A multi-kinase inhibitor
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XL647

Item No. 27049

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-(3,4-dichloro-2-fluorophenyl)-6-methoxy-7-[[(3aα,5β,6aα)-octahydro-2-methylcyclopenta[c]pyrrol-5-yl]methoxy]-4-quinazolinamine
CAS Number
781613-23-8
Synonyms
  • EXEL-7647
  • Tesevatinib
Molecular Formula
C24H25Cl2FN4O2
Formula Weight
491.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 10 mg/mlEthanol: 10 mg/ml
λmax
233, 250, 331 nm
SMILES
ClC1=C(Cl)C(F)=C(NC2=NC=NC3=C2C=C(OC)C(OC[C@@H]4C[C@@](CN(C)C5)([H])[C@@]5([H])C4)=C3)C=C1
InChi Code
InChI=1S/C24H25Cl2FN4O2/c1-31-9-14-5-13(6-15(14)10-31)11-33-21-8-19-16(7-20(21)32-2)24(29-12-28-19)30-18-4-3-17(25)22(26)23(18)27/h3-4,7-8,12-15H,5-6,9-11H2,1-2H3,(H,28,29,30)/t13-,14-,15+
InChi Key
HVXKQKFEHMGHSL-QKDCVEJESA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $107

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    5 mg

    $396

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    10 mg

    $740

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    Product Description

    XL647 is a multi-kinase inhibitor (IC50s = 0.3, 16, 1.5, 8.7, and 1.4 nM for EGFR, ErbB2, KDR, FLT4, and EphB4, respectively).1 It is selective for these kinases over a panel of 10 tyrosine kinases and 55 serine/threonine kinases at 10 μM. XL647 inhibits growth of A431 cells expressing wild-type EGFR and H1975 non-small cell lung cancer (NSCLC) cells expressing both the activating mutant EGFRL858R and the drug resistance-associated mutant EGFRT790M (IC50s = 13 and 920 nM, respectively). In vivo, XL647 (10, 30, and 100 mg/kg) inhibits tumor growth and EGFR phosphorylation in an H1975 mouse xenograft model in a dose-dependent manner.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Gendreau, S.B., Ventura, R., Keast, P., et al. Inhibition of the T790M gatekeeper mutant of the epidermal growth factor receptor by EXEL-7647. Clin. Cancer Res. 13(12), 3713-3723 (2007).