1. Protein Tyrosine Kinase/RTK
  2. FAK
  3. Defactinib hydrochloride

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

Cat. No.: HY-12289A Purity: 99.11%
Handling Instructions

Defactinib hydrochloride (VS-6063 hydrochloride; PF 04554878 hydrochloride) is a novel FAK inhibitor, which inhibits FAK phosphorylation at the Tyr397 site in a time- and dose-dependent manner.

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

Defactinib hydrochloride Chemical Structure

Defactinib hydrochloride Chemical Structure

CAS No. : 1073160-26-5

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Customer Review

Based on 7 publication(s) in Google Scholar

Other Forms of Defactinib hydrochloride:

Top Publications Citing Use of Products

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

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

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    • Customer Review

    Description

    Defactinib hydrochloride (VS-6063 hydrochloride; PF 04554878 hydrochloride) is a novel FAK inhibitor, which inhibits FAK phosphorylation at the Tyr397 site in a time- and dose-dependent manner.

    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].

    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].

    Clinical Trial
    Molecular Weight

    546.95

    Formula

    C₂₀H₂₂ClF₃N₈O₃S

    CAS No.

    1073160-26-5

    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.[H]Cl

    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 : 30 mg/mL (54.85 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.8283 mL 9.1416 mL 18.2832 mL
    5 mM 0.3657 mL 1.8283 mL 3.6566 mL
    10 mM 0.1828 mL 0.9142 mL 1.8283 mL
    *Please refer to the solubility information to select the appropriate solvent.
    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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    Defactinib hydrochloride
    Cat. No.:
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