1. Protein Tyrosine Kinase/RTK
  2. Src
  3. CH6953755

CH6953755 

Cat. No.: HY-135299
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CH6953755 is a potent, orally active and selective YES1 kinase (a member of the SRC family) inhibitor with an IC50 of 1.8 nM. CH6953755 inhibits YES1 kinase, leading to antitumor activity against YES1 Gene -amplified cancers in vitro and in vivo.

For research use only. We do not sell to patients.

CH6953755 Chemical Structure

CH6953755 Chemical Structure

CAS No. : 2055918-71-1

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Description

CH6953755 is a potent, orally active and selective YES1 kinase (a member of the SRC family) inhibitor with an IC50 of 1.8 nM. CH6953755 inhibits YES1 kinase, leading to antitumor activity against YES1 Gene -amplified cancers in vitro and in vivo[1].

IC50 & Target

IC50: 1.8 nM (YES1)[1]

In Vitro

CH6953755 (0.001-1 μM; for 4 days) inhibits the cell growth of YES1-amplified cancer cell lines[1].
CH6953755 (0.001-1 μM; for 2 hours) prevents the autophosphorylation at Tyr426 of YES1 that upregulates enzymatic activity in KYSE70 cells harboring YES1 amplification[1].
CH6953755 (0.1, 0.3, 1, 3 μM) suppresses TEAD luciferase reporter activity in YES1-amplified KYSE70 and RERF-LC-AI[1].

Cell Viability Assay[1]

Cell Line: YES1-amplified cancer cell lines KYSE70 and OACP4 C, and non-YES1–amplified cancer cell line K562 expressing YES1-WT or YES1-GK
Concentration: 0.001, 0.01, 0.1, 1 μM
Incubation Time: 4 days
Result: Inhibited the cell growth of YES1-amplified cancer cell lines.

Western Blot Analysis[1]

Cell Line: KYSE70 cell line
Concentration: 0.001, 0.003, 0.01, 0.03, 0.1, 0.3, 1 μM
Incubation Time: 2 hours
Result: Prevented the autophosphorylation at Tyr426 of YES1 that upregulates enzymatic activity in KYSE70 cells harboring YES1 amplification
In Vivo

CH6953755 (oral; 60 mg/kg/day; for 10 days) shows selective antitumor activity accompanied with phospho-Tyr426 YES1 suppression in xenograft tumors[1].
CH6953755 (oral; 7.5, 15, 30, 60 mg/kg) suppresses phospho-Tyr426 YES1 in a dose-dependent manner[1].

Animal Model: Female BALB/c-nu/nu mice with Rat-2_YES1 xenograft[1]
Dosage: 60 mg/kg
Administration: Oral; daily; for 10 days
Result: Showed selective antitumor activity accompanied with phospho-Tyr426 YES1 suppression in xenograft tumors.
Molecular Weight

552.55

Formula

C₂₆H₂₂F₂N₆O₄S

CAS No.

2055918-71-1

SMILES

CS(=O)(NC1=CC2=C(C=C1C)C=C(C(C3=C(N)N(C4=C(C)C=C(OC5=C(F)C=CC=C5F)N=C4)N=C3)=O)N2)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

CH6953755CH 6953755CH-6953755SrcorallyYES1SRCfamilyantitumorGene-amplifiedcancersautophosphorylationTyr426phospho-Tyr426Inhibitorinhibitorinhibit

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CH6953755
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