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Defactinib

Catalog No. T1996 CAS 1073154-85-4

Synonyms: PF-04554878, VS-6063

Defactinib (VS-6063) is an orally bioavailable, small-molecule focal adhesion kinase (FAK) inhibitor with potential antiangiogenic and antineoplastic activities.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Defactinib, CAS 1073154-85-4

Pack Size	Availability	Price/USD
1 mg	In stock	$ 31.00
2 mg	In stock	$ 41.00
5 mg	In stock	$ 67.00
10 mg	In stock	$ 87.00
25 mg	In stock	$ 153.00
50 mg	In stock	$ 247.00
100 mg	In stock	$ 347.00
200 mg	In stock	$ 597.00
500 mg	In stock	$ 935.00
1 g	In stock	$ 1,230.00
1 mL * 10 mM (in DMSO)	In stock	$ 75.00

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Purity: 99.8%

Purity: 98.51%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Defactinib (VS-6063) is an orally bioavailable, small-molecule focal adhesion kinase (FAK) inhibitor with potential antiangiogenic and antineoplastic activities.
In vitro	In both paclitaxel-sensitive and paclitaxel-resistant models, oral administration of VS-6063 (50 mg/kg) was able to induce growth inhibitory effects.
In vivo	In both paclitaxel-sensitive (SKOV3ip1) and paclitaxel-resistant (SKOV3-TR) cell lines, VS-6063 inhibits the expression of pFAK (Tyr397). In thyroid cancer cell lines, the combined application of VS-6063 and Y15 effectively suppresses cell adhesion and proliferation. Furthermore, in the cell lines SKOV3ip1, SKOV3-TR, HeyA8, and HeyA8-MDR, a synergistic effect between VS-6063 and paclitaxel significantly reduces cell proliferation and induces apoptosis.
Kinase Assay	Cell-free Kinase Activity Assays: IC50 values for TG101348 are determined commercially using the InVitrogen kinase profiling service for a 223 kinase screen that included JAK2 and JAK2V617F or Carna Biosciences for the screen of all Janus kinase family members including JAK1 and Tyk2. ATP concentration is set to approximately the Km value for each kinase.
Cell Research	Ovarian cancer cells are treated with increasing concentrations of VS-6063 for 96 hours and then subjected to the MTT assay. Results are confirmed with triplicate experiments.(Only for Reference)

Synonyms	PF-04554878, VS-6063
Molecular Weight	510.49
Formula	C20H21F3N8O3S
CAS No.	1073154-85-4

Storage

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

Solubility Information

DMSO: 50 mg/mL (97.94 mM)

References and Literature

1. Kang Y, et al. J Natl Cancer Inst. 2013, 105(19), 1485-1495. 2. O'Brien S, et al. Oncotarget. 2014, 5(17), 7945-7959. 3. Su Y, Li R, Ning X, et al. Discovery of 2, 4-diarylaminopyrimidine derivatives bearing dithiocarbamate moiety as novel FAK inhibitors with antitumor and anti-angiogenesis activities[J]. European Journal of Medicinal Chemistry. 2019 May 18;177:32-46.

Citations

1. Su Y, Li R, Ning X, et al. Discovery of 2, 4-diarylaminopyrimidine derivatives bearing dithiocarbamate moiety as novel FAK inhibitors with antitumor and anti-angiogenesis activities. European Journal of Medicinal Chemistry. 2019 May 18;177:32-46 2. Li R, Gong L, Sun J, et al.Discovery of 2, 4-diarylaminopyrimidine derivatives bearing sulfonamide moiety as novel FAK inhibitors.Bioorganic Chemistry.2024: 107134.

Related compound libraries

This product is contained In the following compound libraries：

Tyrosine Kinase Inhibitor Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Inhibitor Library Drug Repurposing Compound Library Anti-Cancer Active Compound Library Anti-Cancer Compound Library Clinical Compound Library NO PAINS Compound Library Target-Focused Phenotypic Screening Library

Related Products

Related compounds with same targets

Masitinib mesylate FAK-IN-10 Excisanin A Defactinib hydrochloride PF-431396 GSK2256098 Masitinib PF-562271

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Keywords

Defactinib 1073154-85-4 Angiogenesis Cytoskeletal Signaling Tyrosine Kinase/Adaptors FAK PTK2 protein tyrosine kinase 2 PTK2 inhibit PF-04554878 Inhibitor PF 04554878 PF04554878 Focal adhesion kinase VS6063 VS-6063 VS 6063 inhibitor

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