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Defactinib hydrochloride

Catalog No. T15092 CAS 1073160-26-5

Synonyms: VS-6063 hydrochloride, PF 04554878 hydrochloride

Defactinib hydrochloride (PF 04554878 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 Chemical Structure

Defactinib hydrochloride, CAS 1073160-26-5

Pack Size	Availability	Price/USD	Quantity
2 mg	5 days	$ 43.00
5 mg	6-8 weeks	$ 67.00

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Purity: 98.06%

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Storage & Solubility Information

Description	Defactinib hydrochloride (PF 04554878 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 suppresses pFAK (protein Focal Adhesion Kinase) expression within three hours, exhibiting a dose-dependent inhibition, particularly at the Tyr397 phosphorylation site, and showing a reduction in expression levels by 48 hours. It effectively diminishes FAK phosphorylation over time and in correlation with the administered dose. Additionally, Reverse Phase Protein Array (RPPA) analysis reveals that Defactinib lowers AKT and YB-1 levels in taxane-resistant cell lines. The inhibition of pFAK (Tyr397) by Defactinib is confirmed to be statistically significant and dose-responsive across various cell lines, as documented in source [1].
In vivo	In the HeyA8 model, PTX monotherapy achieved an 87.4% decrease in tumor weight, while combination therapy yielded a superior 97.9% reduction (P=0.05 compared with PTX). Defactinib treatment at 25 mg/kg, administered orally twice daily, significantly decreased pFAK (Tyr397) levels, with effects reversing within 24 hours, establishing this dose for further experiments. For these, female nude mice with HeyA8 tumors in the peritoneal cavity were divided into four groups (n=10 each): 1) control group receiving vehicle and phosphate-buffered saline, 2) Defactinib (25 mg/kg orally, twice daily), 3) PTX weekly, and 4) both Defactinib and PTX. The SKOV3ip1 model demonstrated a 92.7% tumor weight reduction with the combination therapy compared to PTX alone (P<0.001)[1].

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

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 22.5 mg/mL (41.1 mM), Sonification is recommended.

H2O: 0.1 mg/mL (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 Inhibitor Library Anti-Ovarian Cancer Compound Library Anti-Cancer Active Compound Library

Related Products

Related compounds with same targets

PF-562271 hydrochloride YH-306 NAMI-A CEP-37440 Inulicin Chloropyramine hydrochloride GSK215 Compound 1T-0219 (SC)

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Keywords

Defactinib hydrochloride 1073160-26-5 Angiogenesis Cytoskeletal Signaling Tyrosine Kinase/Adaptors FAK VS-6063 hydrochloride PF 04554878 hydrochloride PF04554878 Hydrochloride VS-6063 Hydrochloride VS6063 Hydrochloride PF-04554878 Hydrochloride Defactinib Hydrochloride PF 04554878 Hydrochloride VS 6063 Hydrochloride inhibitor inhibit

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