2. Protein Tyrosine Kinase/RTK
  3. FAK
  4. Defactinib

Defactinib  (Synonyms: VS-6063; PF-04554878)

Cat. No.: HY-12289 Purity: 99.87%
COA Handling Instructions

Defactinib (VS-6063; PF-04554878) is a novel FAK inhibitor with potential antiangiogenic and antineoplastic activities.

For research use only. We do not sell to patients.

Defactinib Chemical Structure

Defactinib Chemical Structure

CAS No. : 1073154-85-4

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Solution
10 mM * 1 mL in DMSO USD 94 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
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Estimated Time of Arrival: December 31
Solid
5 mg USD 84 In-stock
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10 mg USD 108 In-stock
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50 mg USD 300 In-stock
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100 mg USD 420 In-stock
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200 mg USD 720 In-stock
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Customer Review

Based on 26 publication(s) in Google Scholar

Other Forms of Defactinib:

Top Publications Citing Use of Products

    Defactinib purchased from MCE. Usage Cited in: J Exp Clin Cancer Res. 2018 Jul 28;37(1):175.  [Abstract]

    Western blot verified the inhibition of FAK Y397 phosphorylation via Defactinib in MCF7-YAP-S127A and MDA-MB-231 cells.

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Defactinib (VS-6063; PF-04554878) is a novel FAK inhibitor with potential antiangiogenic and antineoplastic activities.

    IC50 & Target

    FAK[1]
    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[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    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)[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    Molecular Weight

    510.49

    Appearance

    Solid

    Formula

    C20H21F3N8O3S
    CAS No.
    SMILES

    O=C(NC)C1=CC=C(NC2=NC=C(C(F)(F)F)C(NCC3=NC=CN=C3N(C)S(=O)(C)=O)=N2)C=C1
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (97.95 mM; Need ultrasonic)

    H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.9589 mL 9.7945 mL 19.5890 mL
    5 mM 0.3918 mL 1.9589 mL 3.9178 mL
    10 mM 0.1959 mL 0.9795 mL 1.9589 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% saline

      Solubility: 2.5 mg/mL (4.90 mM); Suspended solution; Need ultrasonic

    • 2.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.08 mg/mL (4.07 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.08 mg/mL (4.07 mM); Clear solution

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 99.87%

    COA (248 KB) LCMS (112 KB)

    Handling Instructions (2659 KB)
    References
    Animal Administration
    [1]

    Mice[1]
    To determine the antitumor effects of Defactinib, SKOV3ip1, SKOV3-TR, HeyA8, and HeyA8-MDR cells are injected intraperitoneally. One week after tumor cell injection, mice are randomly assigned to 4 groups of 10 mice (control, PTX alone, Defactinib alone, and PTX with Defactinib); treatment is initiated at 3-4 weeks following injection. PTX at 2 mg/kg (SKOV3ip1 and SKOV3-TR) or 2.5 mg/kg (HeyA8 and HeyA8-MDR) is given intraperitoneally weekly; Defactinib at 25 mg/kg is given orally twice every day. Control mice received HBSS intraperitoneally once a week and vehicle orally twice every day. Mice are monitored daily for adverse effects of therapy and are killed on day 35 (SKOV3ip1 or SKOV3-TR), day 28 (HeyA8 or HeyA8-MDR), or when any of the mice seemed moribund. Total body weight, tumor incidence and mass, and the number of tumor nodules are recorded. Tumors are either fixed in formalin or embedded in paraffin or snap frozen in optimal cutting temperature (OCT) compound in liquid nitrogen.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    References
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    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Keywords:

    Defactinib1073154-85-4VS-6063 PF-04554878VS6063VS 6063PF04554878PF 04554878PF-04554878FAKPTK2 protein tyrosine kinase 2PTK2Focal adhesion kinaseInhibitorinhibitorinhibit

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