产品
编 号：F621003
分子式：C33H38F3N5O3
分子量：609.68
分子式：C33H38F3N5O3
分子量：609.68
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CAS No: 2081093-21-0
产品详情
生物活性：
CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155; compound 34) is a highly potent and orally active type II ABL/c-KIT dual 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) and PDGFRβ (IC50=80 nM) kinases. CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155) arrests cell cycle progression and induces apoptosis.
体内研究：
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.
体外研究：
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) .
CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155; compound 34) is a highly potent and orally active type II ABL/c-KIT dual 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) and PDGFRβ (IC50=80 nM) kinases. CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155) arrests cell cycle progression and induces apoptosis.
体内研究：
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.
体外研究：
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) .
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