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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.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $53 | In Stock | |
5 mg | $125 | In Stock | |
10 mg | $197 | In Stock | |
25 mg | $386 | In Stock | |
50 mg | $619 | In Stock | |
100 mg | $993 | In Stock | |
1 mL x 10 mM (in DMSO) | $152 | In Stock |
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. |
Targets&IC50 | YES1:1.8 nM |
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]. |
Molecular Weight | 552.55 |
Formula | C26H22F2N6O4S |
Cas No. | 2055918-71-1 |
Smiles | Cc1cc2cc([nH]c2cc1NS(C)(=O)=O)C(=O)c1cnn(c1N)-c1cnc(Oc2c(F)cccc2F)cc1C |
Relative Density. | 1.52 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 100 mg/mL (180.98 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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