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CH6953755

CH6953755
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Purity:98.03%
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CH6953755

Catalog No. T10784Cas No. 2055918-71-1
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.
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Pack SizePriceAvailabilityQuantity
1 mg$53In Stock
5 mg$125In Stock
10 mg$197In Stock
25 mg$386In Stock
50 mg$619In Stock
100 mg$993In Stock
1 mL x 10 mM (in DMSO)$152In Stock
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Product Introduction

Bioactivity
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].
Chemical Properties
Molecular Weight552.55
FormulaC26H22F2N6O4S
Cas No.2055918-71-1
Storage & Solubility Information
Storage Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
DMSO: 100 mg/mL (180.98 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.8098 mL9.0490 mL18.0979 mL90.4895 mL
5 mM0.3620 mL1.8098 mL3.6196 mL18.0979 mL
10 mM0.1810 mL0.9049 mL1.8098 mL9.0490 mL
20 mM0.0905 mL0.4524 mL0.9049 mL4.5245 mL
50 mM0.0362 mL0.1810 mL0.3620 mL1.8098 mL
100 mM0.0181 mL0.0905 mL0.1810 mL0.9049 mL

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