• All
  • Primary Antibodies
  • Conjugated Antibodies for IF
  • Conjugated Antibodies for FC
  • Secondary Antibodies
  • Antibody Labeling KitsNew
  • ELISA Kits
  • IHC Kits
  • Magnetic Cell Separation Kits
  • Cytokines & Growth Factors
  • Neutralizing/activating Antibodies
  • Nanobody-based Reagents
  • Accessory Products and Kits
  • Fusion Proteins
×
×
Host
0
Species Reactivity
0
Species Reactivity
0
Conjugate
0
Conjugate
0
Compatible Species
0
Conjugate
0

Lapatinib Ditosylate

Lapatinib Ditosylate (Tykerb ditosylate) 是一种有效的 EGFR 和 ErbB2 抑制剂，对 EGFR 和 ErbB2的 IC50值分别为 10.8 和 9.2 nM。它用于治疗晚期乳腺癌和其他实体瘤。

CAS号

388082-77-7

分子式

C29H26ClFN4O4S·2C7H8O3S

主要靶点

Autophagy|EGFR|Ferroptosis

仅限科研使用

Cat No : CM04454

Print datasheet

Synonyms

Tykerb ditosylate|二甲苯磺酸拉帕替尼|Lapatinib (GW-572016) Ditosylate|GW-572016 ditosylate|二对甲苯磺酸拉帕替尼

验证数据展示

  • CAS No.: 388082-77-7

    Lapatinib Ditosylate
    CAS#: 388082-77-7

产品信息

Lapatinib Ditosylate (Tykerb ditosylate) is an effective EGFR and ErbB2 inhibitor (IC50: 10.8/9.2 nM for EGFR/ErbB2).

CAS号 388082-77-7
分子式 C29H26ClFN4O4S·2C7H8O3S
主要靶点 Autophagy|EGFR|Ferroptosis
主要通路 蛋白酪氨酸激酶|血管生成|JAK/STAT信号通路|凋亡|自噬
分子量 925.46
纯度 98.42%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 Tykerb ditosylate|二甲苯磺酸拉帕替尼|Lapatinib (GW-572016) Ditosylate|GW-572016 ditosylate|二对甲苯磺酸拉帕替尼

靶点活性

ErbB2:9.2 nM (cell free)|EGFR:10.8 nM (cell free)

体内活性

Lapatinib ( 30 and 100 mg/kg, p.o., b.i.d) dose-responsive inhibited the growth of BT474 and HN5 human tumor xenografts. Complete inhibition of tumor growth is seen at the 100 mg/kg dose. At this dose, there is <10% weight loss in treated animals over the course of the 21-day treatment. Lapatinib treatment inhibits tumor xenograft growth of the HN5 and BT474 cells in a dose-responsive manner at 30 and 100 mg/kg orally, twice daily, with complete inhibition of tumor growth at the higher dose [1]. Lapatinib (100 mg/kg/day, p.o.) induces severe oxidative damage in the cardiac tissue of rat [4].

体外活性

Lapatinib (1 μM) induces apoptosis in NCI-N87 and OD19 cells [2]. Lapatinib inhibits the growth of EGFR-overexpressing A431 skin cancer (IC50: 0.14 μM) and ErbB2-overexpressing SK-BR-3 breast cancer cells (IC50: 0.124 μM). It also inhibits the growth of ErbB2-amplified OD19 esophageal (IC50: 0.09 μM)and NCI-N87 gastric cancer cells (IC50: 0.01 μM) as well as several types of gastric cancer cells in which ErbB2 is not amplified (IC50s: 0.35-8.58 μM) [3] .

溶解度

Ethanol:<1 mg/mL,DMSO:93 mg/mL (100.5 mM),H2O:<1 mg/mL

细胞实验

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 days. Relative cell number is estimated using methylene blue staining. The absorbance at 620 nm is read in a Spectra microplate reader. Cell death and cell cycle analysis are assessed by propidium iodide staining and antibody detection of incorporated BrdUrd and staining with propidium iodide [1].

动物实验

CD-1 nude female mice are used for HN5 human tumor xenografts, which are initiated by injection of a cell suspension in PBS: Matrigel (1:1). C.B-17 SCID female mice are used for BT474 human tumor xenografts, which are initiated by implantation of tumor fragments (20-100 mg) from established tumors. Tumor cells and fragments are implanted by s.c. injection in the right flank. The s.c. tumors are measured with calipers, and mice are weighed twice weekly. Tumor weight is estimated from tumor volume using this formula: length×width2/2=tumor volume (mm3). Treatment begins when tumors are palpable, 3-5 mm in diameter. Lapatinib (30 and 100 mg/kg) is administered p.o. twice daily for 21 days in a vehicle of sulfo-butyl-ether-β-cyclodextrin 10% aqueous solution (CD10) [1].

参考文献

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
2.Chefrour M et al. Positive interaction between lapatinib and capecitabine in human breast cancer models: study of molecular determinants. Fundam Clin Pharmacol. 2012 Aug;26(4):530-7.
3.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.
4.Eryilmaz U, et al. S100A1 as a Potential Diagnostic Biomarker for Assessing Cardiotoxicity and Implications for the Chemotherapy of Certain Cancers. PLoS One. 2015 Dec 18;10(12):e0145418.

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
=
×
×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
×
=
×
C1   V1   C2   V2