Lapatinib

Lapatinib

CAT N°: 11493
Price:

From 85.00 72.25

Lapatinib is a dual inhibitor of the EGF receptor (EGFR) and ErbB2 (IC50s = 19 and 3 nM, respectively).{24151} 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 ?M, respectively). Lapatinib also inhibits the growth of ErbB2-amplified OD19 esophageal and NCI-N87 gastric cancer cells (IC50s = 0.09 and 0.01 ?M, respectively) as well as several types of gastric cancer cells in which ErbB2 is not amplified (IC50s = 0.35-8.58 ?M).{36874} It induces apoptosis in NCI-N87 and OD19 cells when used at a concentration of 1 ?M. Lapatinib (50 mg/kg) reduces tumor growth in a BT474 breast cancer mouse xenograft model.{36875} 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.{36874} Formulations containing lapatinib have been used in combination with other therapeutics in the treatment of HER2-overexpressing breast cancer.

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[[[2-(methylsulfonyl)ethyl]amino]methyl]-2-furanyl]-4-quinazolinamine
  • Correlated keywords
    • 388082-78-8 tyrosines kinases 2 HER-2 ErbB 1 ErbB1 EGFR2 HER-2 ErbB epidermal growth factors dual GSKs GWs 572016 GSK572016 GW572016 GW572016X GW-572016X 572016X A-431 SKBR3 SKBR-3 ERb-B2 OD-19 NCIN87 Tyverb
  • Product Overview:
    Lapatinib is a dual inhibitor of the EGF receptor (EGFR) and ErbB2 (IC50s = 19 and 3 nM, respectively).{24151} 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 ?M, respectively). Lapatinib also inhibits the growth of ErbB2-amplified OD19 esophageal and NCI-N87 gastric cancer cells (IC50s = 0.09 and 0.01 ?M, respectively) as well as several types of gastric cancer cells in which ErbB2 is not amplified (IC50s = 0.35-8.58 ?M).{36874} It induces apoptosis in NCI-N87 and OD19 cells when used at a concentration of 1 ?M. Lapatinib (50 mg/kg) reduces tumor growth in a BT474 breast cancer mouse xenograft model.{36875} 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.{36874} Formulations containing lapatinib have been used in combination with other therapeutics in the treatment of HER2-overexpressing breast cancer.

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