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CH6953755

Catalog No. T10784   CAS 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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CH6953755 Chemical Structure
CH6953755, CAS 2055918-71-1
Pack Size Availability Price/USD Quantity
5 mg In stock $ 498.00
50 mg In stock $ 2,530.00
100 mg In stock $ 3,700.00
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Purity: 98.03%
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Biological Description
Chemical Properties
Storage & Solubility Information
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

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (180.98 mM), Sonification is recommended.

TargetMolReferences and Literature

1. Hamanaka N, et al. YES1 Is a Targetable Oncogene in Cancers Harboring YES1 Gene Amplification. Cancer Res. 2019 Nov 15;79(22):5734-5745.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Kinase Inhibitor Library

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Keywords

CH6953755 2055918-71-1 Angiogenesis Tyrosine Kinase/Adaptors Src CH-6953755 CH 6953755 inhibitor inhibit

 

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