| Name | CH6953755 |
| Description | CH6953755 is an orally active, potent and selective YES1 kinase inhibitor (IC50:1.8 nM).CH6953755 has anticancer activity and inhibits cancer cell proliferation by inhibiting YES1 kinase. |
| In vitro | CH6953755 inhibits the growth of cancer cell lines with YES1 amplification in a concentration-dependent manner (0.001-1 μM; 4 days)[1].
Preventing autophosphorylation of YES1 at the Tyr426 site, CH6953755 (0.001-1 μM; 2 hours) upregulates enzymatic activity in KYSE70 cells carrying YES1 amplification[1].In KYSE70 and RERF-LC-AI cells with YES1 amplification, CH6953755 (0.1, 0.3, 1, 3 μM) inhibits TEAD luciferase reporter gene activity[1]. |
| In vivo | CH6953755 exhibits selective antitumor activity in xenograft tumors following oral administration (60 mg/kg/day; 10 days), accompanied by inhibition of phosphorylation at Tyr426 of YES1[1].
In a dose-dependent manner, CH6953755 (oral; 7.5, 15, 30, 60 mg/kg) inhibits phosphorylation at Tyr426 of YES1[1]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 4 mg/mL (7.24 mM), Sonication is recommended.
DMSO : 100 mg/mL (180.98 mM), Sonication is recommended.
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| Keywords | Yes1 | CH-6953755 | CH6953755 | CH 6953755 |
| Inhibitors Related | Nintedanib | Vemurafenib | SI-2 hydrochloride | Staurosporine | Dasatinib | Ibrutinib | iHCK-37 | Pelitinib | Tofacitinib | Dasatinib monohydrate | TAK-901 | MCB-613 |
| Related Compound Libraries | Bioactive Compound Library | Membrane Protein-targeted Compound Library | HIF-1 Signaling Pathway Compound Library | Tyrosine Kinase Inhibitor Library | Kinase Inhibitor Library | Inhibitor Library | Mitochondria-Targeted Compound Library | Orally Active Compound Library | Bioactive Compounds Library Max | Fluorochemical Library | Anti-Cancer Compound Library | Anti-Cancer Active Compound Library |
United States
