A dual inhibitor of EGFR and ErbB2 (IC50s = 19 and 3 nM

Lapatinib – 100 mg

Brand:
Cayman
CAS:
231277-92-2
Storage:
-20
UN-No:
Non-Hazardous - /

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 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).{36874} 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.{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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SKU: 11493 - 100 mg Category:

Description

A dual inhibitor of EGFR and ErbB2 (IC50s = 19 and 3 nM, respectively); 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); inhibits the growth of ErbB2-amplified OD19 esophageal and NCI-N87 gastric cancer cells (IC50s = 0.09 and 0.01 μM, respectively); inhibits the growth of gastric cancer cells in which ErbB2 is not amplified (IC50s = 0.35-8.58 μM); induces apoptosis in NCI-N87 and OD19 cells at 1 μM; reduces tumor growth in a BT474 breast cancer mouse xenograft model at 50 mg/kg; reduces tumor growth in an NCI-N87 mouse xenograft model at 100 mg/kg and induces tumor regression when used in combination with trastuzumab

Formal name: N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[[[2-(methylsulfonyl)ethyl]amino]methyl]-2-furanyl]-4-quinazolinamine

Synonyms:  GSK 572016|GW 572016

Molecular weight: 581.1

CAS: 231277-92-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|EGFR/ErbB/HER Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling

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