CH6953755

Research use only, not for human use.

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.

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.

Cell Viability Assay 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 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

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

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Angiogenesis

Src

Src

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2055918-71-1

552.55

C26H22F2N6O4S

>98% (HPLC)

In Vitro:?DMSO : 125 mg/mL (226.22 mM; Ultrasonic )

Cc1cc2cc([nH]c2cc1NS(C)(=O)=O)C(=O)c1cnn(c1N)-c1cnc(Oc2c(F)cccc2F)cc1C

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(-20℃)

With Ice Pack

≥ 2 years