An irreversible dual inhibitor of EGFR and HER2
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HKI 357

Item No. 14847

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(2E)-N-[4-[[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]amino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-2-butenamide
CAS Number
848133-17-5
Molecular Formula
C31H29ClFN5O3
Formula Weight
574.1
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly Soluble: 1-10 mg/mlEthanol: Sparingly Soluble: 1-10 mg/ml
SMILES
O=C(/C=C/CN(C)C)N([H])C1=C(OCC)C=C(N=CC(C#N)=C2N([H])C3=CC=C(OCC4=CC=CC(F)=C4)C(Cl)=C3)C2=C1
InChi Code
InChI=1S/C31H29ClFN5O3/c1-4-40-29-16-26-24(15-27(29)37-30(39)9-6-12-38(2)3)31(21(17-34)18-35-26)36-23-10-11-28(25(32)14-23)41-19-20-7-5-8-22(33)13-20/h5-11,13-16,18H,4,12,19H2,1-3H3,(H,35,36)(H,37,39)/b9-6+
InChi Key
NERXPXBELDBEPZ-RMKNXTFCSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $69

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    5 mg

    $263

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    10 mg

    $356

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    Product Description

    HKI 357 is an irreversible dual inhibitor of the EGF receptor tyrosine kinases EGFR and HER2 (IC50s = 34 and 33 nM, respectively).1 It inhibits proliferation of A431, SK-BR-3, and SW620 cancer cell lines (IC50s = 120, 2.5, and 511 nM, respectively). HKI 357 suppresses EGFR autophosphorylation and phosphorylation of the downstream effectors AKT and ERK in the gefitinib-susceptible and -resistant cell lines NCI-H1650 and NCI-H1650(G7), respectively.2 In vivo, HKI 357 (10 mg/kg) inhibits tumor growth in BT474, A431, and SUM190 mouse xenograft models.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Tsou, H.-R., Overbeek-Klumpers, E.G., Hallett, W.A., et al. Optimization of 6,7-disubstituted-4-(arylamino)quinoline-3-carbonitriles as orally active, irreversible inhibitors of human epidermal growth factor receptor-2 kinase activity. J. Med. Chem. 48(4), 1107-1131 (2005).

    2. Kwak, E.L., Sordella, R., Bell, D.W., et al. Irreversible inhibitors of the EGF receptor may circumvent acquired resistance to gefitinib. Proc. Natl. Acad. Sci. USA 102(21), 7665-7670 (2005).