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/ EGFR / Gefitinib

吉非替尼 /Gefitinib 98%

货号：A109874 同义名： 吉非替尼 (ZD1839) / ZD1839 Ambeed 开学季，买赠积分，赢豪礼

Gefitinib（ZD1839）（GMP）是按照GMP指南生产的，作为细胞治疗的辅助试剂。Gefitinib是一种强效、选择性和口服活性的EGFR酪氨酸激酶抑制剂。

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Gefitinib 化学结构 CAS号：184475-35-2
Gefitinib 化学结构
CAS号：184475-35-2
Gefitinib 3D分子结构
CAS号：184475-35-2
Gefitinib 化学结构 CAS号：184475-35-2
Gefitinib 3D分子结构 CAS号：184475-35-2
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Gefitinib 纯度/质量文件 产品仅供科研

货号：A109874 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。

Gefitinib 生物活性

靶点

  • EGFR/ErbB1

    Tyr1173 (NR6W cells), IC50:57 nM

    Tyr992 (NR6wtEGFR cells), IC50:37 nM

  • EGFR/ErbB1

    EGFR, IC50:15.5 nM

  • mutant EGFR

    EGFR (858R/T790M), IC50:823.3 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. Gefitinib is an effective EGFR inhibitor with IC50 values of 37 nM, 37 nM, 26 nM and 57 nM for Tyr1173, Tyr992, Tyr1173 and Tyr992 EGFR sites (measured by EGFR tyrosine phosphorylations in cells), respectively in NR6 wt EGFR and NR6W cells. Gefitinib can sufficiently suppress all tyrosine phosphorylation sites, with less sensitivity to Tyr1173 and Tyr992 sites, on EGFR in both the high and low-EGFR-expressing cell lines, as well as EGFR-mediated proliferation. However, EGFR-mediated anchorage-independent growth was not sufficient to inhibit these features in cells expressing EGFRvIII, with approximately four times as resistant to gefitinib as EGFR. Long-term exposure of EGFRvIII-expressing cells to low concentrations of gefitinib (0.01 - 0.1 μM) resulted in increased phosphotyrosine load of the receptor, increased signaling to ERK and stimulation of proliferation and anchorage-independent growth while higher concentrations of gefitinib (1 - 2 μM) completely showed the opposite effect, presumably by inducing EGFRvIII dimerization[1]. Gefitinib (40 mg/kg body weight/day) showed significant inhibition of tumor load when treated with weekly or weekly intermittent dosing regimens in lung adenocarcinoma model whereas a daily dosing regimen did not decrease the tumor load significantly[2].
作用机制 Gefitinib is an ATP-competitive inhibitor of EGFR[3].

Gefitinib 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
16HBE Growth Inhibition Assay 72 h Antiproliferative activity against human 16HBE cells expressing wild type EGFR with IC50 of 1.601 μM 23792318
16HBE 100 μM Function Assay 150 min Induction of nitric oxide production in human 16HBE cells expressing wild type EGFR 23792318
16HBE14o- 10 μM Cytotoxic Assay 72 h Cytotoxicity against human 16HBE14o- cells harboring wild type EGFR assessed as growth inhibition with IC50 of 12.71 μM 23668441
23132-87 Growth Inhibition Assay IC50=864.28 nM SANGER

Gefitinib 动物研究

Dose Mice (p.o.): min = 5 mg/kg[4], max = 300 mg/kg[5]
Administration p.o.
Pharmacokinetics
Animal Rats[6]
Dose 5 mg/kg
Administration i.v.
p.o.
Cmax 230 ng/ml (p.o.)
T1/2 5.3 h (i.v.)
4.1 h (p.o.)
Vdss 9.8 L/kg (i.v.)
AUC0-8 1130 ng·h/ml (p.o.)
F 49.8% (p.o.)
AUC0-inf 3540 ng·h/ml (i.v.)
1780 ng·h/ml (p.o.)
Tmax 4 h (p.o.)
CL 23.6 ml/min/kg (i.v.)

Gefitinib 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
NCT00206414 BREAST CANCER Phase 2 Terminated(Difficulty accruing... 展开 >> subjects the study accrual was closed) 收起 << - United States, Texas ... 展开 >> Baylor Breast Center Houston, Texas, United States, 77030 收起 <<
NCT00820417 Colorectal Cancer ... 展开 >> Head and Neck Cancer Non Small Cell Lung Cancer (NSCLC) 收起 << Phase 1 Completed - Belgium ... 展开 >> UZ Gasthuisberg Leuven, Belgium, 3000 Spain Hospital Universitari Vall d'Hebron Barcelona, Spain, 08035 收起 <<
NCT00025207 Advanced Malignant Mesotheliom... 展开 >>a Epithelial Mesothelioma Recurrent Malignant Mesothelioma Sarcomatous Mesothelioma 收起 << Phase 2 Completed - United States, Illinois ... 展开 >> Cancer and Leukemia Group B Chicago, Illinois, United States, 60606 收起 <<

Gefitinib 参考文献

[1]Pedersen MW, Pedersen N, et al. Differential response to gefitinib of cells expressing normal EGFR and the mutant EGFRvIII. Br J Cancer. 2005 Oct 17;93(8):915-23.

[2]Zhang Q, Li R, et al. Effect of weekly or daily dosing regimen of Gefitinib in mouse models of lung cancer. Oncotarget. 2017 Aug 2;8(42):72447-72456.

[3]Gokhale AG, Rajagopal P, et al. Cockroach in right main bronchus--an unusual foreign body. Indian J Chest Dis Allied Sci. 1992 Apr-Jun;34(2):103-5.

[4]Kishino D, Kiura K, et al. Effect of gefitinib on N-nitrosamine-4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone induced lung tumorigenesis in A/J mice. Lung Cancer. 2009 Sep;65(3):284-9.

[5]Mikumo H, Yanagihara T, et al. Neutrophil elastase inhibitor sivelestat ameliorates gefitinib-naphthalene-induced acute pneumonitis in mice. Biochem Biophys Res Commun. 2017 Apr 22;486(1):205-209.

[6]Pharmacokinetics of gefitinib

Gefitinib 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.24mL

0.45mL

0.22mL

11.19mL

2.24mL

1.12mL

22.38mL

4.48mL

2.24mL

Gefitinib 技术信息

CAS号184475-35-2
分子式C22H24ClFN4O3
分子量 446.9
别名 吉非替尼 (ZD1839) ;ZD1839
运输蓝冰
存储条件

粉末 Keep in dark place,Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度

DMSO: 105 mg/mL(234.95 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

1% CMC Na+water 30 mg/mL suspension

Tags: Gefitinib | ZD1839 | 吉非替尼 (ZD1839) | EGFR | AmBeed-信号通路专用抑制剂 | Gefitinib 纯度/质量文件 | Gefitinib 亚型比较 | Gefitinib 生物活性 | Gefitinib 细胞研究 | Gefitinib 动物研究 | Gefitinib 临床数据 | Gefitinib 参考文献 | Gefitinib 实验方案 | Gefitinib 技术信息

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