Lapatinib


CAS No. : 231277-92-2

(Synonyms: GW572016; GW2016)

231277-92-2
Price and Availability of CAS No. : 231277-92-2
Size Price Stock
50mg $66 In-stock
100mg $86 In-stock
500mg $172 In-stock
1g $198 In-stock
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Cat. No. : HY-50898
M.Wt: 581.06
Formula: C29H26ClFN4O4S
Purity: >98 %
Solubility: DMSO : 125 mg/mL (ultrasonic;warming;heat to 60°C)
Introduction of 231277-92-2 :

Lapatinib (GW572016) is a potent, orally active inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively[1]. IC50 & Target:IC50: 10.2 nM (EGFR), 9.8 nM (ErbB2)[1] In Vitro: Lapatinib (GW2016; 0.03-10 μM; 6 hours; BT474 and HN5 cells) treatment inhibits receptor autophosphorylation of EGFR and ErbB-2 in a dose-responsive manner. Phosphorylation of serine 473 of AKT was inhibited by GW2016 in a dose-dependent manner[1].
Lapatinib (GW2016; 72 hours; HN5, A-43, BT474, N87, and CaLu-3 cells) treatment has a selective inhibition of the proliferation of human tumor cell lines[1].
Lapatinib (GW2016; 1-10 μM; 72 hours; HN5 cells) treatment results in induces G1 arrest[1]. In Vivo: Lapatinib (GW2016; 30-100 mg/kg; oral administration; twice daily; for 21 days; CD-1 nude female mice) treatment inhibits tumor xenograft growth of the HN5 cells in a dose-responsive manner at 30 and 100 mg/kg, with complete inhibition of tumor growth at the higher dose[1].

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