A FAK inhibitor
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Narmafotinib

Item No. 45335

Technical Information
Formal Name
2-[2-[2-[[2-methoxy-4-(1-methyl-4-piperidinyl)phenyl]amino]-5-(trifluoromethyl)-4-pyrimidinyl]ethyl]-benzeneacetamide
CAS Number
1393653-34-3
Synonyms
  • AMP945
  • CTx-0294945
Molecular Formula
C28H32F3N5O2
Formula Weight
Purity
≥98%
A solid
Acetonitrile:Water (1:1): Slightly soluble: 0.1-1 mg/ml
SMILES
FC(F)(F)C1=CN=C(NC2=CC=C(C3CCN(CC3)C)C=C2OC)N=C1CCC4=C(CC(N)=O)C=CC=C4
InChi Code
InChI=1S/C28H32F3N5O2/c1-36-13-11-19(12-14-36)21-8-10-24(25(15-21)38-2)35-27-33-17-22(28(29,30)31)23(34-27)9-7-18-5-3-4-6-20(18)16-26(32)37/h3-6,8,10,15,17,19H,7,9,11-14,16H2,1-2H3,(H2,32,37)(H,33,34,35)
InChi Key
AWJVIOYPZZZYAX-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Narmafotinib is an inhibitor of focal adhesion kinase (FAK).1 It inhibits autophosphorylation of FAK at tyrosine 397 in MDA-MB-231 breast cancer cells (IC50 = 7 nM). Narmafotinib (80 mg/kg), in combination with bevacizumab, reduces tumor growth in an MDA-MB-231 orthotopic mouse model of breast cancer. It also induces intratumoral apoptosis, reduces tumor growth, and increases survival in subcutaneous and orthotopic patient-derived xenograft (PDX) mouse models of pancreatic cancer when administered at a dose of 10 mg/kg in a cycle with the FOLFIRINOX regimen, which includes leucovorin, 5-fluorouracil (Item No. 14416), irinotecan (Item No. 14180), and oxaliplatin (Item No. 13106).2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Street, I., de Sylva, M., Lackovic, K., et alAbstract LB-308: Combination of CTx-0294945 a highly selective inhibitor of focal adhesion kinase with bevacizumab in pre-clinical models of breast cancer. Cancer Res. 72(8_Supplement), (2012).

    2. Burns, C., Murphy, K., Cock, T.-A., et alThe effect of adding a selective FAK inhibitor AMP945 to FOLFIRINOX in a model of pancreatic cancer. J. Clin. Oncol. 41(16_Suppl), (2023).