CH6953755
Modify Date: 2024-01-03 18:48:00
CH6953755 structure
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Common Name | CH6953755 | ||
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| CAS Number | 2055918-71-1 | Molecular Weight | 552.55 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C26H22F2N6O4S | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of CH6953755CH6953755 is a potent, orally active and selective YES1 kinase (a member of the SRC family) inhibitor with an IC50 of 1.8 nM. CH6953755 inhibits YES1 kinase, leading to antitumor activity against YES1 Gene -amplified cancers in vitro and in vivo[1]. |
| Name | CH6953755 |
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| Description | CH6953755 is a potent, orally active and selective YES1 kinase (a member of the SRC family) inhibitor with an IC50 of 1.8 nM. CH6953755 inhibits YES1 kinase, leading to antitumor activity against YES1 Gene -amplified cancers in vitro and in vivo[1]. |
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| Related Catalog | |
| Target |
IC50: 1.8 nM (YES1)[1] |
| In Vitro | CH6953755 (0.001-1 μM; for 4 days) inhibits the cell growth of YES1-amplified cancer cell lines[1]. CH6953755 (0.001-1 μM; for 2 hours) prevents the autophosphorylation at Tyr426 of YES1 that upregulates enzymatic activity in KYSE70 cells harboring YES1 amplification[1]. CH6953755 (0.1, 0.3, 1, 3 μM) suppresses TEAD luciferase reporter activity in YES1-amplified KYSE70 and RERF-LC-AI[1]. Cell Viability Assay[1] Cell Line: YES1-amplified cancer cell lines KYSE70 and OACP4 C, and non-YES1–amplified cancer cell line K562 expressing YES1-WT or YES1-GK Concentration: 0.001, 0.01, 0.1, 1 μM Incubation Time: 4 days Result: Inhibited the cell growth of YES1-amplified cancer cell lines. Western Blot Analysis[1] Cell Line: KYSE70 cell line Concentration: 0.001, 0.003, 0.01, 0.03, 0.1, 0.3, 1 μM Incubation Time: 2 hours Result: Prevented the autophosphorylation at Tyr426 of YES1 that upregulates enzymatic activity in KYSE70 cells harboring YES1 amplification |
| In Vivo | CH6953755 (oral; 60 mg/kg/day; for 10 days) shows selective antitumor activity accompanied with phospho-Tyr426 YES1 suppression in xenograft tumors[1]. CH6953755 (oral; 7.5, 15, 30, 60 mg/kg) suppresses phospho-Tyr426 YES1 in a dose-dependent manner[1]. Animal Model: Female BALB/c-nu/nu mice with Rat-2_YES1 xenograft[1] Dosage: 60 mg/kg Administration: Oral; daily; for 10 days Result: Showed selective antitumor activity accompanied with phospho-Tyr426 YES1 suppression in xenograft tumors. |
| References |
| Molecular Formula | C26H22F2N6O4S |
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| Molecular Weight | 552.55 |
| Storage condition | 2-8°C |