A dual inhibitor of EGFR and ErbB2
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Lapatinib

Item No. 11493

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[[[2-(methylsulfonyl)ethyl]amino]methyl]-2-furanyl]-4-quinazolinamine
CAS Number
231277-92-2
Synonyms
  • GSK 572016
  • GW 572016
Molecular Formula
C29H26ClFN4O4S
Formula Weight
581.1
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 20 mg/mlDMSO:PBS(pH 7.2) (1:2): 0.33 mg/ml
λmax
245, 262, 306, 332, 362 nm
SMILES
O=S(CCNCC(O1)=CC=C1C2=CC3=C(N=CN=C3NC4=CC=C(OCC5=CC(F)=CC=C5)C(Cl)=C4)C=C2)(C)=O
InChi Code
InChI=1S/C29H26ClFN4O4S/c1-40(36,37)12-11-32-16-23-7-10-27(39-23)20-5-8-26-24(14-20)29(34-18-33-26)35-22-6-9-28(25(30)15-22)38-17-19-3-2-4-21(31)13-19/h2-10,13-15,18,32H,11-12,16-17H2,1H3,(H,33,34,35)
InChi Key
BCFGMOOMADDAQU-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $63

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    Product Description

    Lapatinib is a dual inhibitor of the EGF receptor (EGFR) and ErbB2 (IC50s = 19 and 3 nM, respectively).1 It inhibits the growth of EGFR-overexpressing A431 skin cancer and ErbB2-overexpressing SK-BR-3 breast cancer cells (IC50s = 0.14 and 0.124 μM, respectively). Lapatinib also inhibits the growth of ErbB2-amplified OD19 esophageal and NCI-N87 gastric cancer cells (IC50s = 0.09 and 0.01 μM, respectively) as well as several types of gastric cancer cells in which ErbB2 is not amplified (IC50s = 0.35-8.58 μM).2 It induces apoptosis in NCI-N87 and OD19 cells when used at a concentration of 1 μM. Lapatinib (50 mg/kg) reduces tumor growth in a BT474 breast cancer mouse xenograft model.3 It also reduces tumor growth in an NCI-N87 mouse xenograft model when administered at a dose of 100 mg/kg and induces tumor regression when used in combination with trastuzumab.2 Formulations containing lapatinib have been used in combination with other therapeutics in the treatment of HER2-overexpressing breast cancer.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Cho, T.P., Jun, F., Li, H., et al. Synthesis and biological evaluation of pyrrolopyridazine derivatives as novel HER-2 tyrosine kinase inhibitors. Bioorg. Med. Chem. Lett. 19(22), 6437-6440 (2009).

    2. Wainberg, Z.A., Anghel, A., Desai, A.J., et al. Lapatinib, a dual EGFR and HER2 kinase inhibitor, selectively inhibits HER2-amplified human gastric cancer cells and is synergistic with trastuzumab in vitro and in vivo. Clin. Cancer Res. 16(5), 1509-1519 (2010).

    3. Chefrour, M., Milano, G., Formento, P., et al. Positive interaction between lapatinib and capecitabine in human breast cancer models: Study of molecular determinants. Fundam. Clin. Pharmacol. 26(4), 530-537 (2012).