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CHMFL-ABL/KIT-155
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CHMFL-ABL/KIT-155图片
CAS NO:2081093-21-0
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
CHMFL-ABL-KIT-155
产品介绍
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。
生物活性

CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155; compound 34) is a highly potent and orally activetype II ABL/c-KITdual kinase inhibitor (IC50s of 46 nM and 75 nM, respectively), and it also presents significant inhibitory activities to BLK (IC50=81 nM), CSF1R (IC50=227 nM),DDR1(IC50=116 nM),DDR2(IC50=325 nM), LCK (IC50=12 nM) andPDGFRβ(IC50=80 nM) kinases. CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155) arrests cell cycle progression and inducesapoptosis[1].

IC50& Target

IC50: 46 nM (type II ABL), 75 nM (c-KIT), 81 nM (BLK), 227 nM (CSF1R), 116 nM (DDR1), 325 nM (DDR2), 12 nM (LCK), 80 nM (PDGFRβ)[1]

体外研究
(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)[1].

体内研究
(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[1].

分子量

609.68

Formula

C33H38F3N5O3

CAS 号

2081093-21-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.