EGFR
信号通路图
研究领域
- 抑制剂选择性比较
- 溶解性比较
| 目录号 | 产品目录 | 溶解度(25°C) | ||
|---|---|---|---|---|
| 水 | DMSO | 酒精 | ||
| S1023 | Erlotinib HCl (OSI-744) | <1 mg/mL | 4 mg/mL | <1 mg/mL |
| S1025 | Gefitinib (ZD1839) | <1 mg/mL | 89 mg/mL | 4 mg/mL |
| S1028 | Lapatinib (GW-572016) Ditosylate | <1 mg/mL | 100 mg/mL | <1 mg/mL |
| S1011 | Afatinib (BIBW2992) | <1 mg/mL | 97 mg/mL | 15 mg/mL |
| S2150 | Neratinib (HKI-272) | <1 mg/mL | 5 mg/mL | <1 mg/mL |
| S8741 | Avitinib (AC0010) | <1 mg/mL | 97 mg/mL | 97 mg/mL |
| S5098 | Gefitinib hydrochloride | 1 mg/mL | 8 mg/mL | 1 mg/mL |
| S3759 | Norcantharidin | -1 mg/mL | 33 mg/mL | -1 mg/mL |
| S1019 | Canertinib (CI-1033) | <1 mg/mL | 2 mg/mL | 9 mg/mL |
| S2111 | Lapatinib | <1 mg/mL | 100 mg/mL | <1 mg/mL |
| S1143 | AG-490 (Tyrphostin B42) | <1 mg/mL | 58 mg/mL | 6 mg/mL |
| S1167 | CP-724714 | <1 mg/mL | 94 mg/mL | 94 mg/mL |
| S2727 | Dacomitinib (PF299804, PF299) | <1 mg/mL | 19 mg/mL | <1 mg/mL |
| S1173 | WZ4002 | <1 mg/mL | 13 mg/mL | <1 mg/mL |
| S2192 | Sapitinib (AZD8931) | <1 mg/mL | 40 mg/mL | <1 mg/mL |
| S1194 | CUDC-101 | <1 mg/mL | 20 mg/mL | <1 mg/mL |
| S2728 | AG-1478 (Tyrphostin AG-1478) | <1 mg/mL | 25 mg/mL | 13 mg/mL |
| S1079 | PD153035 HCl | <1 mg/mL | 0.5 mg/mL | <1 mg/mL |
| S1392 | Pelitinib (EKB-569) | <1 mg/mL | 13 mg/mL | <1 mg/mL |
| S1056 | AC480 (BMS-599626) | <1 mg/mL | 113 mg/mL | 20 mg/mL |
| S1486 | AEE788 (NVP-AEE788) | <1 mg/mL | 88 mg/mL | <1 mg/mL |
| S7000 | AP26113-analog (ALK-IN-1) | <1 mg/mL | 45 mg/mL | 106 mg/mL |
| S2205 | OSI-420 | <1 mg/mL | 83 mg/mL | <1 mg/mL |
| S1170 | WZ3146 | <1 mg/mL | 93 mg/mL | <1 mg/mL |
| S2752 | HER2-Inhibitor-1 | <1 mg/mL | 100 mg/mL | 3 mg/mL |
| S1179 | WZ8040 | <1 mg/mL | 96 mg/mL | 3 mg/mL |
| S2185 | AST-1306 | <1 mg/mL | 124 mg/mL | <1 mg/mL |
| S7284 | Rociletinib (CO-1686, AVL-301) | <1 mg/mL | 100 mg/mL | <1 mg/mL |
| S1342 | Genistein | <1 mg/mL | 54 mg/mL | 2 mg/mL |
| S2755 | Varlitinib | <1 mg/mL | 6 mg/mL | <1 mg/mL |
| S2922 | Icotinib | <1 mg/mL | 78 mg/mL | 7 mg/mL |
| S2784 | TAK-285 | <1 mg/mL | 110 mg/mL | 54 mg/mL |
| S2867 | WHI-P154 | <1 mg/mL | 75 mg/mL | <1 mg/mL |
| S2554 | Daphnetin | <1 mg/mL | 35 mg/mL | <1 mg/mL |
| S7039 | PD168393 | <1 mg/mL | 73 mg/mL | <1 mg/mL |
| S2895 | Tyrphostin 9 | <1 mg/mL | 56 mg/mL | 56 mg/mL |
| S7206 | CNX-2006 | <1 mg/mL | 100 mg/mL | 29 mg/mL |
| S8009 | AG-18 | <1 mg/mL | 37 mg/mL | 37 mg/mL |
| S7298 | AZ5104 | <1 mg/mL | 97 mg/mL | 23 mg/mL |
| S7297 | Osimertinib (AZD9291) | <1 mg/mL | 99 mg/mL | 43 mg/mL |
| S7557 | CL-387785 (EKI-785) | <1 mg/mL | 63 mg/mL | <1 mg/mL |
| S8294 | Olmutinib (HM61713, BI 1482694) | <1 mg/mL | 97 mg/mL | 23 mg/mL |
| S2250 | (-)-Epigallocatechin Gallate | 23 mg/mL | 72 mg/mL | 83 mg/mL |
| S7786 | Erlotinib | <1 mg/mL | 78 mg/mL | 15 mg/mL |
| S7810 | Afatinib (BIBW2992) Dimaleate | <1 mg/mL | 100 mg/mL | <1 mg/mL |
| S7971 | AZD3759 | <1 mg/mL | 91 mg/mL | 20 mg/mL |
| S7358 | Poziotinib (HM781-36B) | <1 mg/mL | 98 mg/mL | <1 mg/mL |
| S8229 | Brigatinib (AP26113) | <1 mg/mL | 1 mg/mL | 43 mg/mL |
| S8412 | Naquotinib(ASP8273) | <1 mg/mL | 52 mg/mL | 100 mg/mL |
| S2406 | Chrysophanic Acid | <1 mg/mL | 5 mg/mL | <1 mg/mL |
| S7824 | Nazartinib (EGF816, NVS-816) | <1 mg/mL | 99 mg/mL | 99 mg/mL |
| S7926 | Lifirafenib (BGB-283) | <1 mg/mL | 95 mg/mL | 95 mg/mL |
| S4667 | Lidocaine hydrochloride | 54 mg/mL | 54 mg/mL | 54 mg/mL |
| S8036 | Butein | <1 mg/mL | 55 mg/mL | 55 mg/mL |
| S8242 | EAI045 | <1 mg/mL | 76 mg/mL | <1 mg/mL |
| S8312 | NSC228155 | <1 mg/mL | 15 mg/mL | <1 mg/mL |
- EGFR抑制剂（57）
- 新EGFR产品
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| A2000 |
CetuximabCetuximab是一种新型的分子靶向药物，是EGFR的抑制剂，同时也是人源EGFR单克隆抗体，与EGFR的胞外结合区域相互作用并抑制其受配体刺激；MW：145.781 KD。 |
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| S1023 |
Erlotinib HCl (OSI-744)Erlotinib HCl (OSI-744)是一种EGFR抑制剂，在无细胞试验中IC50为2 nM，对EGFR的选择性比对人c-Src或v-Abl高1000多倍。 |
Erlotinib IC50 in HCC827 cell lines measured 48h after treatment with vehicle (control) or with erlotinib. Erlotinib IC50 is shown in parentheses. Data are representative of 3 independent experiments. Effects of treatment for 48h with a vehicle or the indicated doses of MP-470 in parental or ER1 and ER2 cell lines in the absence and presence of erlotinib on the indicated biomarkers. |
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| S1025 |
Gefitinib (ZD1839)Gefitinib (ZD1839)是一种EGFR抑制剂，作用于NR6wtEGFR和NR6W细胞中的Tyr1173，Tyr992，Tyr1173和Tyr992，IC50 分别为37 nM，37nM，26 nM和57 nM。 |
c, HCC4006 lung cancer cells that have acquired a high-mesenchymal state concomitant with becoming resistant to gefitinib (red curve) exhibit increased sensitivity to GPX4 inhibition.
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| S1028 |
Lapatinib (GW-572016) DitosylateLapatinib (GW-572016) Ditosylate是一种有效的EGFR 和 ErbB2抑制剂，在无细胞试验中IC50分别为10.8和9.2 nM。 |
Combination of NVP-AEW541 and lapatinib cooperatively inhibits the growth of NVP-AEW541 resistant murine rhabdomyosarcoma primary cell cultures with Igf1r/Her2 complexes. Cell viability assay for Naïve, untreated (U20325; A) and NVP-AEW541 innately resistant mouse rhabdomyosarcoma primary culture (U44676; B) treated with varying concentrations of NVP-AEW541, lapatinib, or a combination of both. Naïve cells (U20325) were sensitive to NVP-AEW541, but lapatinib had no cooperativity. In contrast, NVP-AEW541 at moderate doses increased cell growth in resistant cell cultures (U44676). However, this paradoxical effect was reduced by the addition of lapatinib, although lapatinib treatment alone had very little effect. C, the NVP-AEW541 resistant primary tumor cell line (U44676) was treated with DMSO, 5 μmol/L lapatinib, 5 μmol/L NVP-AEW541, and a combination of 5 μmol/L NVP-AEW541+lapatinib for 25 minutes and Western blot analysis was done on lysates for p-Igf1r and p-Her2. |
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| S1011 |
Afatinib (BIBW2992)Afatinib (BIBW2992)不可逆地抑制EGFR/ErbB，包括EGFR(wt)，EGFR(L858R)，EGFR(L858R/T790M)，ErbB2（HER2）和ErbB4（HER4），在无细胞试验中IC50分别为0.5 nM，0.4 nM，10 nM，14 nM和1 nM。 |
Cytoxicity of irreversible EGFR TKIS and ethacrynic acid on breast cells lines. A, Mean IC50 value of Afatinib.
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| S2150 |
Neratinib (HKI-272)Neratinib (HKI-272)是一种高度选择性的HER2和EGFR抑制剂，在无细胞试验中IC50分别为59 nM 和 92 nM；微弱抑制KDR和Src，对Akt，CDK1/2/4，IKK-2，MK-2，PDK1，c-Raf和c-Met没有显著的抑制作用。Phase 3。 |
Differential sensitivity of EGFR-mutant glioma and lung cancer cell lines to the irreversible EGFR inhibitors HKI-272 and CI-1033. C, HKI-272 is more potent than CI-1033 in blocking EGFR phosphorylation in SKMG3 cells with EGFR EC mutation. SKMG3 cells were treated with the indicated doses of CI-1033 or HKI-272, and whole lysates were analyzed by immunoblot with the indicated antibodies.
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| S8741New |
Avitinib (AC0010)Avitinib (AC0010) is a pyrrolopyrimidine-based irreversible EGFR inhibitor that is mutation-selective with IC50 value of 0.18 nM against EGFR L858R/T790M double mutations, nearly 43-fold greater potency over wild-type EGFR (IC50 value, 7.68 nM). It has comparable anti-tumor activity and tolerated toxicity. |
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| S5098New |
Gefitinib hydrochlorideGefitinib is an EGFR inhibitor with IC50s of 15.5 nM and 823.3 nM for WT EGFR and EGFR (858R/T790M), respectively. |
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| S3759New |
NorcantharidinNorcantharidin is a synthetic anticancer compound which is a dual inhibitor for c-Met and EGFR in human colon cancers. |
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| S1019 |
Canertinib (CI-1033)Canertinib (CI-1033)是一种泛ErbB抑制剂，作用于EGFR和ErbB2，IC50分别为1.5 nM和9.0 nM，但对PDGFR，FGFR，InsR，PKC，和CDK1/2/4等均无抑制活性。Phase 3。 |
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| S2111 |
LapatinibLapatinib，以 Lapatinib Ditosylate的形式使用，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。 |
Sensitivity to the ErbB1/ErbB2 inhibitor lapatinib is highest for cancer cells from late-stage tumors in culture (mean ± SEM, p = 0.04 or 0.02 as indicated, Student’s t test; values represent the averages of four experiments, each done in triplicate with primary cells from independent mice). |
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| S1143 |
AG-490 (Tyrphostin B42)AG-490 (Tyrphostin B42)是一种EGFR抑制剂，在无细胞试验中IC50为0.1 μM，作用于EGFR比作用于ErbB2选择性高135倍，对JAK2也有抑制作用，对Lck，Lyn，Btk，Syk和Src没有抑制活性。 |
Increased expression of VEGF and p-STAT3 induced by CXCL1 was blocked by either AG490 or SB225022 in AGS cells.
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| S1167 |
CP-724714CP-724714是一种有效的，选择性HER2/ErbB2抑制剂，IC50为10 nM，无细胞试验中比作用于EGFR，InsR，IRG-1R，PDGFR，VEGFR2，Abl，Src，c-Met等选择性高640多倍。Phase 2。 |
For MTT assays, cells (2,000 ~ 5,000 cells/well) were subcultured into 96-well plates according to their growth properties. Cell proliferation was assayed at 72 hr after treatment of CP-724714 by adding 20 μl of 5 mg/ml 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) solution per 100 μl of growth medium. After incubating for 3-4 h at 37°C, the media were removed and 150 µl/well of MTT solvent (either absolute DMSO or isopropanol containing 4 μM HCl and 0.1% Nonidet-40) was added to dissolve the formazan. |
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| S2727 |
Dacomitinib (PF299804, PF299)Dacomitinib (PF299804, PF299)是一种有效的，不可逆的泛ErbB抑制剂，最有效作用于EGFR，无细胞试验中IC50为6 nM，高效作用于携带EGFR或ERBB2突变型(耐Gefitinib)和携带EGFR T790M突变型的NSCLCs。Phase 2。 |
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| S1173 |
WZ4002WZ4002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。 |
Antitum o r activity of WZ4002 and/or E7050 in mouse xenograft models of human tumors. SCID mice-bearing PC-9/Vec (A), PC-9/HGF#5 (B), H1975 (C), or HCC827ER (D) tumors were administered 25 mg/kg WZ4002 and/or E7050 once daily for 14 to 21 days. Tumor volume was measured using calipers on the indicated days. Mean?SE tumor volumes are shown for groups of 4 to 5 mice. |
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| S2192 |
Sapitinib (AZD8931)Sapitinib (AZD8931)是一种可逆的，ATP竞争性EGFR，ErbB2和ErbB3抑制剂，无细胞试验中IC50分别为4 nM，3 nM和4 nM，作用于NSCLC细胞比Gefitinib或Lapatinib更有效，作用于ErbB家族比作用于MNK1和Flt选择性强100倍。Phase 2。 |
Western blot analysis confirm suppression of the biomarker p-EGFR upon treatment with EGFR TKIs in U-CH1 and UM-Chor1. Cells were serum-starved overnight before they were treated with a range of concentrations of the EGFR inhibitors for 4 h and then EGF-spiked (50 ng/ml) for 15 min. Endogenous controls (non-serum-starved, non-EGF-spiked), untreated controls (serum-starved, non-EGF-spiked) and vehicle controls (serum-starved, treated with 2.5% DMSO, EGF-spiked) were included. Phospho-EGFR was measured by western blot.
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| S1194 |
CUDC-101CUDC-101是一种有效的，多靶点抑制剂，作用于HDAC，EGFR和HER2，IC50分别为4.4 nM， 2.4 nM，和15.7 nM，且抑制I/II型HDACs，但是对III型， Sir-type HDACs没有抑制作用。Phase 1。 |
(a) Decay-corrected microPET/CT scan of MDA-MB-231 tumor bearing mice (n = 4) at 2, 4, and 24 h after i.v. injection of [64Cu]7. The image obtained with coinjection of CUDC-101 (20 mg/kg body weight) is shown for a 24 h blockade. Tumors are indicated by arrows. (b) Decay-corrected region-of interest (ROI) analysis on microPET images of the tumor uptake of [64Cu]7 with or without coinjection of CUDC-101 (20 mg/kg body weight). *, P < 0.05; **, P < 0.01.
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| S2728 |
AG-1478 (Tyrphostin AG-1478)AG-1478 (Tyrphostin AG-1478)是一种选择性EGFR抑制剂，在无细胞试验中IC50为3 nM，对HER2-Neu，PDGFR，Trk，Bcr-Abl和InsR几乎没有作用活性。 |
A549 cells were treated with G15 (a specific antagonist of GPR30, 1 uM), AG1478 (a potent antagonist of EGFR, 10 uM), BPA (10-5 M) alone for 15 min or BPA after a 90-min pretreatment with G15 or AG1478 for 15 min. Then the expression of p-ERK1/2 and total ERK1/2 were measured by western blot analysis.
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| S1079 |
PD153035 HClPD153035 HCl是一种有效的，特异性EGFR抑制剂，无细胞试验中Ki和IC50分别为5.2 pM和29 pM；对PGDFR， FGFR， CSF-1， InsR和Src几乎无作用。 |
B. Increased of cell migration induced by EGF is inhibited by a selective ATP competitive inhibitor of EGFR (PD153035). Histograms showing HCT-116 cell migration with or without treatment by EGF +/− PD153035. Results are expressed as mean ± SEM. ***p<0.001, sample significantly different from control (N=3, n=7, Kruskal-Wallis test).
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| S1392 |
Pelitinib (EKB-569)Pelitinib (EKB-569)是一种有效的，不可逆EGFR抑制剂，IC50为38.5 nM。Phase2。 |
IGF-1 and IL-1β mediated induction of Bcl-2 expression involves EGFR. (A) Bcl-2 mRNA levels in AALEBs treated with IGF-1 or IL-1β in the presence or absence of two EGFR tyrosine kinase inhibitors, EKB-569 (1 μM) or PD153035 (1 μM). |
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| S1056 |
AC480 (BMS-599626)AC480 (BMS-599626)是一种选择性的，高效效的HER1和HER2抑制剂，IC50分别为20 nM和30 nM。比对HER4效果强8倍左右，而比对VEGFR2， c-Kit， Lck， MET等的作用强100倍以上。Phase 1。 |
RCH-ACV cells were treated with ponatinib(50 nM), PCI-32765(50 nM), or BMS-599626(500 nM) over a time course, and whole-cell extracts were subjected to immunoblot analysis
for total or phospho-AKT.
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| S1486 |
AEE788 (NVP-AEE788)AEE788 (NVP-AEE788)是一种有效的EGFR和HER2/ErbB2抑制剂，IC50分别为2 nM和6 nM，对VEGFR2/KDR， c-Abl， c-Src，和Flt-1作用效果稍弱，对Ins-R， IGF-1R， PKCα和CDK1没有抑制作用。Phase 1/2。 |
EGFR-SGLT1 interaction is irresponsive to modulators of EGFR’s tyrosine kinase. A: Immunoprecipitation coupled Western blot analysis ofinteractionsbetween EGFR-HA and SGLT1-FlaginHEK293 cells treatedwith EGF or AEE788. EGFR, total EGFR; pEGFR, phosphorylated EGFR; IP, immunoprecipitation; IB, immunoblot. Input, expression levels of indicated exogenous proteinsin HEK293 whole celllysates used for the IP. |
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| S7000 |
AP26113-analog (ALK-IN-1)AP26113-analog (ALK-IN-1) 是AP26113的类似物，是有效的、选择性的ALK抑制剂，同时也是EGFR的抑制剂。 |
Several ALK inhibitors effectively inhibit the growth of CD74–ROS1–addicted Ba/F3 cells. A, Ba/F3 cells expressing CD74–ROS1 (clone #6) were seeded in 96-well plates and treated with the indicated concentration of crizotinib, ceritinib, AP26113, ASP3026, or alectinib for 72 hours. Cell viability was analyzed using the CellTiter-Glo Assay. B, IC50 values (nmol/L) of Ba/F3 cell lines expressing CD74–ROS1 (clone #6) against various ALK inhibitors are shown. Average IC50 values against crizotinib, ceritinib, or AP26113 were calculated from the three independent experiments. IC50 values against ASP3026 and alectinib were calculated from the single experiment. C, inhibition of phospho-ROS1 by various ALK inhibitors in Ba/F3 models. CD74–ROS1–expressing Ba/F3 cells were exposed to increasing concentrations of crizotinib, ceritinib, AP26113, ASP3026, or alectinib for 3 hours. Cell lysates were immunoblotted to detect the indicated proteins. |
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| S2205 |
OSI-420OSI-420是Erlotinib的活性代谢产物(是一种EGFR抑制剂，IC50为2 nM)。 |
Mean plasma concentration vs. time after single-dose oral administration of CCB and ERT in six Wistar rats. |
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| S1170 |
WZ3146WZ3146是一种突变选择性的，不可逆EGFR(L858R)和EGFR(E746_A750)抑制剂，IC50分别为2 nM和2 nM；对ERBB2磷酸化(T798I)没有抑制作用。 |
T47D cells were pretreated with 100ng/ml EGF for 20 min and then treated with the indicated concentrations of WZ3146 for 24 hours.
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| S2752 |
HER2-Inhibitor-1HER2-Inhibitor-1是ARRY-380的类似物。ARRY-380是一种有效的，选择性的HER2抑制剂，IC50为8 nM，等效作用于截短的p95-HER2，作用于HER2比作用于EGFR选择性高500倍。 |
confluent 10cm plates, 24hour FBS starvation, then treatment with compounds at 10nM for 30mins, followed by 5 minutes of 0.05ug/ml of EGF. Pellet was sonicated (setting 5, 5 seconds, twice), then quenched with 2XGSB. Loaded 10ul on AnyKD BioRad gel (20mins at 250V), transfered with BioRad Turbo system for 15 minutes (1.5A, 25V). Blocked with 5% milk for 1 hour at RT. Rocked overnight at 1:1000 in 5% BSA with primary Abs; Anti-rabbit secondary Ab at 1:2000 in 5% milk for 1 hour, developed with Thermo Femto Kit. |
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| S1179 |
WZ8040WZ8040是一种新型的，突变选择性的，不可逆的EGFRT790M抑制剂，对ERBB2磷酸化(T798I)没有抑制作用。 |
After starved in serum-free medium for 24h,A549 cells incubated with the indicated concentrations of WZ8040 for 3h,followed by 20-minute stimolation of 100ng/ml EGF. |
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| S2185 |
AST-1306AST-1306是一种新型，不可逆的EGFR和ErbB2抑制剂，IC50分别为0.5 nM和3 nM，对突变型EGFR T790M/L858R也有效，作用于过表达ErbB2的细胞更有效，作用于ErbB家族比作用于其他激酶选择性高3000倍。 |
Reversal effect of AST-1306 on the sensitivity of NCI-H460/MX20 cells to mitoxantrone. The figure showes the survival curves of cells at different concentrations of mitoxantrone with or without AST-1306. Cell viability was determined by MTT Assay. NCI-H460 is lung cancer cell line while NCI-H460/MX20 is ABCG2 overexpressing drug (mitoxantrone) selected cell line. |
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| S7284 |
Rociletinib (CO-1686, AVL-301)Rociletinib (CO-1686, AVL-301)是一种不可逆的，选择性抑制突变型EGFR，在无细胞试验中作用于EGFRL858R/T790M和EGFRWT， Ki分别为21.5 nM和303.3 nM。Phase 2。 |
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Immunohistochemical studies reveal the tumor cells to be negative for chromogranin and synaptophysin pre-rociletinib and positive for both neuroendocrine markers in the post-rociletinib liver biopsy. The results, in conjunction with the morphology, are consistent with the diagnosis of small cell carcinoma in the rociletinib-resistant specimen. H&E, hematoxylin and eosin.
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| S1342 |
GenisteinGenistein是一种来源于大豆的植物雌激素，是一种高特异性的蛋白酪氨酸激酶(PTK) 的抑制剂，在NIH-3T3细胞中通过EGF或者胰岛素介导而抑制有丝分裂，IC50分别为12μM和19 μM。 |
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| S2755 |
VarlitinibVarlitinib是一种有效的，选择性ErbB1(EGFR)和ErbB2(HER2)抑制剂，IC50分别为7 nM和2 nM。Phase 2。 |
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| S2922 |
IcotinibIcotinib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)。Phase 4。 |
B. Effect of Icotinib treatment on the subcellular localization of ABCG2 in NCI-H460/MX20 cell. ABCG2 staining is shown in green. DAPI (blue) counterstains the nuclei. C. Effect of Icotinib on the ATPase activity of ABCG2: The BeFx-sensitive specific ATPase activity of ABCG2 was determined in the presence of 0-5 μM of Icotinib as described in supplemental methods. The activity in the absence of Icotinib (basal activity) was considered to be 100%, and % -fold stimulation ± S.D. (Y-axis) was plotted as a function of indicated concentrations of Icotinib (X-axis). D. Effect of Icotinib on the photolabeling of ABCG2 with [125I]-IAAP: Crude membranes from ABCG2 expressing MCF7-FLV1000 cells were photo-crosslinked with [125I]-IAAP in the presence and absence of 0-50 μM of Icotinib as described in supplemental methods. [125I]-IAAP incorporated in ABCG2 band was quantified using ImageQuant software and plotted as % [125I]-IAAP incorporated ± S.D. (Y-axis) as a function of varying concentration of Icotinib (X-axis). The upper panel shows a representative autoradiogram from three independent experiments and the arrow represents the ABCG2 band photo-crosslinked with [125I]-IAAP. |
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| S2784 |
TAK-285TAK-285是一种新型，HER2和EGFR(HER1)双重抑制剂，IC50分别为17 nM和23 nM，作用于HER1/2比作用于HER4选择性高10倍以上，对MEK1/5， c-Met， Aurora B， Lck， CSK等作用效果稍弱。Phase 1。 |
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| S2867 |
WHI-P154WHI-P154是一种有效的JAK3抑制剂，IC50为1.8 μM，对JAK1和JAK2没有抑制活性，也抑制EGFR， Src， Abl， VEGFR和MAPK，抑制Stat3而非Stat5磷酸化。 |
Reversal effect of WHI-P154 on the sensitivity of NCI-H460/MX20 cells to mitoxantrone. The figure showes the survival curves of cells at different concentrations of mitoxantrone with or without WHI-P154. Cell viability was determined by MTT Assay. NCI-H460 is lung cancer cell line while NCI-H460/MX20 is ABCG2 overexpressing drug (mitoxantrone) selected cell line. |
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| S2554 |
DaphnetinDaphnetin是天然香豆素衍生物，是一种蛋白激酶抑制剂，抑制EGFR， PKA和PKC，IC50分别为7.67 μM， 9.33 μM和25.01 μM，且具有抗炎和抗氧化剂活动性。 |
C57/BL6 mice (5 mice/group) were intraperitoneally injected with daphnetin (DFN, 5 mg/kg) or DMSO, and then challenged with LPS (37.5 mg/kg) or saline. 16 h after LPS challenge, mice were sacrificed, and then lung and serum were collected. c, Representative photomicrographs showed H&E staining of lung tissue.
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| S7039 |
PD168393PD168393是一种不可逆的EGFR抑制剂，IC50为0.70 nM，不可逆烷基化Cys-773；抑制insulin， PDGFR， FGFR和PKC活性。 |
(B) Immunohistochemical staining for α-actinin and EdU showed that EGFR inhibitor (PD-168393), JNK inhibitor (sp-600125), and SP-1 inhibitor (mithramycin A) could abolish the effect of TIMP-3 siRNA in promoting cardiomyocyte proliferation. n=3 per group for Western blot. At least 2000 cells were quantified in each group. Data are shown as mean±SEM and reflect at least three independent experiments. Scale bar: 100 μm. *, P<0.05, ***, P<0.001 versus respective control.
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| S2895 |
Tyrphostin 9Tyrphostin 9 是第一个EGFR抑制剂，IC50为460 μM，作用于PDGFR更有效，IC50为0.5μM。 |
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| S7206 |
CNX-2006CNX-2006是一种新型，不可逆，突变选择性的EGFR抑制剂，IC50为<20 nM，对野生型EGFR有微弱的抑制作用。 |
d) Western blots for phosphorylation of epidermal growth factor receptor (EGFR) and MET, cleaved PARP as an apoptotic marker, and b-actin in HCC827 and their resistant clones. Total cell lysates were extracted 24 h after exposure of DMSO, 0.5 μM erlotinib, 0.5 μM CNX-2006, PHA-665752 and their combinations.
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| S8009 |
AG-18AG-18抑制EGFR，IC50为35 μM。 |
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| S7298 |
AZ5104AZ5104，是AZD-9291的脱甲基代谢物，是一种有效的EGFR抑制剂，作用于EGFR (L858R/T790M)，EGFR (L858R)，EGFR (L861Q)，和EGFR (野生型)，IC50分别为<1 nM，6 nM，1 nM，和25 nM。Phase 1。 |
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| S7297 |
Osimertinib (AZD9291)AZD9291 是口服不可逆的，突变选择性EGFR抑制剂，在 LoVo细胞中对Exon 19 缺失的 EGFR，L858R/T790M EGFR，和 WT EGFR的IC50分别为12.92，11.44 和 493.8 nM。Phase 3。 |
(C,D) The Ba/F3 cells expressing EGFR-T854A/C797S/del19 (C) and EGFR-T854A/C797S/L858R (D) were treated with gefitinib, afatinib, osimertinib, and brigatinib for 6 hours at indicated concentrations. EGFR phosphorylation and downstream signal pathway were evaluated by Western blotting.
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| S7557 |
CL-387785 (EKI-785)CL-387785 (EKI-785)是一种不可逆的选择性EGFR抑制剂，IC50为370 pM。 |
C, EGFR L718Q and L844V Ba/F3 cells retain sensitivity to irreversible quinazoline EGFR inhibitors. Cells were treated with different drugs at the indicated concentrations, and viable cells were measured after 72 hours of treatment and plotted relative to untreated controls. For Western blot analysis, 3T3 cells expressing the respective constructs were treated with different drugs at indicated concentrations for 16 hours. Cell extracts were immunoblotted to detect the indicated proteins. D, EGFR Del 1/L718Q Ba/F3 cells have a growth disadvantage. Equal number of cells was seeded in the presence of or absence of EGF or IL3. Cell number was evaluated in triplicate at the indicated time points. |
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| S8294 |
Olmutinib (HM61713, BI 1482694)Olmutinib是一种新型的EGFR突变特效性酪氨酸激酶抑制剂、布鲁顿氏酪氨酸激酶抑制剂。 |
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| S2250 |
(-)-Epigallocatechin Gallate(-)-Epigallocatechin Gallate是从绿茶中分离的一种有效的抗氧化剂Polyphenol flavonoid。抑制telomerase和DNA methyltransferase， 阻滞EGF受体和HER-2受体的激活，抑制脂肪酸合成酶以及谷氨酸脱氢酶的活性。 |
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-Epigallocatechin-Gallate-S225001Y0120170210.gif)
(a) Huh7 cells were incubated with HCVcc of JFH-1 for 2 h before overlaying with 1% agarose dissolved in culture medium or with AR3A anti-E2 neutralizing antibodies, in the presence of 20 μg/ml SZA. EGCG (50 μM) was introduced as a positive control. At 48 h post-infection, infected cells were quantified by IF. Nuclei were stained with DAPI. (b) Numbers of cells per positive colony were determined in 15 foci.
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| S7786 |
ErlotinibErlotinib 是一种EGFR抑制剂，IC50 为 2 nM，对EGFR的敏感性比对人c-Src 或 v-Ab高1000多倍。 |
Erlotinib IC50 in HCC827 cell lines measured 48h after treatment with vehicle (control) or with erlotinib. Erlotinib IC50 is shown in parentheses. Data are representative of 3 independent experiments. Effects of treatment for 48h with a vehicle or the indicated doses of MP-470 in parental or ER1 and ER2 cell lines in the absence and presence of erlotinib on the indicated biomarkers. |
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| S7810 |
Afatinib (BIBW2992) DimaleateAfatinib (BIBW2992) Dimaleate 不可逆地抑制 EGFR/HER2，包括 EGFR(wt)，EGFR(L858R)，EGFR(L858R/T790M) 和 HER2，IC50 分别为0.5 nM，0.4 nM，10 nM 和 14 nM；活性比对Gefitinib抵抗型L858R-T790M EGFR突变体高100倍。 |
(F) Stably transduced MCF10A cells were treated with the indicated drugs at 100 nM for 4 h in EGF- and serum-free media. Cell lysates were subjected to immunoblot analyses with the indicated antibodies.
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| S7971 |
AZD3759AZD3759是一种有效的，具有口服活性的，CNS-渗透性EGFR抑制剂，对EGFR (WT)，EGFR (L858R)，和 EGFR (exon 19Del)的IC50分别为0.3 nM，0.2 nM，和 0.2 nM。Phase 1。 |
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| S7358 |
Poziotinib (HM781-36B)Poziotinib (HM781-36B)是一种不可逆的泛-HER抑制剂，对HER1，HER2，和HER4的IC50分别为3.2 nM，5.3 nM和23.5 nM。 |
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| S8229 |
Brigatinib (AP26113)Brigatinib (AP26113)是一种有效的、选择性的ALK抑制剂，IC50=0.6 nM；也是ROS1抑制剂，IC50=0.9 nM。它还能以相对较低的效力抑制FLT3、FLT3(D835Y)、EGFR。 |
Immunoblotting analysis of H3122 and H3122-CER cells showing that brigatinib did not inhibit EGFR phosphorylation (p-EGFR). Total EGFR (t-EGFR) is also shown. Actin was used as a loading control. The cells were treated with brigatinib for 2 hours.
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| S8412 |
Naquotinib(ASP8273)Naquotinib(ASP8273)是一种具有口服活性的、不可逆的、对突变体具有选择性的epidermal growth factor receptor (EGFR)抑制剂，具有潜在的抗肿瘤活性。 |
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| S2406 |
Chrysophanic AcidChrysophanic Acid是Dianella longifolia中的一种天然蒽醌，是一种EGFR/mTOR通道抑制剂。 |
After starved in serum-free medium for 24h, A549 cells incubated with the indicated concentrations of Chrysophanic acid for 3h,followed by 15-minute stimolation of 100ng/ml EGF |
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| S7824 |
Nazartinib (EGF816, NVS-816)Nazartinib (EGF816, NVS-816)是共价的、不可逆的、对突变型EGFR具有选择性的抑制剂，对突变型EGFR(L858R, ex19del)和T790M具有纳摩尔级别的抑制作用，相对于野生型EGFR，其对突变型EGFR更具特异性。 |
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| S7926 |
Lifirafenib (BGB-283)Lifirafenib (BGB-283)有效地抑制RAF激酶家族和EGFR活性，在生化实验检测中，其对重组BRAF(V600E)激酶区域、EGFR和EGFR(T790M/L858R)突变体的IC50分别为23、29、495 nM。 |
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| S4667 |
Lidocaine hydrochlorideLidocaine hydrochloride是一种局部麻醉剂及心脏抑制剂，被用作抗心律失常剂。 |
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| S8036 |
ButeinButein，一种从漆树中分离的植物多酚，可以抑制酪氨酸激酶，NF-κB，STAT3和EGFR活化。 |
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| S8242 |
EAI045EAI045是一种靶向特定耐药性的EGFR突变体的变构抑制剂。对野生型受体无作用。 |
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| S8312 |
NSC228155NSC228155是EGFR的激活剂，与sEGFR的二聚体化功能域II结合、调节EGFR的酪氨酸磷酸化。 |
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