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Lapatinib Ditosylate 二甲苯磺酸拉帕替尼

目录号 M1802 所有产品仅供科研使用,严禁用于人或动物的治疗等任何其他用途,不为任何个人提供产品和服务  


Lapatinib (GW-572016) Ditosylate是一种有效的EGFR和ErbB2抑制剂,IC50分别为10.8和9.2 nM。

Lapatinib Ditosylate结构式

别名:Tykerb

规格 价格 库存状态
Free Sample (0.5-1 mg)  ¥ 0 中国库存现货
10mg ¥ 350 中国库存现货
50mg ¥ 550 中国库存现货
100mg ¥ 700 中国库存现货
200mg ¥ 1000 中国库存现货
500mg ¥ 1500 中国库存现货
其他规格数量报价?

质量标准及产品资料
生物活性

Lapatinib (GW-572016) Ditosylate是一种有效的EGFR和ErbB2抑制剂,IC50分别为10.8和9.2 nM。Lapatinib有效抑制过量表达EGFR的HN5和A-431细胞生长,也抑制过量表达ErbB2的BT474和N87细胞生长,且显著诱导HN5细胞周期停在G1期,也诱导 BT474 细胞凋亡,与抑制AKT磷酸化相关。Lapatinib 作用于含EGFR的L858R和T790M突变的抗Gefitinib的H1975细胞显著抑制Stat3磷酸化,导致细胞生长受抑制,IC50为1-2 μM。Lapatinib 按~100 mg/kg剂量口服处理,每天两次,显著抑制BT474和HN5移植瘤生长,这种作用存在剂量依赖性。与在体外活性一致,Lapatinib按100-150 mg/kg剂量处理携带H1975肿瘤的小鼠,延迟肿瘤生长。

使用AbMole产品发表的文献
产品使用成果展示
数据来源 Proc Natl Acad Sci U S A (2018) . Figure 6. Lapatinib Ditosylate (AbMole BioScience)
方法 i.v.
细胞系/动物模型 NSG mice
浓度 100 mg/kg
处理时间 5 d
实验结果 Again, the single agents displayed modest activity, inhibiting tumor growth, whereas the combination shrank most of the tumors, similar to the BT-474 xenograft model.
数据来源 Proc Natl Acad Sci U S A (2018) . Figure 5. Lapatinib Ditosylate (AbMole BioScience)
方法 Western blotting
细胞系/动物模型 HCC-1419 and MDA-MB-453 cells
浓度 1 μM
处理时间 6, 12, and 24 h
实验结果 To verify that both MCL-1:BIM and MCL-1:BAK complexes were disrupted by S63845, we immunoprecipitated MCL-1 complexes in lysates of the HER2-amplified breast cancer cells, HCC- 1419 and MDA-MB-453, following treatment with lapatinib, S63845 (at two concentrations of 300 nM and 1 μM), or their combination.
数据来源 Proc Natl Acad Sci U S A (2018) . Figure 4. Lapatinib Ditosylate (AbMole BioScience)
方法 Western blotting
细胞系/动物模型 MDA-MB-361 and BT-474 cells
浓度 1 μM
处理时间 24 h
实验结果 Importantly, since HER2 inhibitors like lapatinib block ERK signaling in HER2-amplified breast cancers, it is likely that miR-4728 only has an antagonistic effect in the presence of HER2 inhibitors, while miR-4728 likely promotes tumorigenesis in the absence of HER2 inhibition.
数据来源 Int J Pharm Pharm Sci (2016). Figure 3.Lapatinib (Abmole)
方法 PH test
细胞系/动物模型
浓度
处理时间 1~21 days
实验结果 No significant changes in the vaginal pH were observed between control and treated animals throughout the three phases of the estrous cycle. Even though, on the 12th d, prolonged diestrus phase in treated group animals was evidenced with the vaginal pH as compared with the control mice [fig. 3].
实验参考
体外实验*
细胞系 HFF; BT474, MCF-7, N87, and CaLu-3; HN5, A-431, T47D, HB4a, and HB4a c5.2 cell lines
方法 In Vitro Growth Inhibition Assays For assessment of cell-based potency, cells were plated in 96-well Falcon plates (Becton Dickinson) in the growth media described above. Plating densities that resulted in logarithmic growth of vehicle-treated cells for the duration of the assay were used: HFF, 15,000 cells/cm2; BT474, MCF-7, N87, and CaLu-3, 30,000 cells/cm2; and HN5, A-431, T47D, HB4a, and HB4a c5.2, 10,000 cells/cm2. After 24 h, cells were exposed to compounds at the concentrations indicated in Fig. 2. HFF, BT474, HN5, and N87 cells were treated in low-glucose DMEM containing 5% FBS, 50 μg/ml gentamicin, and 0.3% v/v DMSO. MCF-7 cells were treated in 50% high-glucose DMEM, 50% low-glucose DMEM containing 5% FBS, 50 μg/ml gentamicin, and 0.3% v/v DMSO. T47D, A-431, and CaLu-3 cells were treated in 50% RPMI, 50% low-glucose DMEM containing 5% FBS, 50 μg/ml gentamicin, and 0.3% v/v DMSO. HB4a and HB4a c5.2 cells were treated in 50% DMEM, 50% RPMI 1640 supplemented with 5% FBS, 2.5 μg/ml hydrocortisone, 2.5 μg/ml insulin, 25 μg/ml hygromycin B, 50 μg/ml gentamicin, and 0.3% v/v DMSO. After 3 days, relative cell number was estimated using methylene blue staining. The media were removed, and 100 μl of 0.5% w/v methylene blue dissolved in 50% ethanol and 50% water were added to each well. Plates were washed by immersion in deionized water and allowed to air dry. 1% w/v n-lauroylsarcosine (100 μl) dissolved in PBS was added to each well, and plates were incubated for 30 min at room temperature. The absorbance at 620 nm was read in a Spectra (Tecan) microplate reader. Data were analyzed using curve-fitting macros written for Microsoft Excel. Concentrations with IC50 were interpolated using the method of Levenberg and Marquardt and this equation: y = Vmax × [1 − (xn/(Kn + xn))], where “K” is equal to IC50.
浓度 0~100 μM
处理时间 3 days

*上述方法来自公开文献,仅供相同目的实验参考。如实验目的、材料、方法不同,请参考其他文献。

体内实验*
动物模型 CD-1 nude female mice were used for HN5 human tumor xenografts, C.B-17 SCID female mice were used for BT474 human tumor xenografts
配制 sulfo-butyl-ether-β-cyclodextrin 10% aqueous solution (CD10)
剂量 30 or 100 mg/kg twice daily for 21 days
给药处理 p.o.

*上述方法来自公开文献,仅供相同目的实验参考。如实验目的、材料、方法不同,请参考其他文献。

化学性质
分子量 925.46
分子式 C29H26ClFN4O4S.2C7H8O3S
CAS号 388082-78-8
溶解性(25°C) DMSO 90 mg/mL
储存条件 -20°C, sealed, protect from light
运输方式 冰袋运输,根据产品的不同,可能会有相应调整。
储备液配制

*下述溶液配置方法仅为基于分子量计算出的理论值。不同产品在配置溶液前,需考虑其在不同溶剂中的溶解度限制。

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.0805 mL 5.4027 mL 10.8054 mL
5 mM 0.2161 mL 1.0805 mL 2.1611 mL
10 mM 0.1081 mL 0.5403 mL 1.0805 mL
不同实验动物依据体表面积的等效剂量转换表(参考来源于公开文献
小鼠 大鼠 豚鼠 仓鼠
重量 (kg) 0.02 0.15 1.8 0.4 0.08 10
体表面积 (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km 系数 3 6 12 8 5 20
动物 A (mg/kg) = 动物 B (mg/kg) ×  动物 B的Km系数
动物 A的Km系数

例如,依据体表面积折算法,将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量,需要将20 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到化合物用于大鼠的等效剂量为10 mg/kg。

参考文献

[1] Simonelli M, et al. Eur J Cancer. Phase I pharmacokinetic and pharmacodynamic study of lapatinib in combination with sorafenib in patients with advanced refractory solid tumors.

[2] Bachelot T, et al. Lancet Oncol. Lapatinib plus capecitabine in patients with previously untreated brain metastases from HER2-positive metastatic breast cancer (LANDSCAPE): a single-group phase 2 study.

[3] Jegg AM, et al. Breast Cancer Res Treat. PI3K independent activation of mTORC1 as a target in lapatinib-resistant ERBB2+ breast cancer cells.

[4] de Jonge MJ, et al. Invest New Drugs. Phase I and pharmacokinetic study of pazopanib and lapatinib combination therapy in patients with advanced solid tumors.

[5] Rusnak DW, et al. Mol Cancer Ther. 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.

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