Lapatinib ditosylate monohydrate

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

二甲苯磺酸拉帕替尼是葛兰素史克（GSK）开发的一种抗 Y 化合物，用于治疗乳腺癌和肺癌等实体瘤。

Lapatinib ditosylate is an anti-Y drug developed by GlaxoSmithKline (GSK) as a treatment for solid tumours such as breast and lung Y.(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 cells Concentration:Incubation Time:72 hoursResult: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 daysResult:Inhibited tumor xenograft growth of the HN5 cells in a dose-responsive manner.

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Angiogenesis

EGFR

EGFR| HER2/ErbB2

Cancer

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388082-78-8

943.47

C29H26ClFN4O4S·2(C7H8O3S)·H2O

>98% (HPLC)

Soluble in DMSO

O.CC1=CC=C(C=C1)S(O)(=O)=O.CC1=CC=C(C=C1)S(O)(=O)=O.CC1=CC=C(C=C1)S(O)(=O)=O.CC1=CC=C(C=C1)S(O)(=O)=O.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.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

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(-20℃)

With Ice Pack

≥ 2 years