Lapatinib ditosylate monohydrate | 二甲苯磺酸拉帕替尼一水合物 | GW2016 ditosylate monohydrate | ErbB-2/EGFR Inhibitor

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二甲苯磺酸拉帕替尼水合物 /Lapatinib ditosylate monohydrate {[allProObj[0].p_purity_real_show]}

货号：A447246 同义名： 二甲苯磺酸拉帕替尼一水合物 / GW2016 ditosylate monohydrate;GW572016 ditosylate monohydrate

Lapatinib ditosylate monohydrate (GW572016 ditosylate monohydrate)是一种对ErbB-2和EGFR酪氨酸激酶域的强效抑制剂，对纯化的EGFR和ErbB-2的IC50值分别为10.2 nM和9.8 nM。

Lapatinib ditosylate monohydrate 化学结构
CAS号：388082-78-8

Lapatinib ditosylate monohydrate 3D分子结构
CAS号：388082-78-8

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Lapatinib ditosylate monohydrate 纯度/质量文件产品仅供科研

货号：A447246 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • ACS Appl. Nano Mater., 2025. Ambeed. [ A188026 ]; • Eur. J. Clin. Microbiol. Infect. Dis., 2025. Ambeed. [ A151161 ]; • JJC, 2025, 20(Special Issue)): 27-39. Ambeed. [ A713856 ]; • bioRxiv, 2025. Ambeed. [ A538667 , A714873 , A126729 , A126049 , A446054 ]; • Nature Communications, 2025, 16, 1871. Ambeed. [ A508148 ]; 更多 >

EGFR 亚型比较

产品名称	EGFR/ErbB1 ↓ ↑	ErbB3 ↓ ↑	ErbB4 ↓ ↑	HER2/ErbB2 ↓ ↑	mutant EGFR ↓ ↑	其他靶点	纯度
WZ-3146	++++ EGFR (E746_A750/T790M), IC50: 14 nM EGFR (E746_A750), IC50: 2 nM						99%+
Daphnetin	+ EGFR, IC50: 7.67 μM					PKA,PKC	95%
Lifirafenib	++ EGFR, IC50: 29 nM				+ EGFR(T790M/L858R), IC50: 495 nM		98%
PD168393	++++ EGFR, IC50: 0.70 nM						99%+
Nazartinib	++ mutant EGFR, Ki: 0.031 μM				++ mutant EGFR, Ki: 0.031 μM		98%
Norcantharidin	✔						98%
CL-387785	++++ EGFR, IC50: 370 pM						98%
WHI-P154	+++ EGFR, IC50: 4 nM					VEGFR,Src	98%
Tyrphostin A9	+ EGFR, IC50: 460 μM					PDGFR	98%
AG 555	+ EGFR, IC50: 0.7 μM						98%
AG 494	+ EGFR, IC50: 1.2 μM						99%+
AG-556	+ EGFR, IC50: 5 μM						98%
RG13022	+ EGFR, IC50: 4 μM						99%+
Tyrphostin RG 14620	✔						99%+
Vandetanib	+ EGFR, IC50: 500 nM						99%
CNX-2006	++ mutant EGFR, IC50: <20 nM				++ mutant EGFR, IC50: <20 nM		99%
AZD3759	++++ EGFR (WT), IC50: 0.3 nM EGFR (L858R), IC50: 0.2 nM						98%
Erlotinib	++++ EGFR, IC50: 2 nM						95%
Saracatinib	+++ EGFR (L861Q), IC50: 4 nM EGFR, IC50: 5 nM						99%+
AG1557	✔						99%
Rociletinib	++ EGFR (L858R/T790M), Ki: 21.5 nM EGFR (wt), Ki: 303.3 nM						98%
AG490	+ EGFR, IC50: 0.1 μM						98%
Cetuximab	++++ EGFR, Kd: 0.39 nM						99%
Osimertinib	++ L858R/T790M EGFR, IC50: 11.44 nM WT EGFR, IC50: 12.92 nM						98%
Osimertinib mesylate	✔						98% (Content MsOH 15.2-18.2%)
Chrysophanol	✔					mTOR	98%
PD153035	++++ EGFR, Ki: 5.2 pM						99%+
Olmutinib	✔					BTK	99%+
WZ4002	++++ EGFR (L858R/T790M), IC50: 8 nM EGFR (L858R), IC50: 2 nM						99%+
Icotinib	+++ EGFR, IC50: 5 nM						99%
Desmethyl Erlotinib HCl	++++ EGFR, IC50: 2 nM						99%
Cyasterone	✔						99%+
PP 3	+ EGFR tyrosine kinase, IC50: 2.7 μM						98%
WZ8040	✔						99%+
(-)-Epigallocatechin Gallate	✔						99%
AG 18	+ EGFR, IC50: 35 μM						99%+
O-Desmethyl gefitinib	++ EGFR, IC50: 36 nM						99%
Falnidamol	✔						99%+
AZ-5104	++++ EGFR (L861Q) , IC50: <1 nM EGFR (L858R), IC50: 6 nM		+++ ErbB4, IC50: 7 nM			BRK	99%+
Butein	✔						95%
Genistein	✔						98%
SU5214	+ EGFR, IC50: 36.7 μM						99%+
Naquotinib	✔						99%+
Gefitinib	++ EGFR, IC50: 15.5 nM				+ EGFR (858R/T790M), IC50: 823.3 nM		98%
Theliatinib	+++ WT EGFR, IC50: 3 nM				++ EGFR T790M/L858R, IC50: 22 nM		99%
Lazertinib	++++ L858R/T790M EGFR, IC50: 2 nM WT EGFR, IC50: 76 nM				++++ Del19/T790M, IC50: 1.7 nM		99%+
Gefitinib-based PROTAC 3	++ EGFR, DC50: 22.3 nM						99%+
MTX-211	✔					PI3K	98%
(E)-AG 99	✔						99%+
Licochalcone D	✔					Caspase,PARP	99%
Zipalertinib	+++ EGFR (L861Q), IC50: 4.1 nM EGFR WT, IC50: 8 nM		+++ HER4, IC50: 4 nM		++++ EGFR(d746-750), IC50: 1.4 nM EGFR L858R, IC50: 2 nM		97%
JND3229	+++ EGFR WT, IC50: 6.8 nM				++ EGFR L858R/T790M, IC50: 30.5 nM		99%+
Firmonertinib mesylate	✔						99%+
Tyrphostin AG30	✔						99%+
EGFR-IN-12	++ EGFR, IC50: 21 nM						99%+
Mobocertinib	✔						98%
(Rac)-JBJ-04-125-02	✔						99%
(S)-Sunvozertinib	✔						99%
BLU-945	✔						95%
Poziotinib	+++ HER1, IC50: 3.2 nM		++ HER4, IC50: 23.5 nM	+++ HER2, IC50: 5.3 nM			98%
TAK-285	++ EGFR/HER1, IC50: 23 nM		+ HER4, IC50: 260 nM	++ HER2, IC50: 17 nM			99%+
ARRY-380 analog				✔			99%
Canertinib	++++ EGFR, IC50: 1.5 nM			+++ ErbB2, IC50: 9.0 nM			99%+
Dacomitinib	+++ EGFR, IC50: 6.0 nM		+ ErbB4, IC50: 73.7 nM	+ ErbB2, IC50: 45.7 nM			98%
EGFR/ErbB-2/ErbB-4 inhibitor-2			+ ErbB4, IC50: 1.91 μM	+ ErbB2, IC50: 0.08 μM			99%+
(E/Z)-CP-724714				++ HER2/ErbB2, IC50: 10 nM			98+%
Lapatinib	++ EGFR, IC50: 10.8 nM		+ ErbB4, IC50: 367 nM	+++ ErbB2, IC50: 9.2 nM			98%
AEE788	++++ EGFR, IC50: 2 nM		+ HER4/ErbB4, IC50: 160 nM	+++ HER2/ErbB2, IC50: 6 nM		c-Fms	98+%
AV-412 free base	++++ EGFR, IC50: 0.75 nM			++ ErbB2, IC50: 19 nM	++++ EGFR^L858R/T790M, IC50: 0.51 nM EGFR^T790M, IC50: 0.79 nM		98+%
Neratinib	+ EGFR, IC50: 92 nM			+ HER2, IC50: 59 nM		Src	98%
BMS-599626	++ HER1, IC50: 20 nM		+ HER4, IC50: 190 nM	++ HER2, IC50: 30 nM			98%
Tucatinib				+++ ErbB2, IC50: 8 nM			98%
Allitinib	++++ EGFR, IC50: 0.5 nM		++++ ErbB4, IC50: 0.8 nM	+++ ErbB2, IC50: 3.0 nM			99%
Pelitinib	+ EGFR, IC50: 38.5 nM			+ ErbB2, IC50: 1.255 μM		Src,Raf	99%+
Sapitinib	+++ EGFR, IC50: 4 nM	+++ ErbB3, IC50: 4 nM		+++ ErbB2, IC50: 3 nM			99%+
CUDC-101	+++ EGFR, IC50: 2.4 nM			++ HER2, IC50: 15.7 nM		HDAC	99%+
Varlitinib	+++ ErbB1, IC50: 7 nM			++++ ErbB2, IC50: 2 nM			99%+
Afatinib dimaleate	++++ EGFR (L858R/T790M), IC50: 0.4 nM EGFR (wt), IC50: 0.5 nM			++ HER2, IC50: 14 nM			98%
Canertinib dihydrochloride	+++ EGFR, IC50: 7.4 nM			+++ ErbB2, IC50: 9 nM			99%
Allitinib tosylate	++++ EGFR (T790M/L858R), IC50: 12 nM EGFR, IC50: 0.5 nM		++++ ErbB4, IC50: 0.8 nM	+++ ErbB2, IC50: 3.0 nM			99%
Tyrphostin AG 528	+ EGFR, IC50: 4.9 μM			+ HER2, IC50: 2.1 μM			97%
Afatinib	++++ EGFR (L858R), IC50: 10 nM EGFR (wt), IC50: 0.5 nM		++++ ErbB4, IC50: 1 nM	++ HER2, IC50: 14 nM			99%
Pyrotinib dimaleate	++ EGFR, IC50: 0.013 μM			++ HER2, IC50: 0.038 μM			98%
Epertinib HCl	++++ EGFR, IC50: 1.48 nM		+++ HER4, IC50: 2.49 nM	+++ HER2, IC50: 7.15 nM			99%
Tuxobertinib	++++ EGFR, Kd: 0.2 nM			++++ HER2, Kd: 0.76 nM			99%
ALK-IN-1					++ EGFR(C797S/del19), IC50: 138.6 nM EGFR(del19), IC50: 36.8 nM	ALK	99%
Brigatinib					+ EGFR(del19), IC50: 39.9 nM EGFR(C797S/T790M/del19), IC50: 67.2 nM	ALK,FLT3	98%
Avitinib					++++ EGFR L858R/T790M, IC50: 0.18 nM	BTK	99%+
EAI045					✔		97%
Almonertinib					✔		99%
BI-4020					++++ EGFR^{del19 T790M C797S}, IC50: 0.2 nM		99%+
EGFR-IN-7					++++ EGFR^L858R/T790M, IC50: 0.19 nM EGFR^{d746-750/T790M/C797S}, IC50: 0.26 nM		99%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Lapatinib ditosylate monohydrate 生物活性

描述

Lapatinib ditosylate monohydrate (GW572016 ditosylate monohydrate) is a potent inhibitor targeting the tyrosine kinase domains of ErbB-2 and EGFR, demonstrating IC50 values of 9.8 nM and 10.2 nM against purified ErbB-2 and EGFR respectively^[1].

体内研究

In vivo, Lapatinib (administered orally at doses of 30 to 100 mg/kg twice daily for 21 days; in CD-1 nude female mice) effectively inhibits tumor xenograft growth derived from HN5 cells. This inhibition is dose-responsive, with complete cessation of tumor growth observed at the higher dosage of 100 mg/kg^[1].

体外研究

In cell-based assays, Lapatinib (GW2016; ranging from 0.03 to 10 µM over 6 hours; in BT474 and HN5 cells) effectively inhibits receptor autophosphorylation of both EGFR and ErbB-2 in a dose-responsive manner. Additionally, it also suppresses the phosphorylation of serine 473 on AKT in a dose-dependent fashion^[1].

With a prolonged treatment duration (72 hours; in HN5, A-43, BT474, N87, and CaLu-3 cells), Lapatinib shows selective inhibition of the proliferation of these human tumor cell lines^[1].

Specifically, in HN5 cells treated with Lapatinib (ranging from 1 to 10 µM over 72 hours), the treatment induces G1 cell cycle arrest, contributing to its antiproliferative effects^[1].

Lapatinib ditosylate monohydrate 动物研究

Dose

Rat: 100 mg/kg - 300 mg/kg^[3] (p.o.) Mice: 100 mg/kg^[4] (p.o.), 50 mg/kg^[5] (p.o.)

Administration

p.o.

Pharmacokinetics

Animal	Mice^[6]	Rats^[6]	Dogs^[6]
Dose	10 mg/kg	10 mg/kg	10 mg/kg
Administration	i.v. or p.o.	i.v. or p.o.	i.v. or p.o.
F	50.0% (p.o.)	24.0 ± 11.6% (p.o.)	41.9 ± 6.06% (p.o.)
T_1/2	5.69 h (i.v.) 1.99 h (p.o.)	12.3 ± 8.24 h (i.v.) 3.91 ± 3.98 h (p.o.)	5.85 ± 0.17 h (i.v.) 3.27 ± 1.18 h (p.o.)
T_max	0.50 h (i.v.) 0.50 h (p.o.)	0.08 h (i.v.) 0.50 - 1.00 h (p.o.)	0.08 h (i.v.) 4.00 h (p.o.)
CL	48.0 ml/min/kg (i.v.)	48.8 ± 14.3 ml/min/kg (i.v.)	12.2 ± 2.83 ml/min/kg (i.v.)
C_max	942 ng/ml (i.v.) 504 ng/ml (p.o.)	4557 ± 1210 ng/ml (i.v.) 288 ± 224 ng/ml (p.o.)	3793 ± 167 ng/ml (i.v.) 555 ± 15.1 ng/ml (p.o.)
AUC_∞	3469 ng·h/ml (i.v.) 1735 ng·h/ml (p.o.)	3596 ± 924 ng·h/ml (i.v.) 861 ± 420 ng·h/ml (p.o.)	14087 ± 3094 ng·h/ml (i.v.) 5916 ± 852 ng·h/ml (p.o.)
Vss	9.55 L/kg (i.v.)	6.16 ± 1.95 L/kg (i.v.)	5.70 ± 1.03 L/kg (i.v.)

Lapatinib ditosylate monohydrate 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.

Lapatinib ditosylate monohydrate 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

1.06mL

0.21mL

0.11mL

5.30mL

1.06mL

0.53mL

10.60mL

2.12mL

1.06mL

Lapatinib ditosylate monohydrate 技术信息

CAS号	388082-78-8
分子式	C₄₃H₄₄ClFN₄O₁₁S₃
分子量	943.476

别名	二甲苯磺酸拉帕替尼一水合物 ;GW2016 ditosylate monohydrate;GW572016 ditosylate monohydrate;Lapatinib tosilate hydrate;Lapatinib tosilate;Lapatinib ditoluenesulfonate monohydrate
运输	蓝冰

存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Inert atmosphere,2-8°C

溶解方案

细胞实验：

DMSO: 50 mg/mL(53 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验：请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用；以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

动物实验配方

二甲苯磺酸拉帕替尼水合物 /Lapatinib ditosylate monohydrate {[allProObj[0].p_purity_real_show]}

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Lapatinib ditosylate monohydrate 生物活性

Lapatinib ditosylate monohydrate 动物研究

Lapatinib ditosylate monohydrate 参考文献

Lapatinib ditosylate monohydrate 实验方案

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Lapatinib ditosylate monohydrate 实验方案

Lapatinib ditosylate monohydrate 技术信息

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