Lapatinib ditosylate monohydrate|388082-78-8|(二甲苯磺酸拉帕替尼一水合物; GW572016 ditosylate monohydrate; GW2016 ditosylate monohydrate)-陌孚医药/Medlife

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Lapatinib ditosylate monohydrate (Synonyms: 二甲苯磺酸拉帕替尼一水合物; GW572016 ditosylate monohydrate; GW2016 ditosylate monohydrate)

目录号: PL05096 纯度: ≥99%

CAS No. :388082-78-8

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中文名称	Lapatinib ditosylate monohydrate
中文别名	二甲苯磺酸拉帕替尼;N-(3-氯-4-((3-氟苯基)甲氧基)苯基)-6-(5-(((2-(甲磺酰基)乙基)氨基)甲基)-2-呋喃基)-4-喹唑啉胺二对甲苯磺酸盐;二对甲苯磺酸拉帕替尼;拉帕替尼二甲苯磺酰酸盐;5-羟基色醇;二***磺酸拉帕替尼;二苯甲磺酸拉帕替尼;二对甲苯磺酸拉帕替尼一水合物;二甲苯磺酸拉帕替尼仅供科研使用;二甲苯磺酸拉帕替尼（一水）;二甲苯磺酸拉帕替尼Lapatinib;拉帕替尼;拉帕替尼-D4二甲苯磺酸酯;拉帕替尼二对甲苯磺酸（无水）;拉帕替尼二对甲苯磺酸(一水);拉帕替尼二对甲苯磺酸盐;拉帕替尼二甲磺酸盐;对甲苯磺酸拉帕替尼;二甲苯磺酸拉帕替尼拉帕替尼二对甲苯磺酸盐水合物
英文名称	Lapatinib ditosylate monohydrate
英文别名	Lapatinib Ditosylate;benzenesulfonic acid: N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6 -[5-[(2-methylsulfonylethylamino)methyl]-2-furyl]quinazolin-4-amine h ydrate;N-(3-Chloro-4-((3-fluorophenyl)methoxy)phenyl)-6-(5-(((2-(methylsulfonyl)ethyl)amino)methyl)-2-furanyl)-4-quinazolinamine bis(4-methylbenzenesulfonate);Tykerb N-{3-Chloro-4-[(3-fluorophenyl)-methoxy]-phenyl}-6-{5-{(2-methylsulfonylethy amino)-methyl]-2-furyl}-quinazolin-4-amine-benzenesulfonic acid;Lapatinib ditosylate hydrate;bis(N-(3-chloro-4-(3-fluorobenzyloxy)phenyl)-6-(5-((2-(methylsulfonyl)ethylamino)methyl)furan-...;Lapatinib; Lapatinib Ditosilate;Lapatinib ditosylate Monohydrate;4-Quinazolinamine,N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[[[2-(methylsulfonyl)ethyl]amino]methyl]-2-furanyl]-,bis(4-methylbenzenesulfonate), monohydrate (9CI);N-(3-Chloro-4-((3-fluorophenyl)methoxy)phenyl)-6-(5-(((2-(methylsulfonyl)ethyl)amino)methyl)-2-furanyl)-4-quinazolinamine bis(4-methylbenzenesulfonate) monohydrate;Tykerb;GW572016;GW 572016;Lapatinib base;Lapatinib [INN];Tyverb;Lapatinib (INN);Lapatinib free base;GSK 572016;GSK572016;FMM;N-{3-CHLORO-4-[(3-FLUOROBENZYL)OXY]PHENYL}-6-[5-({[2-(METHYLSULFONYL)ETHYL]AMINO}METHYL)-2-FURYL]-4-QUINAZOLINAMINE;0VUA21238F;NSC745750;N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[(2-methylsulfonylethylamino)methyl]furan-2-yl]quinazolin-4-amine;C29H26ClF
Cas No.	388082-78-8
分子式	C₂₉H₂₆ClFN₄O₄S
分子量	581.06
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情

Lapatinib ditosylate monohydrate (GW572016 ditosylate monohydrate) 是一种 ErbB-2 和 EGFR 酪氨酸激酶结构域的有效抑制剂，对纯化的 EGFR 和 ErbB-2 的 IC₅₀ 值分别为 10.2 和 9.8 nM。

生物活性

Lapatinib ditosylate monohydrate (GW572016 ditosylate monohydrate) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC 50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively.

性状

Solid

IC50 & Target[1][2]

EGFR 10.8 nM (IC50) ErbB2 9.2 nM (IC5

体外研究(In Vitro)

Lapatinib (GW2016; 0.03-10 μM; 6 hours; BT474 and HN5 cells) treatment inhibits receptor autophosphorylation of EGFR and ErbB-2 in a dose-responsive manner. Phosphorylation of serine 473 of AKT was inhibited by GW2016 in a dose-dependent manner.
Lapatinib (GW2016; 72 hours; HN5, A-43, BT474, N87, and CaLu-3 cells) treatment has a selective inhibition of the proliferation of human tumor cell lines.
Lapatinib (GW2016; 1-10 μM; 72 hours; HN5 cells) treatment results in induces G1 arrest. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Lapatinib (GW2016; 30-100 mg/kg; oral administration; twice daily; for 21 days; CD-1 nude female mice) treatment inhibits tumor xenograft growth of the HN5 cells in a dose-responsive manner at 30 and 100 mg/kg, with complete inhibition of tumor growth at the higher dose. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

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.

溶解度数据	In Vitro: DMSO : 50 mg/mL (53.00 mM; ultrasonic and warming and heat to 60°C)配制储备液

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