CHMFL-ABL/KIT-155

价格：询价

品牌：MedChemExpress(MCE) 品牌认证

货号：HY-101034

产品详情

CHMFL-ABL/KIT-155

CAS No. : 2081093-21-0

MCE 国际站：CHMFL-ABL/KIT-155

产品活性：CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155; compound 34) 是一种高效的，具有口服活性的 type II ABL/c-KIT 双激酶抑制剂 (IC₅₀ 分别为 46 nM 和 75 nM)，对 BLK (IC₅₀=81 nM), CSF1R (IC₅₀=227 nM), DDR1 (IC₅₀=116 nM), DDR2 (IC₅₀=325 nM), LCK (IC₅₀=12 nM), PDGFRβ (IC₅₀=80 nM) 激酶也具有明显的抑制活性。CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155) 阻止细胞周期进展和诱导细胞凋亡。

研究领域：Protein Tyrosine Kinase/RTK | Apoptosis

作用靶点：Bcr-Abl | c-Kit | Apoptosis | PDGFR | Discoidin Domain Receptor

In Vitro: CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155) exhibits anti-proliferation activities in the BCR-ABL dependent CML cancer cell lines such as K562 (GI₅₀: 0.027 µM), MEG-01 (GI₅₀: 0.02 µM), and KU812 (GI₅₀: 0.056 µM). It also potently inhibits the growth of c-KIT dependent GISTs cancer cell lines including GIST-T1 (GI₅₀: 0.023 µM), GIST-882 (GI₅₀: 0.095 µM) but not c-KIT independent GIST-48B (GI₅₀: 3.96 µM) .

In Vivo: CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155) (25-100 mg/kg; p.o.; once daily for 28 days) shows dose-dependent tumor progression suppression without apparent toxicity in female nu/nu mice bearing established K562 tumor xenografts.