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Defactinib

CAS No. : 1073154-85-4

MCE 站：Defactinib

产品活性：Defactinib (VS-6063; PF-04554878) 是一种新型 FAK 抑制剂，抑制 FAK 在 Tyr397 位点磷酸化，这种作用具有时间和剂量依赖性。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：FAK

In Vitro: Defactinib (VS-6063) inhibits FAK phosphorylation at the Tyr397 site in a time- ａnd dose-dependent manner. RPPA data shows that Defactinib reduces levels of AKT ａnd YB-1 in taxane-resistant cell lines. The expression of pFAK (Tyr397) is statistically significantly inhibited by Defactinib in a dose-dependent manner in all cell lines. Defactinib inhibits pFAK (Tyr397) expression within 3 hours, with a gradual return of expression by 48 hours.

In Vivo: Defactinib (VS-6063) doses of 25 mg/kg twice a day or greater statistically significantly inhibits pFAK (Tyr397) at 3 hours, with return of expression noted by 24 hours. Therefore, administration of Defactinib at 25 mg/kg twice a day is selected as the dosing schedule for subsequent therapy experiments. For therapy experiments, female nude mice bearing HeyA8 tumors in the peritoneal cavity are randomly divided into 4 groups (n=10 per group): 1) vehicle orally twice daily ａnd phosphate-buffered saline intraperitoneally weekly (control); 2) Defactinib 25 mg/kg orally twice daily; 3) PTX intraperitoneally weekly; ａnd 4) both VDefactinib 25 mg/kg orally twice daily ａnd PTX intraperitoneally weekly. There is an 87.4% reduction in tumor weight by PTX monotherapy in the HeyA8 model, ａnd combination therapy resulted in the greatest tumor weight reduction, with a 97.9% reduction (P=0.05 compared with PTX). In the SKOV3ip1 model, a 92.7% tumor weight reduction is observed in the combination group compared with PTX (P<0.001).

相关产品：Drug Repurposing Compound Library Plus  |  Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  Kinase Inhibitor Library  |  Protein Tyrosine Kinase Compound Library  |  Anti-Cancer Compound Library  |  Clinical Compound Library  |  Drug Repurposing Compound Library  |  Anti-COVID-19 Compound Library  |  Cytoskeleton Compound Library  |  Chemical Probe Library  |  Anti-Pancreatic Cancer Compound Library  |  PF-573228  |  PND-1186  |  Y15  |  Masitinib  |  PF-562271  |  SU6656  |  GSK2256098  |  Fangchinoline  |  NVP-TAE 226  |  Defactinib hydrochloride  |  PROTAC FAK degrader 1  |  BI-3663  |  ALK inhibitor 1  |  Nitidine chloride  |  PF-431396  |  CEP-37440  |  BI-4464  |  Conteltinib  |  ALK inhibitor 2  |  Chloropyramine hydrochloride  |  NAMI-A  |  Batatasin III  |  FAK inhibitor 2  |  FAK inhibitor 5  |  GSK215  |  Petunidin chloride

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