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/ Lapatinib ditosylate

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

货号：A208985 同义名： 二对甲苯磺酸拉帕替尼 / GW572016 ditosylate;GW2016 ditosylate Ambeed 开学季，买赠积分，赢豪礼

Lapatinib ditosylate (GW572016 ditosylate) 是一种强效的ErbB-2和EGFR酪氨酸激酶结构域抑制剂，对纯化EGFR和ErbB-2的IC50值分别为10.2 nM和9.8 nM。

Lapatinib ditosylate 化学结构 CAS号：388082-77-7
Lapatinib ditosylate 化学结构
CAS号：388082-77-7
Lapatinib ditosylate 3D分子结构
CAS号：388082-77-7
Lapatinib ditosylate 化学结构 CAS号：388082-77-7
Lapatinib ditosylate 3D分子结构 CAS号：388082-77-7
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Lapatinib ditosylate 纯度/质量文件 产品仅供科研

货号：A208985 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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• Biomacromolecules, 2024. Ambeed. [ A110759 ]
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产品名称 EGFR/ErbB1 ↓ ErbB3 ↓ ErbB4 ↓ HER2/ErbB2 ↓ mutant EGFR ↓ 其他靶点 纯度
WZ-3146 ++++

EGFR (E746_A750), IC50: 2 nM

EGFR (E746_A750/T790M), IC50: 14 nM

 		{[allProObj[0].p_purity_real_show]}
Daphnetin +

EGFR, IC50: 7.67 μM

 		PKA,PKC {[allProObj[0].p_purity_real_show]}
Lifirafenib ++

EGFR, IC50: 29 nM

 		+

EGFR(T790M/L858R), IC50: 495 nM

 		{[allProObj[0].p_purity_real_show]}
PD168393 ++++

EGFR, IC50: 0.70 nM

 		{[allProObj[0].p_purity_real_show]}
Nazartinib ++

mutant EGFR, Ki: 0.031 μM

 		++

mutant EGFR, Ki: 0.031 μM

 		{[allProObj[0].p_purity_real_show]}
Norcantharidin ✔ {[allProObj[0].p_purity_real_show]}
CL-387785 ++++

EGFR, IC50: 370 pM

 		{[allProObj[0].p_purity_real_show]}
WHI-P154 +++

EGFR, IC50: 4 nM

 		VEGFR,Src {[allProObj[0].p_purity_real_show]}
Tyrphostin A9 +

EGFR, IC50: 460 μM

 		PDGFR {[allProObj[0].p_purity_real_show]}
AG 555 +

EGFR, IC50: 0.7 μM

 		{[allProObj[0].p_purity_real_show]}
AG 494 +

EGFR, IC50: 1.2 μM

 		{[allProObj[0].p_purity_real_show]}
AG-556 +

EGFR, IC50: 5 μM

 		{[allProObj[0].p_purity_real_show]}
RG13022 +

EGFR, IC50: 4 μM

 		{[allProObj[0].p_purity_real_show]}
Tyrphostin RG 14620 ✔ {[allProObj[0].p_purity_real_show]}
Vandetanib +

EGFR, IC50: 500 nM

 		{[allProObj[0].p_purity_real_show]}
CNX-2006 ++

mutant EGFR, IC50: <20 nM

 		++

mutant EGFR, IC50: <20 nM

 		{[allProObj[0].p_purity_real_show]}
AZD3759 ++++

EGFR (L858R), IC50: 0.2 nM

EGFR (WT), IC50: 0.3 nM

 		{[allProObj[0].p_purity_real_show]}
Erlotinib ++++

EGFR, IC50: 2 nM

 		{[allProObj[0].p_purity_real_show]}
Saracatinib +++

EGFR (L861Q), IC50: 4 nM

EGFR, IC50: 5 nM

 		{[allProObj[0].p_purity_real_show]}
AG1557 ✔ {[allProObj[0].p_purity_real_show]}
Rociletinib ++

EGFR (wt), Ki: 303.3 nM

EGFR (L858R/T790M), Ki: 21.5 nM

 		{[allProObj[0].p_purity_real_show]}
AG490 +

EGFR, IC50: 0.1 μM

 		{[allProObj[0].p_purity_real_show]}
Cetuximab ++++

EGFR, Kd: 0.39 nM

 		{[allProObj[0].p_purity_real_show]}
Osimertinib ++

L858R/T790M EGFR, IC50: 11.44 nM

WT EGFR, IC50: 12.92 nM

 		{[allProObj[0].p_purity_real_show]}
Osimertinib mesylate ✔ {[allProObj[0].p_purity_real_show]}
Chrysophanol ✔ mTOR {[allProObj[0].p_purity_real_show]}
PD153035 ++++

EGFR, Ki: 5.2 pM

 		{[allProObj[0].p_purity_real_show]}
Olmutinib ✔ BTK {[allProObj[0].p_purity_real_show]}
WZ4002 ++++

EGFR (L858R), IC50: 2 nM

EGFR (L858R/T790M), IC50: 8 nM

 		{[allProObj[0].p_purity_real_show]}
Icotinib +++

EGFR, IC50: 5 nM

 		{[allProObj[0].p_purity_real_show]}
Desmethyl Erlotinib HCl ++++

EGFR, IC50: 2 nM

 		{[allProObj[0].p_purity_real_show]}
Cyasterone ✔ {[allProObj[0].p_purity_real_show]}
PP 3 +

EGFR tyrosine kinase, IC50: 2.7 μM

 		{[allProObj[0].p_purity_real_show]}
WZ8040 ✔ {[allProObj[0].p_purity_real_show]}
(-)-Epigallocatechin Gallate ✔ {[allProObj[0].p_purity_real_show]}
AG 18 +

EGFR, IC50: 35 μM

 		{[allProObj[0].p_purity_real_show]}
O-Desmethyl gefitinib ++

EGFR, IC50: 36 nM

 		{[allProObj[0].p_purity_real_show]}
Falnidamol ✔ {[allProObj[0].p_purity_real_show]}
AZ-5104 ++++

EGFR (L858R), IC50: 6 nM

EGFR (L861Q) , IC50: <1 nM

 		+++

ErbB4, IC50: 7 nM

 		BRK {[allProObj[0].p_purity_real_show]}
Butein ✔ {[allProObj[0].p_purity_real_show]}
Genistein ✔ {[allProObj[0].p_purity_real_show]}
SU5214 +

EGFR, IC50: 36.7 μM

 		{[allProObj[0].p_purity_real_show]}
Naquotinib ✔ {[allProObj[0].p_purity_real_show]}
Gefitinib ++

EGFR, IC50: 15.5 nM

 		+

EGFR (858R/T790M), IC50: 823.3 nM

 		{[allProObj[0].p_purity_real_show]}
Theliatinib +++

WT EGFR, IC50: 3 nM

 		++

EGFR T790M/L858R, IC50: 22 nM

 		{[allProObj[0].p_purity_real_show]}
Lazertinib ++++

L858R/T790M EGFR, IC50: 2 nM

WT EGFR, IC50: 76 nM

 		++++

Del19/T790M, IC50: 1.7 nM

 		{[allProObj[0].p_purity_real_show]}
Gefitinib-based PROTAC 3 ++

EGFR, DC50: 22.3 nM

 		{[allProObj[0].p_purity_real_show]}
MTX-211 ✔ PI3K {[allProObj[0].p_purity_real_show]}
(E)-AG 99 ✔ {[allProObj[0].p_purity_real_show]}
Licochalcone D ✔ Caspase,PARP {[allProObj[0].p_purity_real_show]}
Zipalertinib +++

EGFR WT, IC50: 8 nM

EGFR (L861Q), IC50: 4.1 nM

 		+++

HER4, IC50: 4 nM

 		++++

EGFR L858R, IC50: 2 nM

EGFR(d746-750), IC50: 1.4 nM

 		{[allProObj[0].p_purity_real_show]}
JND3229 +++

EGFR WT, IC50: 6.8 nM

 		++

EGFR L858R/T790M, IC50: 30.5 nM

 		{[allProObj[0].p_purity_real_show]}
Firmonertinib mesylate ✔ {[allProObj[0].p_purity_real_show]}
Tyrphostin AG30 ✔ {[allProObj[0].p_purity_real_show]}
EGFR-IN-12 ++

EGFR, IC50: 21 nM

 		{[allProObj[0].p_purity_real_show]}
Mobocertinib ✔ {[allProObj[0].p_purity_real_show]}
(Rac)-JBJ-04-125-02 ✔ {[allProObj[0].p_purity_real_show]}
(S)-Sunvozertinib ✔ {[allProObj[0].p_purity_real_show]}
BLU-945 ✔ {[allProObj[0].p_purity_real_show]}
Poziotinib +++

HER1, IC50: 3.2 nM

 		++

HER4, IC50: 23.5 nM

 		+++

HER2, IC50: 5.3 nM

 		{[allProObj[0].p_purity_real_show]}
TAK-285 ++

EGFR/HER1, IC50: 23 nM

 		+

HER4, IC50: 260 nM

 		++

HER2, IC50: 17 nM

 		{[allProObj[0].p_purity_real_show]}
ARRY-380 analog ✔ {[allProObj[0].p_purity_real_show]}
Canertinib ++++

EGFR, IC50: 1.5 nM

 		+++

ErbB2, IC50: 9.0 nM

 		{[allProObj[0].p_purity_real_show]}
Dacomitinib +++

EGFR, IC50: 6.0 nM

 		+

ErbB4, IC50: 73.7 nM

 		+

ErbB2, IC50: 45.7 nM

 		{[allProObj[0].p_purity_real_show]}
EGFR/ErbB-2/ErbB-4 inhibitor-2 +

ErbB4, IC50: 1.91 μM

 		+

ErbB2, IC50: 0.08 μM

 		{[allProObj[0].p_purity_real_show]}
(E/Z)-CP-724714 ++

HER2/ErbB2, IC50: 10 nM

 		{[allProObj[0].p_purity_real_show]}
Lapatinib ++

EGFR, IC50: 10.8 nM

 		+

ErbB4, IC50: 367 nM

 		+++

ErbB2, IC50: 9.2 nM

 		{[allProObj[0].p_purity_real_show]}
AEE788 ++++

EGFR, IC50: 2 nM

 		+

HER4/ErbB4, IC50: 160 nM

 		+++

HER2/ErbB2, IC50: 6 nM

 		c-Fms {[allProObj[0].p_purity_real_show]}
AV-412 free base ++++

EGFR, IC50: 0.75 nM

 		++

ErbB2, IC50: 19 nM

 		++++

EGFRT790M, IC50: 0.79 nM

EGFRL858R/T790M, IC50: 0.51 nM

 		{[allProObj[0].p_purity_real_show]}
Neratinib +

EGFR, IC50: 92 nM

 		+

HER2, IC50: 59 nM

 		Src {[allProObj[0].p_purity_real_show]}
BMS-599626 ++

HER1, IC50: 20 nM

 		+

HER4, IC50: 190 nM

 		++

HER2, IC50: 30 nM

 		{[allProObj[0].p_purity_real_show]}
Tucatinib +++

ErbB2, IC50: 8 nM

 		{[allProObj[0].p_purity_real_show]}
Allitinib ++++

EGFR, IC50: 0.5 nM

 		++++

ErbB4, IC50: 0.8 nM

 		+++

ErbB2, IC50: 3.0 nM

 		{[allProObj[0].p_purity_real_show]}
Pelitinib +

EGFR, IC50: 38.5 nM

 		+

ErbB2, IC50: 1.255 μM

 		Raf,Src {[allProObj[0].p_purity_real_show]}
Sapitinib +++

EGFR, IC50: 4 nM

 		+++

ErbB3, IC50: 4 nM

 		+++

ErbB2, IC50: 3 nM

 		{[allProObj[0].p_purity_real_show]}
CUDC-101 +++

EGFR, IC50: 2.4 nM

 		++

HER2, IC50: 15.7 nM

 		HDAC {[allProObj[0].p_purity_real_show]}
Varlitinib +++

ErbB1, IC50: 7 nM

 		++++

ErbB2, IC50: 2 nM

 		{[allProObj[0].p_purity_real_show]}
Afatinib dimaleate ++++

EGFR (wt), IC50: 0.5 nM

EGFR (L858R/T790M), IC50: 0.4 nM

 		++

HER2, IC50: 14 nM

 		{[allProObj[0].p_purity_real_show]}
Canertinib dihydrochloride +++

EGFR, IC50: 7.4 nM

 		+++

ErbB2, IC50: 9 nM

 		{[allProObj[0].p_purity_real_show]}
Allitinib tosylate ++++

EGFR (T790M/L858R), IC50: 12 nM

EGFR, IC50: 0.5 nM

 		++++

ErbB4, IC50: 0.8 nM

 		+++

ErbB2, IC50: 3.0 nM

 		{[allProObj[0].p_purity_real_show]}
Tyrphostin AG 528 +

EGFR, IC50: 4.9 μM

 		+

HER2, IC50: 2.1 μM

 		{[allProObj[0].p_purity_real_show]}
Afatinib ++++

EGFR (wt), IC50: 0.5 nM

EGFR (L858R), IC50: 10 nM

 		++++

ErbB4, IC50: 1 nM

 		++

HER2, IC50: 14 nM

 		{[allProObj[0].p_purity_real_show]}
Pyrotinib dimaleate ++

EGFR, IC50: 0.013 μM

 		++

HER2, IC50: 0.038 μM

 		{[allProObj[0].p_purity_real_show]}
Epertinib HCl ++++

EGFR, IC50: 1.48 nM

 		+++

HER4, IC50: 2.49 nM

 		+++

HER2, IC50: 7.15 nM

 		{[allProObj[0].p_purity_real_show]}
Tuxobertinib ++++

EGFR, Kd: 0.2 nM

 		++++

HER2, Kd: 0.76 nM

 		{[allProObj[0].p_purity_real_show]}
ALK-IN-1 ++

EGFR(del19), IC50: 36.8 nM

EGFR(C797S/del19), IC50: 138.6 nM

 		ALK {[allProObj[0].p_purity_real_show]}
Brigatinib +

EGFR(del19), IC50: 39.9 nM

EGFR(C797S/T790M/del19), IC50: 67.2 nM

 		ALK,FLT3 {[allProObj[0].p_purity_real_show]}
Avitinib ++++

EGFR L858R/T790M, IC50: 0.18 nM

 		BTK {[allProObj[0].p_purity_real_show]}
EAI045 ✔ {[allProObj[0].p_purity_real_show]}
Almonertinib ✔ {[allProObj[0].p_purity_real_show]}
BI-4020 ++++

EGFRdel19 T790M C797S, IC50: 0.2 nM

 		{[allProObj[0].p_purity_real_show]}
EGFR-IN-7 ++++

EGFRd746-750/T790M/C797S, IC50: 0.26 nM

EGFRL858R/T790M, IC50: 0.19 nM

 		{[allProObj[0].p_purity_real_show]}
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。
产品名称 HER2 ↓ 其他靶点 纯度
Poziotinib ++++

HER2, IC50: 5.3 nM

 		{[allProObj[0].p_purity_real_show]}
Tyrphostin AG 879 +

HER2-Neu, IC50: 1.0 μM

 		{[allProObj[0].p_purity_real_show]}
TAK-285 +

HER2, IC50: 17 nM

 		{[allProObj[0].p_purity_real_show]}
ARRY-380 analog ✔ {[allProObj[0].p_purity_real_show]}
Canertinib +++

ErbB2, IC50: 9.0 nM

 		EGFR {[allProObj[0].p_purity_real_show]}
(E/Z)-CP-724714 ++

HER2/ErbB2, IC50: 10 nM

 		{[allProObj[0].p_purity_real_show]}
Lapatinib +++

ErbB2, IC50: 9.2 nM

 		EGFR {[allProObj[0].p_purity_real_show]}
AEE788 ++++

HER2/ErbB2, IC50: 6 nM

 		EGFR {[allProObj[0].p_purity_real_show]}
Neratinib +

HER2, IC50: 59 nM

 		Src,EGFR {[allProObj[0].p_purity_real_show]}
BMS-599626 +

HER2, IC50: 30 nM

 		{[allProObj[0].p_purity_real_show]}
Mubritinib ++++

HER2/ErbB2, IC50: 6.0 nM

 		{[allProObj[0].p_purity_real_show]}
Tucatinib +++

ErbB2, IC50: 8 nM

 		{[allProObj[0].p_purity_real_show]}
Sapitinib ++++

ErbB2, IC50: 3 nM

 		EGFR {[allProObj[0].p_purity_real_show]}
CUDC-101 ++

HER2, IC50: 15.7 nM

 		HDAC,EGFR {[allProObj[0].p_purity_real_show]}
Afatinib dimaleate ++

HER2, IC50: 14 nM

 		{[allProObj[0].p_purity_real_show]}
Afatinib ++

HER2, IC50: 14 nM

 		{[allProObj[0].p_purity_real_show]}
Pertuzumab ✔ {[allProObj[0].p_purity_real_show]}
Trastuzumab ✔ {[allProObj[0].p_purity_real_show]}
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 生物活性

描述 Deregulated expression of receptors EGFR and HER2, two closely related members of the ErbB family of transmembrane receptor tyrosine kinases, has been implicated in the development and malignancy of numerous types of human cancers, making them become a potential target for therapy. Lapatinib Ditosylate is the ditosylate form of lapatinib. Lapatinib is a potent and selective inhibitor of ErbB-2 and EGFR with IC50 values of 9.8nM and 10.2nM (measured by kinase activity assay), respectively. Treatment with lapatinib at concentration ranging in 0.03-10μM for 6h caused dose-dependent decrease of autophosphorylation of both EGFR and ErbB-2 in HN5 and BT474 cells, alone with the decreased phosphorylation level of the key signal transduction mediator AKT. Cell lines with overexpression of ErbB-2 or EGFR, including A431, HN5, BT474, N87, CaLu-3 and HB4a c5.2, were more sensitive to lapatinib with IC50 values ranging in 0.09-0.21μM 72h growth inhibition assays, showing the selective inhibition of cell growth by lapatinib. Induction of G1 arrest can be observed in HN5, EGFR-overexpressing cell line, treated with 1 or 10μM lapatinib. Apoptosis can be significantly induced by 10μM lapatinib after 72h in BT474 cells. Oral administration of lapatinib at dose of 100mg/kg twice daily for 21 days achieved a complete inhibition of tumor growth in both BT474 and HN5 human tumor xenografts[1].
作用机制 Lapatinib is an ATP-competitive inhibitor of both EGFR and HER2.[1]

Lapatinib ditosylate 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
22Rv1 cell Cytotoxicity assay 4 days Cytotoxicity against human 22Rv1 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50=6.06 μM 22169601
A253 cell Growth inhibition assay Inhibition of human A253 cell growth in a cell viability assay, IC50=2.0483 μM SANGER
A388 cell Growth inhibition assay Inhibition of human A388 cell growth in a cell viability assay, IC50=2.0483 μM SANGER
A431 cells Cytotoxicity assay Cytotoxicity against human A431 cells after 72 hrs by SRB assay, IC50=0.104 μM 19888761

Lapatinib ditosylate 动物研究

Dose Mice[2]: 2 mg/kg - 100 mg/kg (p.o.), 10 mg/kg (i.v.), rat[2]: 2 mg/kg - 10 mg/kg (p.o.), 10 mg/kg (i.v.)
Administration p.o., i.v.
Pharmacokinetics
Animal Mice[2] Rats[2] Dogs[2]
Dose 10 mg/kg 10 mg/kg 10 mg/kg
Administration i.v. i.v. i.v.
AUC∞ 3469 ng·h/ml 3596 ± 924 ng·h/ml 14087 ± 3094 ng·h/ml
T1/2 5.69 h 12.3 ± 8.24 h 5.85 ± 0.17 h
Tmax 0.5 h 0.08 h 0.08 h
CL 48.0 ml/min/kg 48.8 ± 14.3 ml/min/kg 12.2 ± 2.83 ml/min/kg
Cmax 942 ng/ml 4557 ± 1210 ng/ml 3793 ± 167 ng/ml
Vss 9.55 L/kg 6.16 ± 1.95 L/kg 5.70 ± 1.03 L/kg

Lapatinib ditosylate 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00849329 Neoplasms, Breast Phase 1 Completed - United States, South Carolina ... 展开 >> GSK Investigational Site Greenville, South Carolina, United States, 29605 Korea, Republic of GSK Investigational Site Seoul, Korea, Republic of, 135-710 GSK Investigational Site Songpa-gu, Seoul, Korea, Republic of, 138-736 Spain GSK Investigational Site Hospitalet de Llobregat (Barcelona), Spain, 08907 收起 <<
NCT00486954 Neoplasms, Gastrointestinal Tr... 展开 >>act 收起 << Phase 3 Completed - China, Guangdong ... 展开 >> GSK Investigational Site Guangzhou, Guangdong, China, 510060 China GSK Investigational Site Beijing, China, 100021 GSK Investigational Site Beijing, China, 100071 GSK Investigational Site Shanghai, China, 200032 Japan GSK Investigational Site Tokyo, Japan, 113-8677 Korea, Republic of GSK Investigational Site Hwasun, Korea, Republic of, 519-809 GSK Investigational Site Seongnam-si Gyeonggi-do, Korea, Republic of, 463-707 GSK Investigational Site Seoul, Korea, Republic of, 110-744 GSK Investigational Site Seoul, Korea, Republic of, 120-752 GSK Investigational Site Seoul, Korea, Republic of, 135-710 Taiwan GSK Investigational Site Kaohsiung, Taiwan, 807 GSK Investigational Site Niaosong Township, Kaohsiung, Taiwan, 833 GSK Investigational Site Tainan County, Taiwan, 736 GSK Investigational Site Tainan, Taiwan, 704 GSK Investigational Site Taipei, Taiwan, 100 GSK Investigational Site Taipei, Taiwan, 112 GSK Investigational Site Tau-Yuan County, Taiwan, 333 收起 <<
NCT00486954 - Completed - -

Lapatinib ditosylate 参考文献

[1]Pharmacokinetics of lapatinib

Lapatinib ditosylate 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.08mL

0.22mL

0.11mL

5.40mL

1.08mL

0.54mL

10.81mL

2.16mL

1.08mL

Lapatinib ditosylate 技术信息

CAS号388082-77-7
分子式C43H42ClFN4O10S3
分子量 925.461
别名 二对甲苯磺酸拉帕替尼 ;GW572016 ditosylate;GW2016 ditosylate
运输蓝冰
存储条件

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度

DMSO: 120 mg/mL(129.67 mM)，配合低频超声助溶，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
动物实验配方

2% DMSO+30% PEG 300+water 10 mg/mL

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