A FAK inhibitor
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Defactinib

Item No. 17737

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-methyl-4-[[4-[[[3-[methyl(methylsulfonyl)amino]-2-pyrazinyl]methyl]amino]-5-(trifluoromethyl)-2-pyrimidinyl]amino]-benzamide
CAS Number
1073154-85-4
Synonyms
  • PF-04554878
  • VS-6063
Molecular Formula
C20H21F3N8O3S
Formula Weight
510.5
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 1 mg/mlDMSO: 1 mg/mlDMSO:PBS (pH 7.2) (1:3): 0.25 mg/ml
λmax
220, 307 nm
SMILES
O=C(NC)C1=CC=C(NC2=NC=C(C(F)(F)F)C(NCC3=NC=CN=C3N(C)S(C)(=O)=O)=N2)C=C1
InChi Code
InChI=1S/C20H21F3N8O3S/c1-24-18(32)12-4-6-13(7-5-12)29-19-28-10-14(20(21,22)23)16(30-19)27-11-15-17(26-9-8-25-15)31(2)35(3,33)34/h4-10H,11H2,1-3H3,(H,24,32)(H2,27,28,29,30)
InChi Key
FWLMVFUGMHIOAA-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $41

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    5 mg

    $128

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    10 mg

    $235

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    25 mg

    $389

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    Product Description

    Focal adhesion kinase (FAK) is a non-receptor tyrosine kinase that plays a vital role in many oncogenic pathways.1,2 Defactinib is a dose-dependent inhibitor of FAK, with maximal inhibition of FAK autophosphorylation in cells achieved at 10 µM.3 It is less effective against the related kinase PYK2. Defactinib restores the chemosensitivity of taxane-resistant cells to paclitaxel (Item No. 10461), although it is not cytotoxic alone.3 Defactinib decreases YB-1 phosphorylation and nuclear accumulation in an Akt-dependent manner. It is orally bioavailable, inhibiting FAK and augmenting paclitaxel action in suppressing the growth and number of ovarian cancer cell tumors in mice.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Schwock, J., Dhani, N., and Hedley, D.W. Targeting focal adhesion kinase signaling in tumor growth and metastasis. Expert Opin. Ther. Targets 14(1), 77-94 (2010).

    2. Lee, B.Y., Timpson, P., Horvath, L.G., et al. FAK signaling in human cancer as a target for therapeutics. Pharmacol. Ther. 146, 132-149 (2015).

    3. Kang, Y., Hu, W., Ivan, C., et al. Role of focal adhesion kinase in regulating YB-1-mediated paclitaxel resistance in ovarian cancer. JNCI 105(19), 1485-1495 (2013).