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Defactinib hydrochloride

Catalog No. T15092 CAS 1073160-26-5

Synonyms: PF 04554878 hydrochloride, VS-6063 hydrochloride

Defactinib hydrochloride is a novel inhibitor of FAK. Which inhibits FAK phosphorylation at the Tyr397 site in a time- and dose-dependent manner.

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Defactinib hydrochloride, CAS 1073160-26-5

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100 mg	6-8 weeks	Inquiry

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Purity: 98.06%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Defactinib hydrochloride is a novel inhibitor of FAK. Which inhibits FAK phosphorylation at the Tyr397 site in a time- and dose-dependent manner.
In vitro	Defactinib inhibits pFAK expression within 3 hours, with a gradual return of expression by 48 hours. Defactinib inhibits FAK phosphorylation at the Tyr397 site in a time- and dose-dependent manner. RPPA data displays 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 [1].
In vivo	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). Defactinib (25 mg/kg; twice a day or greater statistically; 3 hours) treatment significantly inhibits pFAK (Tyr397), 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. In the SKOV3ip1 model, a 92.7% tumor weight reduction is observed in the combination group compared with PTX (P<0.001)[1].

Synonyms	PF 04554878 hydrochloride, VS-6063 hydrochloride
Molecular Weight	546.95
Formula	C20H22ClF3N8O3S
CAS No.	1073160-26-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 2 years

Solubility Information

DMSO: 22.5mg/mL (41.1mM), Need ultrasonic

H2O: 0.1 mg/mL (insoluble)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Kang Y, et al. Role of focal adhesion kinase in regulating YB-1-mediated resistance in ovarian cancer. J Natl Cancer Inst. 2013 Oct 2;105(19):1485-95.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Anti-Cancer Active Compound Library Anti-Cancer Compound Library Anti-Ovarian Cancer Compound Library Inhibitor Library Bioactive Compounds Library Max Bioactive Compound Library

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Related compounds with same targets

2119738-71-3 PF-03814735 5α-Hydroxycostic acid FAK inhibitor 2 Excisanin A Conteltinib Masitinib Chloropyramine hydrochloride

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Keywords

Defactinib hydrochloride 1073160-26-5 Angiogenesis Cytoskeletal Signaling Tyrosine Kinase/Adaptors FAK PF 04554878 hydrochloride VS-6063 hydrochloride inhibitor inhibit

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