An inhibitor of IGF-1R
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PQ401

Item No. 20979

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-(5-chloro-2-methoxyphenyl)-N'-(2-methyl-4-quinolinyl)-urea
CAS Number
196868-63-0
Molecular Formula
C18H16ClN3O2
Formula Weight
341.8
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: 50 mMEthanol: 25 mM
SMILES
CC1=NC2=CC=CC=C2C(NC(NC3=C(OC)C=CC(Cl)=C3)=O)=C1
InChi Code
InChI=1S/C18H16ClN3O2/c1-11-9-15(13-5-3-4-6-14(13)20-11)21-18(23)22-16-10-12(19)7-8-17(16)24-2/h3-10H,1-2H3,(H2,20,21,22,23)
InChi Key
YBLWOZUPHDKFOT-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $86

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    10 mg

    $135

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    50 mg

    $587

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    Product Description

    PQ401 is an inhibitor of insulin-like growth factor 1 receptor (IGF-1R).1 It inhibits autophosphorylation of the recombinant IGF-1R kinase domain (IC50 = <1 μM) in a cell-free assay as well as IGF-1-stimulated IGF-1R autophosphorylation in MCF-7 cells (IC50 = 12 μM). PQ401 reduces cell viability of U87MG glioma cells with an IC50 value of 5 μM and induces apoptosis and inhibits cell migration in a concentration-dependent manner.2 It inhibits IGF-1-stimulated proliferation of MCF-7 cells in vitro (IC50 = 6 μM) and reduces tumor growth in an MCNeuA model of murine breast cancer when administered at doses of 50 and 100 mg/kg.1 PQ401 also has antimalarial activity against the P. falciparum strain 3D7 (EC50 = 53 nM).3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Gable, K.L., Maddux, B.A., Penaranda, C., et al. Diarylureas are small-molecule inhibitors of insulin-like growth factor I receptor signaling and breast cancer cell growth. Mol. Cancer Ther. 5(4), 1079-1086 (2006).

    2. Zhou, X., Zhao, X., Li, X., et al. PQ401, an IGF-1R inhibitor, induces apoptosis and inhibits growth, proliferation and migration of glioma cells. J. Chemother. 28(1), 44-49 (2016).

    3. Zhang, Y., Anderson, M., Weisman, J.L., et al. Evaluation of diarylureas for activity against Plasmodium falciparum. ACS Med. Chem. Lett. 1(9), 460-465 (2010).