産品名稱

産品編号

CAS NO.

規格

價格（元）

Lapatinib拉帕替尼

MZ20306-50MG

231277-92-2

50mg

320

Lapatinib拉帕替尼

MZ20306-100MG

231277-92-2

100mg

540

Lapatinib拉帕替尼

MZ20306-1G

231277-92-2

1g

1850

         質量     

溶劑體積

濃度

1mg             

5mg             

10mg            

100mg          

1mM

1.7210 mL

8.6050 mL

17.2099 mL

172.0993 mL

5mM

0.3442 mL

1.7210 mL

3.4420 mL

34.4199 mL

10mM

0.1721 mL

0.8605 mL

1.7210 mL

17.2099 mL

50mM

0.0344 mL

0.1721 mL

0.3442 mL

3.4420 mL

文獻1，Rusnak DW et al. The effects of the novel, reversible epidermal growth factor receptor/ErbB-2 tyrosine kinase inhibitor, GW2016, on the growth of human normal and tumor-derived cell lines in vitro and in vivo. Mol Cancer Ther. 2001 Dec;1(2):85-94. PMID: 12467226

體外研究：

細胞類型（Cell type）：EGFR-overexpressing cell lines HN5, ErbB-2-overexpressing cell lines BT474, Normal human foreskin fibroblasts (HFF)

藥物(wù)配制（Preparation）：GW2016 was dissolved in DMSO

實驗方法（Assay）：Cells are plated in 96-well plates in the media at the following densities: HFF and HN5, 1000 cells/well and BT474, 5000 cells/well.After 24 h, the cells are exposed to vehicle (0.3% DMSO) or Lapatinib (1 nM, 10 nM, 100 nM, 1μM, 10μM, and 100μM).Lapatinib is removed from the cells after 72 h and is replaced by either DMEM containing 10% FBS and 50 μg/mL Gentamicin (HFF and HN5) or RPMI containing 10% FBS and 50 μg/mL Gentamicin (BT474). Methylene blue staining is performed at the time points over a total period of 16 day.

體内研究：

動物(wù)模型（Animal Model）：BT474 human tumor xenografts (established in C.B-17 SCID female mice), HN5 human tumor xenografts (established in CD-1 nude female mice)

藥物(wù)配制（Preparation）：GW2016 was dissolved in a vehicle of sulfo-butyl-ether-β-cyclodextrin 10% aqueous solution.

給藥劑量（Dosages）：Experimental compounds (30mg/kg and 100mg/kg) were administered p.o. twice daily for 21 days in a vehicle of sulfo-butyl-ether-β-cyclodextrin 10% aqueous solution.

實驗結果（Results）：GW2016 was potent at inhibiting the growth of BT474 and HN5 human tumor xenografts. A dose-responsive inhibition of both models occurred on treatment of tumor-bearing mice with 30 and 100 mg/kg GW2016 orally, twice daily. Complete inhibition of tumor growth was seen at the 100 mg/kg dose.

文獻2，Wainberg ZA et al. Lapatinib, a dual EGFR and HER2 kinase inhibitor, selectively inhibits HER2-amplified human gastric cancer cells and is synergistic with trastuzumab in vitro and in vivo. Clin Cancer Res. 2010 Mar 1;16(5):1509-19. PMID: 20179222

體外研究：

細胞類型（Cell type）：14 established human gastric and esophageal cancer cell lines that express variable levels of EGFR and HER2: AGS, NCI-N87, KATO III, SNU-1, SNU-5, and SNU-16; NUGC4, NUGC3, FU97, IM95, IM95m, MKN74, and MKN1; OE19;

藥物(wù)配制（Preparation）：Lapatinib was prepared as a 10 mmol/L stock solution in DMSO.

實驗方法（Assay）：Cells were plated into 24-well plates at a density of 2 × 104to 6 × 104and grown in cell line– specific medium in decreasing concentrations of both lapatinib (ranging between 10 and 0.3125 μM) and erlotinib (ranging between 10 and 0.3125 μM). The same cell lines were treated with trastuzumab at a fixed dose of 10 μg/mL. Cells were harvested by trypsinization on day 6 and counted using a particle counter.

體内研究：

動物(wù)模型（Animal Model）：N87-bearing xenografts

藥物(wù)配制（Preparation）：Lapatinib was dissolved in 0.5% hydroxypropyl methylcellulose (HPMC) with 0.1% Tween 80.

注射劑量（Dosages）：N87 cells (5×106cells with 50% Matrigel) were injected s.c. into nude mice and mice were randomized into one of four groups (n = 11/group).Treatment started at day 4 after injection with either lapatinib (100 mg/kg daily for 3 wkby oral gavage in 0.5% hydroxypropyl methylcellulose and 0.1% Tween 80),trastuzumab (10 mg/kgin sterile PBS,i.p. twice weekly) or sterile PBS (i.p. twice weekly) or the combination of lapatinib and trastuzumab at the doses above. Tumors were measured biweekly. After 23 d of treatment, the animals were euthanized.

實驗結果（Results）：Both single-agent lapatinib and trastuzumab caused tumor regression in N87 xenografts. In addition, the combination showed near complete tumor resolution by day 23.

貨号

名稱

規格              

MZ20306-50MG         

Lapatinib 拉帕替尼

50mg

MZ20307-50MG

Lapatinib Ditosylate 二甲苯磺酸拉帕替尼

50mg

MZ20304-10MG

Afatinib (BIBW2992)阿 法替尼

10mg

MZ20305-10MG

Afatinib Dimaleate 阿法替尼雙馬來酸鹽         

10mg

MZ20308-1G

Erlotinib 埃羅替尼

1g