格

价格

库存

数量

10 mg

待询

50 mg

待询

产品介绍

生物活性

产品描述

CHI3L1-IN-3 is a CHI3L1 inhibitor that binds to CHI3L1 with dissociation constants (Kd) of 13.76 μM and 13.5 μM as measured by MST and SPR assays, respectively. It demonstrates an extended plasma half-life and microsomal stability, along with a low intrinsic clearance rate. In three-dimensional multicellular glioblastoma (GBM) spheroid models, CHI3L1-IN-3 induces dose-dependent cytotoxicity, reduces spheroid mass, and inhibits cell migration. This compound is valuable for glioblastoma research.

体外活性

CHI3L1-IN-3 (Compound 11g) 在小鼠和人类中显示出增强的稳定性，其血浆半衰期分别为2.0小时和2.5小时，而微粒体半衰期为小鼠2.2小时和人类2.8小时，同时清除率较低，小鼠为15 mL/min/mg，人在19 mL/min/mg。CHI3L1-IN-3 (50 μM, 72 h) 在hBMECs和HepG2细胞中表现出低细胞毒性，并且在NHA细胞中无毒性。该化合物(5-25 μM, 72 h) 能够剂量依赖性抑制胶质母细胞瘤（GBM）球体的细胞活力，其中CHI3L1-IN-3 (10 μM, 72 h) 导致球体重量减少超过50%，与广泛的细胞死亡和结构凝聚力丧失相一致。此外，CHI3L1-IN-3 (10 μM, 24-96 h) 可抑制GBM球体迁移达60%。在胶质母细胞瘤细胞系中，CHI3L1-IN-3 显示出抗增殖活性，IC 50 值分别为U251 MG细胞2.19 μM和T98G细胞5.06 μM。该化合物(5-25 μM, 72 h) 还剂量依赖性降低GBM球体中的pSTAT3水平。