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抑制剂/激动剂
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蛋白质酪氨酸激酶(Protein Tyrosine Kinase) JAK-STAT-Signaling 肿瘤生长增殖和凋亡
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EGFR
HER2
/ Lapatinib

拉帕替尼 /Lapatinib 98%

货号：A254504 同义名： GW572016;GW2016 Ambeed 开学季，买赠积分，赢豪礼

Lapatinib（GW572016）对ErbB-2和EGFR酪氨酸激酶结构域具有强效抑制作用，对纯化EGFR和ErbB-2的IC50值分别为10.2 nM和9.8 nM。

Lapatinib 化学结构 CAS号：231277-92-2
Lapatinib 化学结构
CAS号：231277-92-2
Lapatinib 3D分子结构
CAS号：231277-92-2
Lapatinib 化学结构 CAS号：231277-92-2
Lapatinib 3D分子结构 CAS号：231277-92-2
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Lapatinib 纯度/质量文件 产品仅供科研

货号：A254504 标准纯度： 98%
批次查询： 批次纯度:

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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

 		99%+
Daphnetin +

EGFR, IC50: 7.67 μM

 		PKA,PKC 95%
Lifirafenib ++

EGFR, IC50: 29 nM

 		+

EGFR(T790M/L858R), IC50: 495 nM

 		96%
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

 		98%
CNX-2006 ++

mutant EGFR, IC50: <20 nM

 		++

mutant EGFR, IC50: <20 nM

 		98%
AZD3759 ++++

EGFR (L858R), IC50: 0.2 nM

EGFR (WT), IC50: 0.3 nM

 		98%
Erlotinib ++++

EGFR, IC50: 2 nM

 		95%
Saracatinib +++

EGFR (L861Q), IC50: 4 nM

EGFR, IC50: 5 nM

 		99%+
AG1557 ✔ 98%
Rociletinib ++

EGFR (wt), Ki: 303.3 nM

EGFR (L858R/T790M), Ki: 21.5 nM

 		98%
AG490 +

EGFR, IC50: 0.1 μM

 		98%
Cetuximab ++++

EGFR, Kd: 0.39 nM

 		95%
Osimertinib ++

L858R/T790M EGFR, IC50: 11.44 nM

WT EGFR, IC50: 12.92 nM

 		99%
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), IC50: 2 nM

EGFR (L858R/T790M), IC50: 8 nM

 		99%+
Icotinib +++

EGFR, IC50: 5 nM

 		98+%
Desmethyl Erlotinib HCl ++++

EGFR, IC50: 2 nM

 		98%
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

 		98%
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

 		98+%
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 97%
Zipalertinib +++

EGFR (L861Q), IC50: 4.1 nM

EGFR WT, IC50: 8 nM

 		+++

HER4, IC50: 4 nM

 		++++

EGFR L858R, IC50: 2 nM

EGFR(d746-750), IC50: 1.4 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 ✔ 98%
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 ✔ 98%
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

 		++++

EGFRT790M, IC50: 0.79 nM

EGFRL858R/T790M, IC50: 0.51 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

 		99+%
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

 		Raf,Src 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 (wt), IC50: 0.5 nM

EGFR (L858R/T790M), IC50: 0.4 nM

 		++

HER2, IC50: 14 nM

 		98%
Canertinib dihydrochloride +++

EGFR, IC50: 7.4 nM

 		+++

ErbB2, IC50: 9 nM

 		98%
Allitinib tosylate ++++

EGFR, IC50: 0.5 nM

EGFR (T790M/L858R), IC50: 12 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

 		98%
Afatinib ++++

EGFR (wt), IC50: 0.5 nM

EGFR (L858R), IC50: 10 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

 		98%
Tuxobertinib ++++

EGFR, Kd: 0.2 nM

 		++++

HER2, Kd: 0.76 nM

 		98%
ALK-IN-1 ++

EGFR(C797S/del19), IC50: 138.6 nM

EGFR(del19), IC50: 36.8 nM

 		ALK 98+%
Brigatinib +

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

EGFR(del19), IC50: 39.9 nM

 		ALK,FLT3 98%
Avitinib ++++

EGFR L858R/T790M, IC50: 0.18 nM

 		BTK 99%+
EAI045 ✔ 97%
Almonertinib ✔ 98%
BI-4020 ++++

EGFRdel19 T790M C797S, IC50: 0.2 nM

 		99%+
EGFR-IN-7 ++++

EGFRL858R/T790M, IC50: 0.19 nM

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

 		98%
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

 		98%
Tyrphostin AG 879 +

HER2-Neu, IC50: 1.0 μM

 		95%
TAK-285 +

HER2, IC50: 17 nM

 		99%+
ARRY-380 analog ✔ 98%
Canertinib +++

ErbB2, IC50: 9.0 nM

 		EGFR 99%+
(E/Z)-CP-724714 ++

HER2/ErbB2, IC50: 10 nM

 		98+%
Lapatinib +++

ErbB2, IC50: 9.2 nM

 		EGFR 98%
AEE788 ++++

HER2/ErbB2, IC50: 6 nM

 		EGFR 98+%
Neratinib +

HER2, IC50: 59 nM

 		EGFR,Src 98%
BMS-599626 +

HER2, IC50: 30 nM

 		99+%
Mubritinib ++++

HER2/ErbB2, IC50: 6.0 nM

 		99%+
Tucatinib +++

ErbB2, IC50: 8 nM

 		98%
Sapitinib ++++

ErbB2, IC50: 3 nM

 		EGFR 99%+
CUDC-101 ++

HER2, IC50: 15.7 nM

 		EGFR,HDAC 99%+
Afatinib dimaleate ++

HER2, IC50: 14 nM

 		98%
Afatinib ++

HER2, IC50: 14 nM

 		99%
Pertuzumab ✔ 95%
Trastuzumab ✔ 95%
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 生物活性

靶点

  • EGFR/ErbB1

    EGFR, IC50:10.8 nM

  • HER2/ErbB2

    ErbB2, IC50:9.2 nM

  • ErbB4

    ErbB4, IC50:367 nM

  • HER2

    ErbB2, IC50:9.2 nM
描述 EGFR (epidermal growth factor receptor) family consists of four members that belong to the ErbB lineage of proteins (ErbB1 - 4) with an external domain that binds activating ligands, such as EGF, and is overexpressed in a significant percentage of carcinomas and contributes to the malignant phenotype. Upon activation, EGFR phosphorylates both the receptor itself and a variety of “effector” protein. Lapatinib is a dual inhibitor of both EGFR and ErbB2 with IC50 values of 10.8 nM and 9.2 nM (measured by kinase activity), respectively, 300-fold selective over other kinases tested except for ErbB-4 (IC50 = 367 nM). Treatment with Lapatinib for 6h inhibited receptor autophosphorylation of EGFR and ErbB-2, as well as phosphorylation of serine-473 of AKT, the key signal transduction mediator, in a dose-responsive manner at concentration ranged from 0.03 to 10 μM in BT474 and HN5 cell lines. Lapatinib showed growth inhibition with IC50 values ranged from 0.09 - 12μM in EGFR-overexpressing cell lines HN5 and A-431, the ErbB-2-overexpressing cell lines BT474, N87 and CaLu-3,as well as tumor cell lines expressing low levels of EGFR and ErbB-2, MCF-7 and T47D cells. Treatment with 1 and 10 μM Lapatinib resulted in induction of G1 arrest and increased number of cells with sub-2N DNA content, consistent with cell death by an apoptotic mechanism, in EGFR-overexpressing cell line, HN5, and BT474 cells. Complete inhibition of tumor growth was seen at dose of 100mg/kg, orally, twice daily, in BT474 and HN5 human tumor xenografts[1].
作用机制 Lapatinib binds reversibly and a very slow off-rate to the ATP binding pocket in an inactive-like conformation, thus preventing autophosphorylation of the target[2].

Lapatinib 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
A101D Growth Inhibition Assay IC50=20.8587 μM SANGER
A253 Growth Inhibition Assay IC50=1.97335 μM SANGER
A388 Growth Inhibition Assay IC50=0.72258 μM SANGER
A4-Fuk Growth Inhibition Assay IC50=22.2149 μM SANGER

Lapatinib 动物研究

Dose Rat (p.o.): 50 mg/kg - 500 mg/kg[3]
Administration p.o.
Pharmacokinetics
Animal Mice[4] Rats[4] Dogs[4]
Dose 10 mg/kg 10 mg/kg 10 mg/kg
Administration i.v. i.v. i.v.
Cmax 942 ng/ml 4557 ± 1210 ng/ml 3793 ± 167 ng/ml
T1/2 5.69 h 12.3 ± 8.24 h 5.85 ± 0.17 h
CL 48.0 ml/min/kg 48.8 ± 14.3 ml/min/kg 12.2 ± 2.83 ml/min/kg
Tmax 0.5 h 0.08 h 0.08 h
Vss 9.55 L/kg 6.16 ± 1.95 L/kg 5.70 ± 1.03 L/kg
AUC∞ 3469 ng·h/ml 3596 ± 924 ng·h/ml 14087 ± 3094 ng·h/ml

Lapatinib 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
NCT00555152 Ductal Breast Carcinoma In Sit... 展开 >>u HER2/Neu Positive 收起 << Not Applicable Completed - United States, Alabama ... 展开 >> University of Alabama at Birmingham Cancer Center Birmingham, Alabama, United States, 35233 United States, Texas M D Anderson Cancer Center Houston, Texas, United States, 77030 收起 <<
NCT00555152 - Completed - -
NCT00999804 Breast Cancer Phase 2 Active, not recruiting January 2018 United States, Alabama ... 展开 >> University of Alabama - Birmingham Birmingham, Alabama, United States, 35294 United States, Illinois University of Chicago Chicago, Illinois, United States, 60637 United States, Indiana Indiana University Indianapolis, Indiana, United States, 46202 United States, Maryland Johns Hopkins Baltimore, Maryland, United States, 21231 United States, Massachusetts Dana Farber Cancer Institute Boston, Massachusetts, United States, 02130 United States, North Carolina Duke University Durham, North Carolina, United States, 27705 United States, Tennessee Vanderbilt University Medical Center Nashville, Tennessee, United States, 37212 United States, Texas Baylor College of Medicine Lester and Sue Smith Breast Center Houston, Texas, United States, 77030 收起 <<

Lapatinib 参考文献

[1]Rusnak DW, Lackey K, 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]Wood ER, Truesdale AT, et al. A unique structure for epidermal growth factor receptor bound to GW572016 (Lapatinib): relationships among protein conformation, inhibitor off-rate, and receptor activity in tumor cells. Cancer Res. 2004 Sep 15;64(18):6652-9.

[3]ASSESSMENT REPORT FOR TYVERB

[4]Pharmacokinetics of lapatinib

Lapatinib 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.72mL

0.34mL

0.17mL

8.60mL

1.72mL

0.86mL

17.21mL

3.44mL

1.72mL

Lapatinib 技术信息

CAS号231277-92-2
分子式C29H26ClFN4O4S
分子量 581.058
别名 GW572016;GW2016;GSK572016
运输蓝冰
存储条件

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度

DMSO: 120 mg/mL(206.52 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

IP 2% DMSO+2% Tween80+35% PEG300+water 10 mg/mL clear

PO 0.5% CMC-Na 45 mg/mL suspension

Tags: Lapatinib | GW572016;GW2016;GSK572016 | EGFR | HER2 | AmBeed-信号通路专用抑制剂 | Lapatinib 纯度/质量文件 | Lapatinib 亚型比较 | Lapatinib 生物活性 | Lapatinib 细胞研究 | Lapatinib 动物研究 | Lapatinib 临床数据 | Lapatinib 参考文献 | Lapatinib 实验方案 | Lapatinib 技术信息

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