Lapatinib

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种 EGFR 和 ErbB2 的可逆、选择性双酪氨酸激酶抑制剂，在无细胞测定中 IC50 分别为 10.8 和 9.2 nM。

A reversible, selective dual tyrosine kinase inhibitor of both EGFR and ErbB2 with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively; displays no significant activity against other kinases, including ErbB4, c-Src, and c-Raf1; reduces tyrosine phosphorylation of EGFR and erbB2, and inhibits activation of Erk1/2 and AKT both in vitro and in vivo; inhibits tumor xenograft growth of the HN5 and BT474 cells in a dose-responsive manner at 30 and 100 mg/kg; orally active.Breast Cancer Approved(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.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.Lapatinib (GW2016; 1-10 μM; 72 hours; HN5 cells) treatment results in induces G1 arrest.(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.

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.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.Lapatinib (GW2016; 1-10 μM; 72 hours; HN5 cells) treatment results in induces G1 arrest. Western Blot Analysis Cell Line:BT474 and HN5 cells Concentration:0.03 μM, 0.1 μM, 0.3 μM, 1 μM, 3 μM, or 10 μM Incubation Time:6 hours Result:Inhibited receptor autophosphorylation of EGFR and ErbB-2 in a dose-responsive manner. Phosphorylation of serine 473 of AKT was also inhibited in a dose-dependent manner.Cell Proliferation Assay Cell Line:HN5, A-43, BT474, N87, and CaLu-3 cellsConcentration:Incubation Time:72 hours Result:Inhibited the growth of tumor cells overexpressing EGFR or ErbB-2.Cell Cycle Analysis Cell Line:HN5 cells Concentration:1 μM, or 10 μM Incubation Time:72 hours Result:Resulted in induction of G1 arrest.

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. Animal Model:CD-1 nude female mice (4-6 weeks old) with HN5 cells Dosage:30 mg/kg, 100 mg/kg Administration:Oral administration; twice daily; for 21 days Result:Inhibited tumor xenograft growth of the HN5 cells in a dose-responsive manner.

GW572016 | GW-572016 | GW 572016

Angiogenesis

EGFR

C-Raf-1|c-Src|EGFR|HER2/ErbB2

Cancer

Breast Cancer

231277-92-2

581.0576

C29H26ClFN4O4S

>98% (HPLC)

DMSO: ≥ 39 mg/mL

CS(=O)(=O)CCNCC1=CC=C(O1)C1=CC2=C(C=C1)N=CN=C2NC1=CC(Cl)=C(OCC2=CC(F)=CC=C2)C=C1

4-Quinazolinamine, N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[[[2-(methylsulfonyl)ethyl]amino]methyl]-2-furanyl]-

(-20℃)

With Ice Pack

≥ 2 years