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.
Product information
CAS Number: 2055918-71-1
Molecular Weight: 552.55
Formula: C26H22F2N6O4S
Chemical Name: N-(2-{5-amino-1-[6-(2,6-difluorophenoxy)-4-methylpyridin-3-yl]-1H-pyrazole-4-carbonyl}-5-methyl-1H-indol-6-yl)methanesulfonamide
Smiles: CC1C=C2C=C(NC2=CC=1NS(C)(=O)=O)C(=O)C1C=NN(C=1N)C1=CN=C(C=C1C)OC1C(F)=CC=CC=1F
InChiKey: YVXUHNOWRKWXSJ-UHFFFAOYSA-N
InChi: InChI=1S/C26H22F2N6O4S/c1-13-7-15-9-21(32-20(15)10-19(13)33-39(3,36)37)24(35)16-11-31-34(26(16)29)22-12-30-23(8-14(22)2)38-25-17(27)5-4-6-18(25)28/h4-12,32-33H,29H2,1-3H3
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 125 mg/mL (226.22 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
CH6953755 (0.001-1 μM; for 4 days) inhibits the cell growth of YES1-amplified cancer cell lines. 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. CH6953755 (0.1, 0.3, 1, 3 μM) suppresses TEAD luciferase reporter activity in YES1-amplified KYSE70 and RERF-LC-AI.
In Vivo:
CH6953755 (oral; 60 mg/kg/day; for 10 days) shows selective antitumor activity accompanied with phospho-Tyr426 YES1 suppression in xenograft tumors. CH6953755 (oral; 7.5, 15, 30, 60 mg/kg) suppresses phospho-Tyr426 YES1 in a dose-dependent manner.
Products are for research use only. Not for human use.
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