Home>>Signaling Pathways>> Ubiquitination/ Proteasome>> Autophagy>>Lapatinib Ditosylate

Lapatinib Ditosylate Sale

(Synonyms: 二甲苯磺酸拉帕替尼; GW572016 ditosylate monohydrate; GW2016 ditosylate monohydrate) 目录号 : GC16593

Lapatinib Ditosylate (GW572016 ditosylate monohydrate) 是有效的 ErbB-2 和 EGFR 酪氨酸激酶结构域抑制剂,对纯化的 EGFR 和 ErbB-2 的 IC50 值分别为 10.2 和 9.8 nM。

Lapatinib Ditosylate Chemical Structure

Cas No.:388082-78-8

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥756.00
现货
50mg
¥347.00
现货
100mg
¥525.00
现货

电话:400-920-5774 Email: sales@glpbio.cn

Customer Reviews

Based on customer reviews.

Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

View current batch:

产品描述

Lapatinib Ditosylate is a selective dual inhibitor of ErbB-2 and EGFR with IC50 value against ErbB-2 and EGFR of 9.2 and 10.8 nM in vitro, respectively. [1]
The EGFR and ErbB-2 all are the type I receptor tyrosine kinase that exists on the cell surface and have been recognised as potential targets for cancers. A conformational change happens by binding of its specific ligands in the receptor then activates the kinase domain. Whereas, erbB2 is generally thought that it has no known direct activating ligand, and it may become active by heterodimerization with other ligand-bound family members. EGFR dimerization stimulates protein-tyrosine kinase activity and elicits downstream signaling by several other proteins. These proteins initiate several signal transduction pathway. EGFR and ErbB-2 are well known to stimulate cell division through the Ras pathway, and resulting in cell growth through the PI3K pathway. [1]
Lapatinib is a selective inhibitor of the ErbB-2 and EGFR. Lapatinib was>300 fold selective for ErbB-2 and EGFR over other kinases, such as MEK, ERK. Lapatinib likely competed intracellular ATP with Erb-2 and EGFR,then inhibit the activation of them. Lapatinib inhibited the growth of human tumor cells in a cell-based proliferation assay. The IC50 values was < 0.16nM in the ErbB-2- and EGFR -overexpressing cell lines: HN5, A-431. In the cell lines expressing low level ErbB-2- and EGFR. The IC50 values were about 25-fold higher than in the overexpressing cell lines. Lapatinib resulted in G1 arrest at 10nM in HN5 cells. Lapatinib inhibited phos phorylated Er k1/2 100% at 5 nM in an erbB2 overexpressing cell line. Lapatinib inhibited EGF stimulated p-Erk1/ 2 at 1 nM and complet ely inh ibited p-AKT.[1, 2]
In human breast cancer xenografts, tumor volumes in mice at the dose of 75 mg/kg of lapatinib twice daily were significantly smaller than the vehicle control, at day 21.[3] Lapatinib completely inhibited the growth of HN5 and BT474 human tumor xenografts at the 100 mg/kg dose, twice daily.[1]
References:
1.Rusnak DW, Lackey K, Affleck K, Wood ER, Alligood KJ, Rhodes N, Keith BR, Murray DM, Knight WB, Mullin RJ 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, 1(2):85-94.
2.Xia W, Mullin RJ, Keith BR, Liu LH, Ma H, Rusnak DW, Owens G, Alligood KJ, Spector NL: Anti-tumor activity of GW572016: a dual tyrosine kinase inhibitor blocks EGF activation of EGFR/erbB2 and downstream Erk1/2 and AKT pathways. Oncogene 2002, 21(41):6255-6263.
3.Konecny GE, Pegram MD, Venkatesan N, Finn R, Yang G, Rahmeh M, Untch M, Rusnak DW, Spehar G, Mullin RJ et al: Activity of the dual kinase inhibitor lapatinib (GW572016) against HER-2-overexpressing and trastuzumab-treated breast cancer cells. Cancer Res 2006, 66(3):1630-1639.

Chemical Properties

Cas No. 388082-78-8 SDF
别名 二甲苯磺酸拉帕替尼; GW572016 ditosylate monohydrate; GW2016 ditosylate monohydrate
化学名 N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[(2-methylsulfonylethylamino)methyl]furan-2-yl]quinazolin-4-amine;4-methylbenzenesulfonic acid;hydrate
Canonical SMILES 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)C2=CC3=C(C=C2)N=CN=C3NC4=CC(=C(C=C4)OCC5=CC(=CC=C5)F)Cl
分子式 C29H26ClFN4O4S 2C7H8O3S 分子量 925.46
溶解度 ≥ 24.3 mg/mL in DMSO 储存条件 4°C, protect from light
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

制备储备液
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
  • 摩尔浓度计算器

  • 稀释计算器

  • 分子量计算器

质量
=
浓度
x
体积
x
分子量
 
 
 
*在配置溶液时,请务必参考产品标签上、MSDS / COA(可在Glpbio的产品页面获得)批次特异的分子量使用本工具。

计算

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % saline
计算重置

Research Update

1. Lapatinib ditosylate: expanding therapeutic options for receptor tyrosine-protein kinase erbB-2-positive breast cancer. Drugs Today (Barc). 2011 May;47(5):335-45. doi: 10.1358/dot.2011.47.5.1584110.
Abstract
Lapatinib ditosylate is a tyrosine kinase inhibitor targeting HER2 receptor that exhibits activity in transtuzumab-resistant advanced tumors, recurrent local advanced inflammatory breast cancer and brain metastases. The combination of lapatinib ditosylate , trastuzumab and paclitaxel significantly improved pathological complete response in Neo-ALTTO trails.
2. RON confers lapatinib resistance in HER2-positive breast cancer cells. Cancer Lett. 2013 Oct 28;340(1):43-50. doi: 10.1016/j.canlet.2013.06.022. Epub 2013 Jun 27.
Abstract
RON plays an important role in lapatinib-resistance mediation, where small-molecular RON inhibitors and siRNA could restore lapatinib sensitivity in SK-BR-3-LR cells.
4. Lapatinib as a component of neoadjuvant therapy for HER2-positive operable breast cancer (NSABP protocol B-41): an open-label, randomised phase 3 trial. Lancet Oncol. 2013 Nov;14(12):1183-92. doi: 10.1016/S1470-2045(13)70411-X. Epub 2013 Oct 4.
Abstract
Lapatinib plus paclitaxel and lapatinib plus trastuzumab were evaluated respectively for their effects on tumor response in HER2+ breast cancer patients with prior treatment of doxorubicin plus cyclophosphamide.
5. Addition of amino acid moieties to lapatinib increases the anti-cancer effect via amino acid transporters. Biopharm Drug Dispos. 2014 Jan;35(1):60-9. doi: 10.1002/bdd.1872. Epub 2013 Nov 19.
Abstract
The enhanced anticancer activity of val-lapatinib and tyr-lapatinib in various cancer cells, including human breast cancer cells and lung cancer cells, is possible caused by increased uptake of them into cancer cells via amino acid transporter, since they were found to inhibited glutamine transport in cancer cells.