An EGFR receptor tyrosine kinase inhibitor
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Pelitinib

Item No. 15627

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[4-[(3-chloro-4-fluorophenyl)amino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-2E-butenamide
CAS Number
257933-82-7
Synonyms
  • EKB-569
Molecular Formula
C24H23ClFN5O2
Formula Weight
467.9
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20mg/mLDMF:PBS (pH 7.2) (1:5): 0.16 mg/mLDMSO: 10 mg/mL
λmax
209, 260, 283 nm
SMILES
FC(C=C1)=C(Cl)C=C1NC2=C(C#N)C=NC3=C2C=C(NC(/C=C/CN(C)C)=O)C(OCC)=C3
InChi Code
InChI=1S/C24H23ClFN5O2/c1-4-33-22-12-20-17(11-21(22)30-23(32)6-5-9-31(2)3)24(15(13-27)14-28-20)29-16-7-8-19(26)18(25)10-16/h5-8,10-12,14H,4,9H2,1-3H3,(H,28,29)(H,30,32)/b6-5+
InChi Key
WVUNYSQLFKLYNI-AATRIKPKSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    5 mg

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    $236

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    Product Description

    Pelitinib is a cyanoquinoline that irreversibly inhibits the EGFR receptor tyrosine kinase (IC50 = 39 nM).1 It inhibits HER2 with a much weaker potency (IC50 = 1.2 μM).1 By disrupting Akt and MAPK pathways, pelitinib can induce apoptosis and suppress the growth of tumor cell lines, displaying particularly strong efficacy against hepatocellular carcinoma cells (IC50s = ~2 μM).2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Arkin, M., and Moasser, M.M. HER2 directed small molecule antagonists. Curr. Opin. Investig. Drugs 9(12), 1264-1276 (2008).

    2. Kim, H., and Lim, H.Y. Novel EGFR-TK inhibitor EKB-569 inhibits hepatocellular carcinoma cell proliferation by AKT and MAPK pathways. J. Korean Med. Sci. 26(12), 1563-1568 (2011).