A dual MET/AXL inhibitor
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NPS 1034

Item No. 19627

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-(4-fluorophenyl)-N-[3-fluoro-4-[(3-phenyl-1H-pyrrolo[2,3-b]pyridin-4-yl)oxy]phenyl]-2,3-dihydro-1,5-dimethyl-3-oxo-1H-pyrazole-4-carboxamide
CAS Number
1221713-92-3
Molecular Formula
C31H23F2N5O3
Formula Weight
551.6
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 25 mg/mlDMSO:PBS (pH 7.2)(1:5): 0.16 mg/mlEthanol: 1 mg/ml
λmax
286 nm
SMILES
FC(C=C(NC(C1=C(C)N(C)N(C2=CC=C(F)C=C2)C1=O)=O)C=C3)=C3OC4=C5C(NC=C5C6=CC=CC=C6)=NC=C4
InChi Code
InChI=1S/C31H23F2N5O3/c1-18-27(31(40)38(37(18)2)22-11-8-20(32)9-12-22)30(39)36-21-10-13-25(24(33)16-21)41-26-14-15-34-29-28(26)23(17-35-29)19-6-4-3-5-7-19/h3-17H,1-2H3,(H,34,35)(H,36,39)
InChi Key
RGAZVGZUBCFHRJ-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

    $178

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    10 mg

    $293

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    25 mg

    $583

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    Product Description

    NPS 1034 is a dual inhibitor of the receptor tyrosine kinase activities of MET (IC50 = 48 nM) and AXL (IC50 = 10.3 nM), receptors for hepatocyte growth factor and vitamin K-dependent proteins, respectively.1 It synergistically inhibits cell proliferation when used in combination with gefitinib (Item No. 13166) or erlotinib (Item No. 10483) in NSCLC cells with acquired resistance to EGFR receptor tyrosine kinase inhibitors.1 NPS 1034 inhibits autophosphorylation of numerous constitutively active mutant forms of MET (IC50s <25 nM) and inhibits the invasion and migration of MET mutant-transfected cells.2 It also inhibits growth of MKN45 xenograft tumors in mice treated orally with 30 mg/kg NPS 1034 for 25 days.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Rho, J.K., Choi, Y.J., Kim, S.Y., et al. MET and AXL inhibitor NPS-1034 exerts efficacy against lung cancer cells resistant to EGFR kinase inhibitors because of MET or AXL activation. Cancer Res. 74(1), 253-262 (2014).

    2. Shin, J.-S., Hong, S.-W., Moon, J.-H., et al. NPS-1034, a novel MET inhibitor, inhibits the activated MET receptor and its constitutively active mutants. Invest New Drugs 32(3), 389-399 (2014).