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

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

製品番号: HY-12289 純度: 99.74%
取扱説明書

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

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Defactinib 構造式

Defactinib 構造式

CAS 番号 : 1073154-85-4

容量 価格(税別) 在庫状況 数量
無料サンプル (0.5-1 mg)   今すぐ申し込む  
10 mM * 1  mL in DMSO USD 94 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 84 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 108 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 300 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 420 在庫あり
Estimated Time of Arrival: December 31
200 mg USD 720 在庫あり
Estimated Time of Arrival: December 31
500 mg   お問い合わせ  
1 g   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

カスタマーレビュー

Based on 10 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.

    Western blot verified the inhibition of FAK Y397 phosphorylation via Defactinib in MCF7-YAP-S127A and MDA-MB-231 cells.
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    • 純度とドキュメンテーション

    • 参考文献

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    製品説明

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

    IC50 & Target

    FAK[1]

    体外実験

    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].

    体内実験

    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].

    臨床実験
    分子量

    510.49

    分子式

    C₂₀H₂₁F₃N₈O₃S

    CAS 番号

    1073154-85-4

    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

    輸送条件

    Room temperature in continental US; may vary elsewhere.

    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

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

    H2O : < 0.1 mg/mL (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.
    体内:
    • 1.

      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

    • 2.

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

      Solubility: ≥ 2.5 mg/mL (4.90 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    参考文献
    動物実験
    [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 はこれらの方法の精度を確認していません。 こちらは参照専用です。

    参考文献

    純度: 99.74%

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    Keywords:

    DefactinibVS-6063PF-04554878VS6063VS 6063PF04554878PF 04554878FAKPTK2 protein tyrosine kinase 2PTK2Focal adhesion kinaseInhibitorinhibitorinhibit

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    製品名:
    Defactinib
    製品番号:
    HY-12289
    数量:
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