EGFR/HER2
Inhibitory Selectivity
| Catalog No. | Inhibitor Name | EGFR/ErbB1 | HER2/ErbB2 | ErbB3 | ErbB4 | Other |
| A10362 | Erlotinib HCl | **** | | | | |
| A10422 | Gefitinib | ** | | | | |
| A10514 | Lapatinib Ditosylate | ** | ** | | * | c-Src |
| A10141 | Afatinib | **** | ** | | | |
| A10638 | Neratinib | * | * | | | KDR,Src |
| A10211 | Canertinib | **** | *** | | | |
| A11752 | Lapatinib | ** | ** | | * | c-Src |
| A10047 | AG-490 | * | * | | | JAK2 |
| A10242 | CP-724714 | | ** | | | |
| A11051 | Dacomitinib | *** | * | | * | |
| A10991 | WZ4002 | **** | | *** | | |
| A10116 | Sapitinib | *** | *** | | | HDAC,HDAC1,HDAC6 |
| A10246 | CUDC-101 | *** | ** | | | |
| A11022 | AG-1478 | *** | | | | |
| A10702 | PD153035 HCl | **** | | | | Src,MEK/ERK,Raf |
| A10706 | Pelitinib | * | * | | | c-Abl,FLT1,c-Fms |
| A10043 | AEE788 | **** | *** | | * | MEK,LCK,VEGFR2 |
| A11209 | AC480 | ** | * | | * | |
| A10678 | OSI-420 | **** | | | | |
| A10990 | WZ3146 | **** | | | | |
| A11155 | AST-1306 | **** | *** | | **** | |
| A13028 | Rociletinib | ** | | | | |
| A11158 | Varlitinib | *** | **** | | | |
| A13825 | Icotinib | *** | | | | MEK1,Aurora B,LCK |
| A11236 | TAK-285 | ** | ** | | * | Src,VEGFR,JAK3 |
| A14049 | WHI-P154 | *** | | | | |
| A12725 | PD168393 | **** | | | | |
| A13755 | CNX-2006 | ** | | | | PDGFR |
| A11949 | Tyrphostin 9 | * | | | | |
| A15940 | AG-18 | * | | | | |
| A15551 | AZD3759 | **** | | | | |
| A14985 | Afatinib Dimaleate | **** | ** | | | |
| A13146 | CL-387785 | **** | | | | |
| A13044 | Poziotinib | *** | *** | | ** | |
| A13681 | Osimertinib | ** | | | | BLK,ACK1,BRK |
| A15516 | AZ5104 | **** | | | *** | |
| A10992 | WZ8040 |
| | | | topo II |
| A10426 | Genistein |
| | | | |
| A12448 | Butein |
| | | | mTOR |
| A10210 | Chrysophanic Acid |
| | | | |
| A10053 | Tyrphostin AG 879 | | * | | | Trk |
| A10286 | Daphnetin | * | | | | PKC, PKA |
| A11027 | Irbinitinib (ARRY-380, ONT-380) | | **** | | | |
| A11028 | AV-412 | *** | * | | | |
| A11334 | BIBX 1382 | **** | * | | | |
| A12867 | CGP-52411 | * | | | | |
| A13588 | Tyrphostin AG 183 | * | | | | |
| A15509 | WHI-P180 | * | | | | Cdk2 |
| A10612 | Mubritinib (TAK 165) | | **** | | | |
| A16413 | ARRY-380 (Irbinitinib) | | **** | | | |
Notes:
1.Hover mouse over " * " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " * " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.
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Antioxidant, antiangiogenic, antitumor agent
(-)-Epigallocatechin gallate是一种从绿茶中分离出来的强效抗氧化剂多酚类黄酮。
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- Wafa Dridi, .et al. Influence of polysaccharide concentration on polyphenol-polysaccharide interactions, Carbohydr Polym, 2021, 274:118670 PMID: 34702486
- A S D'Costa, .et al. Inhibition of starch digestion by flavonoids: Role of flavonoid-amylase binding kinetics, Food Chem, 2020, Oct 1;341(Pt 2):128256 PMID: 33035827
- Fenteany G, .et al. Multilevel structure-activity profiling reveals multiple green tea compound families that each modulate ubiquitin-activating enzyme and ubiquitination by a distinct mechanism, Sci Rep, 2019, Sep 5;9(1):12801 PMID: 31488855
- LiliSun, .et al. Comparative Effect of Black, Green, Oolong and White Tea Intake on Body Weight Gain and Bile Acid Metabolism, Nutrition, 2019, pii:S0899-9007(18)31140-7
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EGFR 抑制剂
Pelitinib (EKB-569)是一种有效的,不可逆EGFR抑制剂,IC50为38.5 nM
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- Shi P, .et al. The Third-Generation EGFR Inhibitor, Osimertinib, Promotes c-FLIP Degradation, Enhancing Apoptosis Including TRAIL-Induced Apoptosis in NSCLC Cells with Activating EGFR Mutations, Transl Oncol, 2019, Mar 8;12(5):705-713 PMID: 30856555
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HER2 抑制剂
Neratinib (HKI-272)是一种酪氨酸激酶抑制剂。
了解更多
- Hamzehlou S, .et al. Anti-tumor activity of neratinib, a pan-HER inhibitor, in gastric adenocarcinoma cells, Eur J Pharmacol, 2019, Nov 15;863:172705 PMID: 31574259
- Li Li, .et al. Evidence for activated Lck protein tyrosine kinase as the driver of proliferation in acute myeloid leukemia cell, CTV-1, Leukemia Res, 2019, 78:12-20 PMID: 30660961
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HER2/ErbB2 抑制剂
Canertinib (CI-1033)是一种不可逆的酪氨酸激酶抑制剂，对EGFR（IC50 0.8 nM），HER-2（IC50 19 nM）和ErbB-4（IC50 7 nM）具有活性。
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- Fukuda N, .et al. Rapid Evaluation of Tyrosine Kinase Activity of Membrane Integrated Human Epidermal Growth Factor Receptor Using the Yeast Gγ Recruitment System, ACS Synth Biol., 2015, 4(4):421-9 PMID: 25006755
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EGFR 抑制剂
BIBW2992 (Afatinib)是酪氨酸激酶抑制剂（TKI），它不可逆地抑制人表皮生长因子受体2（Her2）和表皮生长因子受体（EGFR）激酶。
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- Aya Hasan Alshammari, .et al. Discrimination of hand-foot skin reaction caused by tyrosine kinase inhibitors based on direct keratinocyte toxicity and vascular endothelial growth factor receptor-2 inhibition, Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Van Sebille YZ, .et al. Use of zebrafish to model chemotherapy and targeted therapy gastrointestinal toxicity, Exp Biol Med (Maywood), 2019, Jun 11:1535370219855334 PMID: 31184924
- Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
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pan-EGFR/pan-erbB 抑制剂
AZD8931 (Sapitinib)是ErbB1，ErbB2和ErbB3受体信号传导的等效抑制剂。
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- Takeshi Ito, .et al. Mathematical analysis of gefitinib resistance of lung adenocarcinoma caused by MET amplification, Biochem Biophys Res Commun, 2019, in Press
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EGFR 抑制剂
WZ4002是一种新型的，突变选择性EGFR抑制剂，作用于EGFR(L858R)/(T790M)，在BaF3细胞系中IC50为2 nM/8 nM；对ERBB2磷酸化(T798I)没有抑制作用。
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EGFR 抑制剂
Gefitinib (Iressa)是一种EGFR抑制剂，可阻断靶细胞中表皮生长因子受体(EGFR)的信号传导。
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- Hamzehlou S, .et al. Anti-tumor activity of neratinib, a pan-HER inhibitor, in gastric adenocarcinoma cells, Eur J Pharmacol, 2019, Nov 15;863:172705 PMID: 31574259
- Mansi Srivastava, .et al. Inhibition of the TIRAP-c-Jun interaction as a therapeutic strategy for AP1-mediated inflammatory responses, Int Immunopharmacol, 2019, 71: 188-197 PMID: 30909134
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EGFR 抑制剂
Erlotinib hydrochloride是一种可逆的酪氨酸激酶抑制剂，作用于表皮生长因子受体（EGFR）。
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- Yuta Yamamoto, .et al. Quantitative determination of erlotinib in human serum using competitive enzyme-linked immunosorbent assay, J Pharm Anal, 2018, Apr; 8(2): 119-123 PMID: 29736298
- Aikawa S, .et al. Proliferation of mouse endometrial stromal cells in culture is highly sensitive to lysophosphatidic acid signaling, Biochem Biophys Res Commun, 2017, Feb 26;484(1):202-208 PMID: 28073697
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HER2 抑制剂
Lapatinib是一种双重酪氨酸激酶抑制剂，可阻断HER2生长受体途径。
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EGFR 抑制剂
AG-1478 (Tyrphostin AG-1478)是EGFR激酶的抑制剂，IC50值为3 nM。
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- Khattab M, .et al. Conformational Plasticity in Tyrosine Kinase Inhibitor-Kinase Interactions Revealed with Fluorescence Spectroscopy and Theoretical Calculations, J Phys Chem B, 2018, May 3;122(17):4667-4679 PMID: 29629773
- Muhammad Khattab, .et al. A pH-induced conformational switch in a tyrosine kinase inhibitor identified by electronic spectroscopy and quantum chemical calculations, Sci Rep, 2017, 7: 16271 PMID: 29176733
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EGFR 抑制剂
OSI-420 (Desmethyl Erlotinib,CP-473420)是一种口服活性EGFR酪氨酸激酶抑制剂，可通过抑制细胞间结构域来抑制受体酪氨酸激酶（TKs）。
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- Yuta Yamamoto, .et al. Quantitative determination of erlotinib in human serum using competitive enzyme-linked immunosorbent assay, J Pharm Anal, 2018, Apr; 8(2): 119-123 PMID: 29736298
- Janet L. Martin, .et al. Inhibition of basal-like breast cancer growth by FTY720 in combination with epidermal growth factor receptor kinase blockade, Breast Cancer Res, 2017, 19: 90 PMID: 28778177
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HDAC 抑制剂
CUDC-101是一种抑制多种靶标的新型化合物，旨在抑制HDAC，EGFR和Her2。
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EGFR 抑制剂
WZ8040是一种新型的EGFR抑制剂，可抑制含有EGFR-T790M的细胞系的生长并抑制EGFR磷酸化。
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EGFR 抑制剂
WZ3146是EGFR受体激酶突变体的抑制剂，该突变体在活性位点网守残基（T790M）中带有突变，并且对野生型EGFR激酶的效力要低得多。
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EGFR 抑制剂
PD153035 (HCl salt)是EGFR酪氨酸激酶活性的极其有效和特异的抑制剂。
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HER2/ErbB2 抑制剂
CP-724714是一种有效的，选择性HER2/ErbB2抑制剂，可抑制HER2激酶（IC50 3.8 ng/ml）。
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- Yu Muta, .et al. Composite regulation of ERK activity dynamics underlying tumour-specific traits in the intestine, Nat Commun, 2018, 9: 2174 PMID: 29872037
- Gina M. Sizemore, .et al. Stromal PTEN determines mammary epithelial response to radiotherapy, Nat Commun, 2018, 9: 2783 PMID: 30018330
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EGFR 抑制剂
BMS 599626 (AC480)是一种选择性的，高效效的HER1，HER2和HER4酪氨酸激酶抑制剂（IC50分别为22、32和190 nM），具有潜在的抗肿瘤活性。
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HER2 抑制剂
Arry-380 analog是一种ErbB-2抑制剂，可选择性结合并抑制ErbB-2的磷酸化，从而导致表达ErbB-2的肿瘤细胞的生长抑制和死亡。
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EGFR 抑制剂
AV-412是一种EGFR / HER2抑制剂，可与表皮生长因子受体（EGFR）和人表皮生长因子受体2（HER2）结合并抑制其生长，这可能会导致肿瘤生长和血管生成受到抑制。
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- Le Zhang, .et al. High-throughput drug library screening identifies colchicine as a thyroid cancer inhibitor, Oncotarget, 2016, Apr 12; 7(15): 19948-19959 PMID: 26942566
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EGFR 抑制剂
AG 490是EGF受体酪氨酸激酶的选择性抑制剂 (EGFR和ErbB2的IC50值分别为2和13.5μM)。也抑制对Lck，Lyn，Btk，Syk和Src无活性的JAK2。
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- Matozaki M, .et al. Involvement of Stat3 phosphorylation in mild heat shock-induced thermotolerance, Exp Cell Res, 2019, Feb 15. pii: S0014-4827(18)31030-9 PMID: 30776355
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EGFR 抑制剂
AEE788是一种口服生物可用的多受体酪氨酸激酶抑制剂，可抑制EGFR，HER2和VEGF2酪氨酸激酶的磷酸化。
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EGFR 抑制剂
Chrysophanic acid (Chrysophanol)是通过抑制EGFR/mTOR通路来阻止结肠癌细胞的增殖。
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EGFR 抑制剂
PF299804是一种有效的，可口服的酪氨酸激酶人表皮生长因子受体（HER）1（EGFR），HER2和HER4不可逆抑制剂。
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- Aya Hasan Alshammari, .et al. Discrimination of hand-foot skin reaction caused by tyrosine kinase inhibitors based on direct keratinocyte toxicity and vascular endothelial growth factor receptor-2 inhibition, Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Hamzehlou S, .et al. Anti-tumor activity of neratinib, a pan-HER inhibitor, in gastric adenocarcinoma cells, Eur J Pharmacol, 2019, Nov 15;863:172705 PMID: 31574259
- Momeny M, .et al. The ERBB receptor inhibitor dacomitinib suppresses proliferation and invasion of pancreatic ductal adenocarcinoma cells, Cell Oncol (Dordr), 2019, Apr 25 PMID: 31025257
- Majid Momeny, .et al. Dacomitinib, a pan-inhibitor of ErbB receptors, suppresses growth and invasive capacity of chemoresistant ovarian carcinoma cells, Sci Rep, 2017, 7: 4204 PMID: 28646172
- Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
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EGFR, HER2 and VEGFR 抑制剂
XL647 (Tesevatinib)是一种口服生物可利用的小分子RTK抑制剂，可结合并抑制在肿瘤细胞增殖和肿瘤血管形成中起主要作用的几种酪氨酸受体激酶，包括EGFR，HER2，ERBB2，VEGFR和EphB4。
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EGFR 抑制剂
AST-1306是一种新型的苯胺-喹唑啉化合物，在无细胞和基于细胞的系统中均抑制野生型表皮生长因子受体（EGFR）和ErbB2以及EGFR抗性突变体的酶活性。
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EGFR, PKA,PKC 抑制剂
Daphnetin是一种香豆素类似物，可作为几种蛋白激酶的抑制剂。它在体外抑制EGFR激酶（IC50 = 7.67 ?M），PKA（IC50 = 9.33 ?M）和PKC（IC50 = 25 ?M）。蜂胶对EGFR激酶的抑制作用与ATP竞争，对肽底物没有竞争性。还可以用作有效的抗氧化剂和抗疟疾剂。
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HER2/ErbB2 抑制剂
Mubritinib (TAK 165)是一种有效的EGFR和p34cdc2抑制剂，IC50分别为6 nM和0.2 ?M。Mubritinib（TAK 165）也抑制p33cdk2和p33cdk5。
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EGFR 抑制剂
ARRY334543 (Varlitinib)是一种有效的EGFR和ErbB-2口服活性小分子抑制剂。
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- Hamzehlou S, .et al. Anti-tumor activity of neratinib, a pan-HER inhibitor, in gastric adenocarcinoma cells, Eur J Pharmacol, 2019, Nov 15;863:172705 PMID: 31574259
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Genistin (Genistoside)是一种异黄酮，存在于许多饮食植物中，如大豆和葛根。显示出刺激体内雌激素依赖性乳腺癌细胞生长。
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- Azuma T, .et al. Distribution of six anticancer drugs and a variety of other pharmaceuticals, and their sorption onto sediments, in an urban Japanese river, Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. Detection of pharmaceuticals and phytochemicals together with their metabolites in hospital effluents in Japan, and their contribution to sewage treatment plant influents, Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
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VEGFR/EGFR 抑制剂
BMS-690514是一种有效的选择性表皮生长因子受体（EGFR），HER2和HER4抑制剂，以及VEGF受体激酶。
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HER2/EGFR 抑制剂
TAK-285是一种研究性的HER2/EGFR抑制剂，可在具有完整血脑屏障 (BBB) 的大鼠中穿透CNS。TAK-285对HER2和EGFR激酶具有抑制活性，HER2和EGFR的IC50值分别为17 nmol/L (95％CI 12-24)和23 nmol/L (95％CI 18-30)。
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EGFR 抑制剂
AST-6是表皮生长因子受体1和2的新型不可逆抑制剂，可在体内外抑制肿瘤生长。
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HER2 抑制剂
Tyrphostin AG 879是神经生长因子（NGF）TrkA酪氨酸激酶活性的抑制剂。
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Lapatinib (free base)是一种双重酪氨酸激酶抑制剂，是一种有效的EGFR和ErbB2抑制剂，在无细胞试验中IC50分别为10.2和9.8 nM。可阻断HER2生长受体途径。
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- Aya Hasan Alshammari, .et al. Discrimination of hand-foot skin reaction caused by tyrosine kinase inhibitors based on direct keratinocyte toxicity and vascular endothelial growth factor receptor-2 inhibition, Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Hamzehlou S, .et al. Anti-tumor activity of neratinib, a pan-HER inhibitor, in gastric adenocarcinoma cells, Eur J Pharmacol, 2019, Nov 15;863:172705 PMID: 31574259
- Momeny M, .et al. The ERBB receptor inhibitor dacomitinib suppresses proliferation and invasion of pancreatic ductal adenocarcinoma cells, Cell Oncol (Dordr), 2019, Apr 25 PMID: 31025257
- Tzeng SF, .et al. O-Glycosylation-mediated signaling circuit drives metastatic castration-resistant prostate cancer, FASEB J, 2018, Jun 15:fj201800687 PMID: 29906246
- Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
- Yuki Kawasaki, .et al. Feedback control of ErbB2 via ERK-mediated phosphorylation of a conserved threonine in the juxtamembrane domain, Sci Rep, 2016, 6: 31502 PMID: 27531070
- Tetsuya Saita, .et al. Preparation of Antibodies and Development of an Enzyme-Linked Immunosorbent Assay for the Tyrosine Kinase Inhibitors Lapatinib and Nilotinib., Biol Pharm Bull. , 2015, 38(10):1652-7 PMID: 26424026
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EGFR 抑制剂
BIBX 1382是一种细胞可渗透的嘧啶嘧啶化合物，可作为一种有效的，可逆的，ATP竞争性高选择性的EGFR抑制剂。
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EGFR 抑制剂
AG-17是人表皮样癌细胞系A431中EGFR激酶的抑制剂，IC50值为460 μM，作用于PDGFR更有效，IC50值为0.5μM。
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Butein是一种植物多酚，用作特定的蛋白酪氨酸激酶抑制剂。
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VEGFR/FGFR/EGFR 抑制剂?
SU-5402是有效且选择性的血管内皮生长因子受体(VEGFR)和成纤维细胞生长因子受体(FGFR)抑制剂(在VEGFR2, FGFR1, PDGFRβ和EGFR处IC50值分别为0.02、0.03、0.51和> 100μM)。
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PKC 抑制剂
PKC 412 (Midostaurin)是一种广谱蛋白激酶抑制剂。抑制常规PKC亚型α/β/γ，PDFRβ，VEGFR2，Syk，Flk-1，Flt3，Cdk1/B，PKA，c-Kit，c-Fgr，c-Src，VEGFR1和EGFR。显示有效的抗肿瘤活性。
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EGFR 抑制剂
CGP-52411是表皮生长因子受体（EGFR）的选择性抑制剂（体外IC50 = 0.3μM）。还抑制和逆转与阿尔茨海默氏病有关的Aβ42纤维的形成。
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ErbB 抑制剂
ARRY-543 (Varlitinib,ASLAN001)是一种新型口服ErbB家族抑制剂，与批准的ErbB抑制剂不同，它直接或间接靶向ErbB家族的所有成员，包括ErbB3，在治疗通过多个ErbB家族成员发出信号的肿瘤方面具有潜在优势。
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EGFR 抑制剂
CO-1686是一种新型的口服靶向共价（不可逆）抑制剂，可抑制表皮生长因子受体（EGFR）的致癌突变形式，目前正在研究用于治疗非小细胞肺癌（NSCLC）。
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EGFR 抑制剂
Icotinib hydrochloride是一种有效的特异性表皮生长因子受体（EGFR）酪氨酸激酶抑制剂（TKI），IC（50）为5 nM，包括EGFR（L858R），EGFR（L861Q），EGFR（T790M）和EGFR的突变体（T790M，L858R）。
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EGFR 抑制剂
AZD-9291 (Osimertinib)是第三代EGFR抑制剂，在临床前研究中显示出希望，并为已对现有EGFR抑制剂产生耐药性的晚期肺癌患者提供了希望。
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- Liu YN, .et al. Acquired resistance to EGFR tyrosine kinase inhibitors is mediated by the reactivation of STC2/JUN/AXL signaling in lung cancer, Int J Cancer, 2019, Jun 4 PMID: 31162839
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EGFR 抑制剂
Tyrphostin AG 183抑制EGFR（表皮生长因子受体）酪氨酸激酶（IC50 = 800 nM）。
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EGFR 抑制剂
CNX-2006是一种有效的突变体选择性EGFR抑制剂，在具有激活性EGFR突变的细胞以及具有T790M突变的细胞中具有出色的体外活性。CNX-2006是CO-1686的原型，目前正在I期临床试验中，用于治疗EGFR突变型肺癌。
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EGFR 抑制剂
Icotinib是一种有效的特异性EGFR抑制剂，IC50为5 nM，包括EGFR，EGFR（L858R），EGFR（L861Q），EGFR（T790M）和EGFR（T790M，L858R）。
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(-)-Gallocatechin具有清除自由基的能力。它抑制牙龈卟啉单胞菌在颊上皮细胞上的生长和粘附。
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JAK3 抑制剂
WHI-P 154是一种JAK3抑制剂，IC50 = 1.8uM。WHI-P 154还在体外抑制巨噬细胞中的STAT1激活，iNOS表达和NO生成。
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