Defactinib (VS-6063, PF-04554878)

Catalog No.S7654

Defactinib (VS-6063, PF-04554878) Chemical Structure

Molecular Weight(MW): 510.49

Defactinib (VS-6063, PF-04554878) is a selective, and orally active FAK inhibitor. Phase 2.

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USD 107 In stock
USD 297 In stock
USD 557 In stock
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1 Customer Review

  • (C) D2.A1 cells were pretreated for 18 hours with the indicated concentration of Defactinib. (D) D2.A1 cells were pretreated for 10 minutes with indicated concentrations of Defactinib. cells were serum starved for 18 hours with or without inhibitor pretreatment and cells were subsequently stimulated with FGF2 (20ng/ml) for 30 minutes and analyzed by immunoblot for downstream phosphorylation of Erk1/2. Expression of total Erk1/2 was analyzed as a loading control.

    Mol Cancer Ther, 2016, 15(9):2096-106. Defactinib (VS-6063, PF-04554878) purchased from Selleck.

Purity & Quality Control

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Biological Activity

Description Defactinib (VS-6063, PF-04554878) is a selective, and orally active FAK inhibitor. Phase 2.
Targets
FAK [1]
In vitro

In taxane-sensitive (SKOV3ip1) and taxane-resistant (SKOV3-TR) cell lines, VS-6063 significantly inhibits pFAK (Tyr397) expression. The combination of VS-6063 and paclitaxel synergistically decreases proliferation and increases apoptosis in SKOV3ip1, SKOV3-TR, HeyA8 and HeyA8-MDR cells. [1] The combination of VS-6063 and Y15 synergistically decreases viability, clonogenicity, and cell attachment in thyroid cancer cell lines. [2]

In vivo In both PTX-sensitive and PTX-resistant models, VS-6063 (50 mg/kg p.o.) enhances tumor growth inhibition by paclitaxel. [1]

Protocol

Cell Research:[1]
+ Expand
  • Cell lines: SKOV3ip1, SKOV3-TR, HeyA8 and HeyA8-MDR cells
  • Concentrations: ~10 μM
  • Incubation Time: 96 hours
  • Method: 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)
Animal Research:[1]
+ Expand
  • Animal Models: Mice bearing SKOV3ip1, SKOV3-TR, HeyA8 or HeyA8-MDR tumors
  • Formulation: PBS
  • Dosages: 50 mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 5 mg/mL warmed (9.79 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents individually and in order:
5% DMSO+50% PEG 300+5% Tween 80+ddH2O
5mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 510.49
Formula

C20H21F3N8O3S

CAS No. 1073154-85-4
Storage powder
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02758587 Not yet recruiting Carcinoma, Non-small-cell Lung|Mesothelioma|Pancreatic Neoplasms NHS Greater Glasgow and Clyde|University of Glasgow|Cancer Research UK|Merck Sharp & Dohme Corp.|Verastem, Inc.|University of Edinburgh|University of Southampton|University of Leicester|Queens University, Belfast June 2016 Phase 1|Phase 2
NCT02546531 Recruiting Advanced Solid Tumors|Solid Tumors|Pancreatic Cancer Washington University School of Medicine January 2016 Phase 1
NCT02913716 Completed Healthy Subjects Verastem, Inc. August 2015 Phase 1
NCT02465060 Recruiting Advanced Malignant Neoplasm|Lymphoma|Recurrent Plasma Cell Myeloma|Recurrent Solid Neoplasm|Refractory Malignant Neoplasm|Refractory Plasma Cell Myeloma National Cancer Institute (NCI) August 2015 Phase 2
NCT01943292 Completed Non Hematologic Cancers Verastem, Inc. September 2013 Phase 1
NCT01870609 Terminated Malignant Pleural Mesothelioma Verastem, Inc. September 2013 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID