CHMFL-ABL/KIT-155
Modify Date: 2024-01-09 20:16:44
CHMFL-ABL/KIT-155 structure
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Common Name | CHMFL-ABL/KIT-155 | ||
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| CAS Number | 2081093-21-0 | Molecular Weight | 609.68 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C33H38F3N5O3 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of CHMFL-ABL/KIT-155CHMFL-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[1]. |
| Name | CHMFL-ABL/KIT-155 |
|---|
| Description | 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[1]. |
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| Related Catalog | |
| 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] |
| 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]. |
| 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]. |
| References |
| Molecular Formula | C33H38F3N5O3 |
|---|---|
| Molecular Weight | 609.68 |