CH6953755

SKU: orb1710073

Description

CH6953755 is a potent and selective oral YES1 kinase inhibitor with an IC50 of 1.8 nM. It suppresses cancer cell proliferation in vitro and demonstrates antitumor efficacy in vivo, making it a valuable research tool for oncology studies targeting YES1-dependent signaling pathways.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 2055918-71-1
• MW: 552.55
• Purity: 98.87% (May vary between batches)
• Formula: C₂₆H₂₂F₂N₆O₄S
• SMILES: Cc1cc2cc([nH]c2cc1NS(C)(=O)=O)C(=O)c1cnn(c1N)-c1cnc(Oc2c(F)cccc2F)cc1C
• Target: Src
• Solubility: DMSO:100 mg/mL (180.98 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (7.24 mM)

Bioactivity

• Target IC50:
  YES1:1.8 nM
• 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. In a dose-dependent manner, CH6953755 (oral; 7.5, 15, 30, 60 mg/kg) inhibits phosphorylation at Tyr426 of YES1.
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• In Vitro:
  CH6953755 inhibits the growth of cancer cell lines with YES1 amplification in a concentration-dependent manner (0.001-1 μM; 4 days). Preventing autophosphorylation of YES1 at the Tyr426 site, CH6953755 (0.001-1 μM; 2 hours) upregulates enzymatic activity in KYSE70 cells carrying YES1 amplification.In KYSE70 and RERF-LC-AI cells with YES1 amplification, CH6953755 (0.1, 0.3, 1, 3 μM) inhibits TEAD luciferase reporter gene activity.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CH-6953755, CH6953755, CH 6953755, Yes1, YES1

Compound Identifiers

PubChem CID

124149825