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Merck
CN

SML2259

拉帕替尼

≥98% (HPLC), EGFR/ErbB1 and HER2/ErbB2 inhibitor, powder

别名:

拉帕替尼, GD 2016, GSK 572016, GW-572016, GW572016, N-（3-氯-4-（（3-氟苯基）甲氧基）苯基）-6-（5-（（2-甲基磺酰基乙基氨基）甲基）-2-呋喃基）喹唑啉-4-胺, N-（3-氯-4-（（3-氟苯基）甲氧基）苯基）-6-（5-（（（（2-（甲基磺酰基）乙基）氨基）甲基）-2-呋喃基）-4-喹唑啉胺

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关于此项目

经验公式（希尔记法）:
C29H26ClFN4O4S
化学文摘社编号:
231277-92-2
分子量:
581.06
NACRES:
NA.77
UNSPSC Code:
12352200
MDL number:
MFCD09264194

主要文件

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产品名称

拉帕替尼, ≥98% (HPLC)

InChI

1S/C29H26ClFN4O4S/c1-40(36,37)12-11-32-16-23-7-10-27(39-23)20-5-8-26-24(14-20)29(34-18-33-26)35-22-6-9-28(25(30)15-22)38-17-19-3-2-4-21(31)13-19/h2-10,13-15,18,32H,11-12,16-17H2,1H3,(H,33,34,35)

SMILES string

CS(=O)(CCNCC1=CC=C(C2=CC=C3N=CN=C(C3=C2)NC4=CC=C(C(Cl)=C4)OCC5=CC=CC(F)=C5)O1)=O

InChI key

BCFGMOOMADDAQU-UHFFFAOYSA-N

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

Gene Information

human ... EGFR(1956), ERBB2(2064)

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相关类别

Biochem/physiol Actions

拉帕替尼(lapatinb)是针对表皮生长因子受体(EGFR/ErbB1)和人表皮生长因子受体2(HER2/ErbB2)的双酪氨酸激酶抑制剂。它与三磷酸腺苷(ATP)竞争酪氨酸激酶结构域上的结合位点。已有研究表明拉帕替尼参与乳腺、肺、外阴、胃和头颈癌等多种人癌细胞中的体外生长抑制和凋亡诱导。

pictograms

Exclamation mark
GHS07

signalword

Warning

Hazard Classifications

Aquatic Chronic 4 - Eye Irrit. 2 - Lact.

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

历史批次信息供参考:

分析证书(COA)

Lot/Batch Number
0000468779
0000144063
0000144063
0000468779
0000162120

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Lapatinib in breast cancer
Bilancia D, et al.
Annals of Oncology, 18, vi26-vi30 (2007)
Dongwei Zhang et al.
Molecular cancer therapeutics, 7(7), 1846-1850 (2008-07-23)
Epidermal growth factor receptor (EGFR/ErbB1) and HER2 (ErbB2/neu), members of the ErbB receptor tyrosine kinase family, are frequently overexpressed in breast cancer and are known to drive tumor growth and progression, making them promising targets for cancer therapy. Lapatinib is
Sharad Verma et al.
PloS one, 13(2), e0190942-e0190942 (2018-02-02)
HER-2 belongs to the human epidermal growth factor receptor (HER) family. Via different signal transduction pathways, HER-2 regulates normal cell proliferation, survival, and differentiation. Recently, it was reported that MCF10A, BT474, and MDA-MB-231 cells bearing the HER2 K753E mutation were
Egle Avizienyte et al.
The Biochemical journal, 415(2), 197-206 (2008-07-01)
Recent clinical data indicates that the emergence of mutant drug-resistant kinase alleles may be particularly relevant for targeted kinase inhibitors. In order to explore how different classes of targeted therapies impact upon resistance mutations, we performed EGFR (epidermal-growth-factor receptor) resistance
Richard M Tehan et al.
Journal of natural products, 85(5), 1363-1373 (2022-05-03)
The genome of entomopathogenic fungus Tolypocladium inflatum Gams encodes 43 putative biosynthetic gene clusters for specialized metabolites, although genotype-phenotype linkages have been reported only for the cyclosporins and fumonisins. T. inflatum was cultured in defined minimal media, supplemented with or
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