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Lapatinib (ditosylate monohydrate)


CAS No. : 388082-78-8

(Synonyms: GW572016 (ditosylate monohydrate); GW2016 (ditosylate monohydrate))

388082-78-8
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Cat. No. : HY-50898B
M.Wt: 943.48
Formula: C43H44ClFN4O11S3
Purity: >98 %
Solubility: DMSO : 50 mg/mL (ultrasonic;warming;heat to 60°C)
Introduction of 388082-78-8 :

Lapatinib ditosylate monohydrate (GW572016 ditosylate monohydrate) 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]. 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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