EGFR
信号通路图
研究领域
抑制剂选择性比较
EGFR产品
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| A2000 |
Cetuximab (anti-EGFR)Cetuximab (anti-EGFR)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。 |
Mice showed progression disease to first-line treatment were randomized 1:1 to the two arms of treatment and were treated until onset of progression disease or until the end-time of experiment in case of response (fixed to 52 weeks from the start of first-line therapy ), as indicated in in the Materials and Methods section. Growth curves of HCC827 xenografts treated in secondline with osimertinib plus selumetinib or cetuximab are represented as changes in the values of volumes as percentage compared to baseline tumor volume at the time of progression diasease to first-line (defined as 100%) for each case. Median tumor volume at PD2 was of 348 mm3.
|
|
| 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。 |
Effects of combined treatment with erlotinib and NPS-1034 in HCC827/ER cells with AXL activation. Lysates were immunoprecipitated with an anti-AXL antibody and immunoblotted with antibodies for phosphotyrosine (p-Tyr) and AXL. HCC827/ER cells were treated with erlotinib. E, erlotinib; N, NPS-1034. **, P < 0.001 for the combination of erlotinib plus NPS-1034 versus either the control or drug alone. |
|
| 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。Gefitinib 可通过阻滞PI3K/AKT/mTOR信号通路来促进肺癌细胞的自噬和细胞凋亡。 |
Perturbation of EGFR by its ligand EGF and gefitinib (ZD-1839 Iressat; inhibits EGFR) produces opposite responses in the predicted EGFR target genes SOCS2 and NR2E1. |
|
| 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. |
|
| 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。Afatinib可诱导自噬。 |
Inhibition of signaling pathway activation in lung tumor cell lines by kinase inhibitors. Lung tumor cells were cultured in 10% FBS until reaching ∼80% confluence and then the cells were starved in serum-free medium for overnight, followed by 4-hour treatment with the inhibitors. Cell lysates were then prepared and used for determination of the pathway activation signals by the CEER assay. |
|
| S1006 |
Saracatinib (AZD0530)Saracatinib (AZD0530)是一种有效的Src抑制剂，无细胞试验中IC50为2.7 nM，对c-Yes， Fyn， Lyn， Blk， Fgr和Lck也具有活性；但对Abl和EGFR (L858R和L861Q)活性较低。Saracatinib可诱导自噬。Phase 2/3。 |
C and D, in vivo subcutaneous tumor growth curves (C) and tumor weight quantification of intersected subcutaneous tumor tissues (D) of Huh7 cells after stable LHBs expression under saracatinib treatment (25 mg/kg body weight daily for 4 weeks; n =18). *, P < 0.05. E and F,in vivo subcutaneous tumor growth curves (E) and tumor weight quantification of intersected subcutaneous tumor tissues (F) of SK-Hep1 cells after stable LHBs expression under saracatinib treatment (25 mg/kg body weight daily for 4 weeks; n = 18). *, P < 0.05. |
|
| S8852New |
Pyrotinib (SHR-1258)Pyrotinib (SHR-1258) 是一种有效的、具有选择性的、不可逆的 EGFR 和 HER2 双重酪氨酸激酶抑制剂，其对应的IC50值分别为0.013 μM和0.038 μM。 |
||
| S6805New |
Tyrphostin AG-528Tyrphostin AG-528 是一种 epidermal growth factor receptors (EGFR) 和 ErbB2/HER2 的有效抑制剂，其IC50值分别为4.9 μM和2.1 μM。Tyrphostin AG-528 具有抗癌活性。 |
||
| S6813New |
Mobocertinib (TAK788)Mobocertinib (TAK788) 是一种研究用的TKI，是有效的、选择性的 epidermal growth factor receptor (EGFR) 和 HER2 突变体的临床前抑制剂。Mobocertinib (TAK788) 是一种抗肿瘤药。 |
||
| S0360New |
EGFR InhibitorEGFR inhibitor 是一种可透过细胞的4,6-二取代嘧啶化合物，是一种具有高度选择性的 EGFR kinase 的抑制剂，其IC50值为21 nM。EGFR inhibitor 可直接使 microtubules 解聚，可作为研究EGFR途径和微管动力学的化学探针。 |
||
| S6809New |
SU5214SU5214是 VEGF receptor 2 (VEGFR2/FLK-1) 和 EGFR 的抑制剂，对应的IC50值分别为14.8 µM 和 36.7 µM。 |
||
| S2115New |
RG 13022RG-13022抑制免疫沉淀反应中EGF receptor的自磷酸化反应，IC50为4 µM。 |
||
| S1054New |
AG99AG99是一种有效、选择性的EGFR抑制剂。 |
||
| S6698New |
TQB3804 (EGFR-IN-7)TQB3804 is a selective and potent EGFR kinase inhibitor, has IC50 values of 7.92 nM,0.218 nM and 0.16 nM for EGFR(WT), EGFR(19del/T790M/C797S) and EGFR(L858R/T790M/C797S) respectively, and shows anti-tumor activity. |
||
| S8814New |
TAS6417TAS6417是一种新型的EGFR抑制剂，靶向EGFR突变体，对野生型EGFR抑制效力较低，IC50范围为1.1 ± 0.1到8.0 ± 1.1 nmol/L。 |
||
| S6546New |
PD153035PD153035是一种特定的、有效的EGFR抑制剂，Ki值为5.2 pM。 |
||
| S6530New |
EBE-A22EBE-A22是PD 153035的衍生物。PD 153035可抑制ErbB-1磷酸化，而EBE-A22无此活性。 |
||
| S6541New |
MTX-211MTX-211是PI3K和EGFR的双重抑制剂。 |
||
| S6509New |
AG 494AG-494是EGFR受体自身磷酸化的抑制剂，IC50为1.2 μM。它抑制依赖于EGF的细胞生长，IC50为6 μM。 |
||
| S6523New |
RG14620RG14620是一种EGFR抑制剂，可直接抑制ABCG2的传送功能。 |
||
| S6525New |
AG 555AG-555是酪氨酸激酶抑制剂，可与拓扑异构酶I直接相互作用，因而阻止DNA松弛。它抑制EGFR，IC50为0.7 μM。 |
||
| 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。 |
HER2 mutations V777L, D769H, V842I, G309A induce gain-of-function over HER2 WT in MCF10A mammary epithelial cells. B, HER2 WT, L755S, and del.755–759 cells were grown in Matrigel in the presence of DMSO vehicle (0.5%), neratinib (0.5 μmol/L) or gefitinib (0.5 μmol/L). Phase contrast images were obtained as in A. C, MCF10A-HER2 WT or mutants were seeded in soft agar. After 7 days of growth, they were treated with DMSO vehicle (0.5%), lapatinib (0.5 μmol/L) or neratinib (0.5 μmol/L) for an additional week. Error bars represent 95% highest posterior density intervals. *, Significant difference between the HER2 mutant and HER2 WT; #, the effect of inhibitor treatment was significant (95% highest posterior density interval did not contain 0 for both). D, photomicrographs of the colonies in soft agar on day 12, magnification ×40. |
|
| 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。 |
(B–C) LNCaP (B) and LNCaP-AI (C) cells were transiently transfected with sPLA2-IIa(-800)-Luc (0.5 lg). The cells were then treated with Erlotinib (20 lM), Gefitinib (20 lM), Lapatinib (20 lM), CI-1033 (8 lM), LY294002 (20 lM) and Bortezomib (20 lM) without or with EGF (100 ng/ml) for 24 h. Luciferase assay was performed according to a standard protocol with Renilla luciferase as an internal control. Data are presented as the mean (±SD) of duplicate values of a representative experiment that was independently repeated for five times. |
|
| 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。Lapatinib 可诱导 ferroptosis 和细胞自噬。 |
Aberrantly activated PI3K/AKT pathway mediates lapatinib resistance in SK-BR-3-LR cells. (A and B) After drug treatment, phosphorylation of HER2, EGFR, AKT, and ERK1/2 was determined by Western blotting using specific antibodies. |
|
| 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。 |
IL6 normally induces WASF3 expression in MDA231 cells, but co-treatments
with AG490 (a pan-JAK inhibitor) show a dose-dependent reduction of both WASF3 levels and activated STAT3 levels.
|
|
| 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。 |
|
|
| S2727 |
Dacomitinib (PF-00299804)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。Dacomitinib 抑制 ERBB2 和 ERBB4 ，其对应的IC50值分别为45.7 nM和73.7 nM。Dacomitinib 可高效作用于携带EGFR或ERBB2突变型(耐Gefitinib)和携带EGFR T790M突变型的NSCLCs。Dacomitinib 可抑制细胞生长并诱导凋亡。Phase 2。 |
|
|
| 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. |
|
| 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。 |
|
|
| 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.
|
|
| 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.
|
|
| 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。 |
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). |
|
| 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。 |
HBMEC were preincubated with the indicated concentrations of either ErB1/2/4 inhibitor (Pelitinib; EKB-569), and cells were then infected for 4 h with the unencapsulated strain, MC58 siaD. The numbers of adherent (black bars) and invasive (gray bars) bacteria were determined in a gentamicin protection assay. The graphs show the percentages of adhesion and invasion of inhibitor-treated cells, relative to control cells (means 盨D of three independent experiments performed in duplicate). *, P < 0.05.
|
|
| 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。 |
Co-treatments of PI-103 and EGFR inhibitors enhance cytotoxicity in SUM149PT cells. Cells were treated with 0.3 uM of PI-103 in combination with different concentrations (0.1 and 1 uM) of EGFR inhibitors (BMS-599626) for -72 hrs. Cell viability was measured by MTT assay as described in Materials and methods. Data from two independent experiments performed in triplicate are shown as mean+SEM. *P < 0.05; **P < 0.01; ***P < 0.001. |
|
| 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. |
|
| 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. |
|
| 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. |
|
| 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.
|
|
| 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. |
|
| 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. |
|
| S2185 |
Allitinib (AST-1306)AST-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. |
|
| S7284 |
Rociletinib (CO-1686)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。 |
Western blot analysis of H1975 mock and H1975 EGFR cells treated with the indicated concentrations of EGF and rociletinib for phosphorylated (p-) and total (t-) EGFR, AKT, ERK1/2, and b-actin. |
|
| 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。 |
||
| 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。 |
|
|
| 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. |
|
| 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。 |
||
| 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. |
|
| 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.
|
|
| 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.
|
|
| 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。 |
||
| 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.
|
|
| S8009 |
AG-18AG-18抑制EGFR，IC50为35 μM。 |
||
| 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。 |
||
| S8724 |
LazertinibLazertinib (YH25448,GNS-1480)是一种有效的、对突变型具有高选择性的、不可逆的EGFR抑制剂，对Del19/T790M、L858R/T790M、Del19、L85R和野生型EGFR的IC50分别为1.7 nM, 2 nM, 5 nM, 20.6 nM和76 nM。对ErbB2和ErbB4的IC50值更高。 |
||
| 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。 |
Western blot analysis for total (t-) and phosphorylated (p-) EGFR, AKT, ERK1/2, and β actin in H1975 parental and resistant (COR#3, AZDR#1) cells. |
|
| 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. |
|
| S8362 |
Tucatinib (Irbinitinib, ONT-380)Tucatinib (Irbinitinib, ONT-380) 是一种具有口服活性、可逆的、ATP竞争性的的ErbB2（HER2）小分子抑制剂。在细胞实验中，ARRY-380对ErbB-2和p95 HER2的IC50s分别为8 nM和7 nM，对HER2的选择性是对EGFR的500倍。具有潜在的抗肿瘤活性。 |
||
| S8294 |
Olmutinib (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。 |
||
| 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。 |
|
|
| 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可诱导自噬。 |
Effects of combined treatment with erlotinib and NPS-1034 in HCC827/ER cells with AXL activation. Lysates were immunoprecipitated with an anti-AXL antibody and immunoblotted with antibodies for phosphotyrosine (p-Tyr) and AXL. HCC827/ER cells were treated with erlotinib. E, erlotinib; N, NPS-1034. **, P < 0.001 for the combination of erlotinib plus NPS-1034 versus either the control or drug alone. |
|
| S5098 |
Gefitinib hydrochlorideGefitinib is an EGFR inhibitor with IC50s of 15.5 nM and 823.3 nM for WT EGFR and EGFR (858R/T790M), respectively. |
||
| 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。 |
Inhibition of signaling pathway activation in lung tumor cell lines by kinase inhibitors. Lung tumor cells were cultured in 10% FBS until reaching ∼80% confluence and then the cells were starved in serum-free medium for overnight, followed by 4-hour treatment with the inhibitors. Cell lysates were then prepared and used for determination of the pathway activation signals by the CEER assay. |
|
| 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。 |
||
| 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。Poziotinib可诱导凋亡和G1细胞周期阻滞。Phase 2。 |
||
| 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.
|
|
| S5078 |
Osimertinib mesylateOsimertinib mesylate is the mesylate form of osimertinib, which is an oral, third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) drug. |
||
| 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。 |
||
| 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 |
|
| S7824 |
Nazartinib (EGF816)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。 |
||
| S3759 |
NorcantharidinNorcantharidin is a synthetic anticancer compound which is a dual inhibitor for c-Met and EGFR in human colon cancers. |
||
| S8584 |
Theliatinib (HMPL-309)Theliatinib (HMPL-309)是一种高效的EGFR抑制剂，对EGFR的Ki值为0.05 nM，对EGFR和EGFR T790M/L858R突变体的IC50值分别为3 nM和22 nM。它对EGFR的选择性是对其他72种激酶的50倍以上。 |
||
| 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。 |
||
| 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。 |
||
| 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。 |
||
| 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。 |
||
| S9414 |
CyasteroneCyasterone is the main phytoecdysteroid component found in Cyathula capitata. It is a natural EGFR inhibitor and maybe a promising anti-cancer agent. |
||
| S8817 |
HS-10296HS-10296 (Almonertinib, Ameile) 是一种EGFR激活突变和对EGFR T790M具有耐受性突变的抑制剂，其对野生型EGFR仅具有有限活性。 |
||
| S8741 |
Avitinib (AC0010)Avitinib (AC0010)是不可逆的EGFR抑制剂，对于突变型EGFR具有选择性，对EGFR L858R/T790M双突变体的IC50为0.18 nM，是对野生型EGFR效力的近43倍（IC50=7.68 nM for WT EGFR）。Avitinib具有抗肿瘤活性和耐受性毒性。 |
||
| 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。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| A2000 |
Cetuximab (anti-EGFR)Cetuximab (anti-EGFR)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。 |
Mice showed progression disease to first-line treatment were randomized 1:1 to the two arms of treatment and were treated until onset of progression disease or until the end-time of experiment in case of response (fixed to 52 weeks from the start of first-line therapy ), as indicated in in the Materials and Methods section. Growth curves of HCC827 xenografts treated in secondline with osimertinib plus selumetinib or cetuximab are represented as changes in the values of volumes as percentage compared to baseline tumor volume at the time of progression diasease to first-line (defined as 100%) for each case. Median tumor volume at PD2 was of 348 mm3.
|
|
| 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。 |
Effects of combined treatment with erlotinib and NPS-1034 in HCC827/ER cells with AXL activation. Lysates were immunoprecipitated with an anti-AXL antibody and immunoblotted with antibodies for phosphotyrosine (p-Tyr) and AXL. HCC827/ER cells were treated with erlotinib. E, erlotinib; N, NPS-1034. **, P < 0.001 for the combination of erlotinib plus NPS-1034 versus either the control or drug alone. |
|
| 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。Gefitinib 可通过阻滞PI3K/AKT/mTOR信号通路来促进肺癌细胞的自噬和细胞凋亡。 |
Perturbation of EGFR by its ligand EGF and gefitinib (ZD-1839 Iressat; inhibits EGFR) produces opposite responses in the predicted EGFR target genes SOCS2 and NR2E1. |
|
| 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. |
|
| 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。Afatinib可诱导自噬。 |
Inhibition of signaling pathway activation in lung tumor cell lines by kinase inhibitors. Lung tumor cells were cultured in 10% FBS until reaching ∼80% confluence and then the cells were starved in serum-free medium for overnight, followed by 4-hour treatment with the inhibitors. Cell lysates were then prepared and used for determination of the pathway activation signals by the CEER assay. |
|
| S1006 |
Saracatinib (AZD0530)Saracatinib (AZD0530)是一种有效的Src抑制剂，无细胞试验中IC50为2.7 nM，对c-Yes， Fyn， Lyn， Blk， Fgr和Lck也具有活性；但对Abl和EGFR (L858R和L861Q)活性较低。Saracatinib可诱导自噬。Phase 2/3。 |
C and D, in vivo subcutaneous tumor growth curves (C) and tumor weight quantification of intersected subcutaneous tumor tissues (D) of Huh7 cells after stable LHBs expression under saracatinib treatment (25 mg/kg body weight daily for 4 weeks; n =18). *, P < 0.05. E and F,in vivo subcutaneous tumor growth curves (E) and tumor weight quantification of intersected subcutaneous tumor tissues (F) of SK-Hep1 cells after stable LHBs expression under saracatinib treatment (25 mg/kg body weight daily for 4 weeks; n = 18). *, P < 0.05. |
|
| S8852New |
Pyrotinib (SHR-1258)Pyrotinib (SHR-1258) 是一种有效的、具有选择性的、不可逆的 EGFR 和 HER2 双重酪氨酸激酶抑制剂，其对应的IC50值分别为0.013 μM和0.038 μM。 |
||
| S6805New |
Tyrphostin AG-528Tyrphostin AG-528 是一种 epidermal growth factor receptors (EGFR) 和 ErbB2/HER2 的有效抑制剂，其IC50值分别为4.9 μM和2.1 μM。Tyrphostin AG-528 具有抗癌活性。 |
||
| S6813New |
Mobocertinib (TAK788)Mobocertinib (TAK788) 是一种研究用的TKI，是有效的、选择性的 epidermal growth factor receptor (EGFR) 和 HER2 突变体的临床前抑制剂。Mobocertinib (TAK788) 是一种抗肿瘤药。 |
||
| S0360New |
EGFR InhibitorEGFR inhibitor 是一种可透过细胞的4,6-二取代嘧啶化合物，是一种具有高度选择性的 EGFR kinase 的抑制剂，其IC50值为21 nM。EGFR inhibitor 可直接使 microtubules 解聚，可作为研究EGFR途径和微管动力学的化学探针。 |
||
| S6809New |
SU5214SU5214是 VEGF receptor 2 (VEGFR2/FLK-1) 和 EGFR 的抑制剂，对应的IC50值分别为14.8 µM 和 36.7 µM。 |
||
| S2115New |
RG 13022RG-13022抑制免疫沉淀反应中EGF receptor的自磷酸化反应，IC50为4 µM。 |
||
| S1054New |
AG99AG99是一种有效、选择性的EGFR抑制剂。 |
||
| S6698New |
TQB3804 (EGFR-IN-7)TQB3804 is a selective and potent EGFR kinase inhibitor, has IC50 values of 7.92 nM,0.218 nM and 0.16 nM for EGFR(WT), EGFR(19del/T790M/C797S) and EGFR(L858R/T790M/C797S) respectively, and shows anti-tumor activity. |
||
| S8814New |
TAS6417TAS6417是一种新型的EGFR抑制剂，靶向EGFR突变体，对野生型EGFR抑制效力较低，IC50范围为1.1 ± 0.1到8.0 ± 1.1 nmol/L。 |
||
| S6546New |
PD153035PD153035是一种特定的、有效的EGFR抑制剂，Ki值为5.2 pM。 |
||
| S6530New |
EBE-A22EBE-A22是PD 153035的衍生物。PD 153035可抑制ErbB-1磷酸化，而EBE-A22无此活性。 |
||
| S6541New |
MTX-211MTX-211是PI3K和EGFR的双重抑制剂。 |
||
| S6509New |
AG 494AG-494是EGFR受体自身磷酸化的抑制剂，IC50为1.2 μM。它抑制依赖于EGF的细胞生长，IC50为6 μM。 |
||
| S6523New |
RG14620RG14620是一种EGFR抑制剂，可直接抑制ABCG2的传送功能。 |
||
| S6525New |
AG 555AG-555是酪氨酸激酶抑制剂，可与拓扑异构酶I直接相互作用，因而阻止DNA松弛。它抑制EGFR，IC50为0.7 μM。 |
||
| 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。 |
HER2 mutations V777L, D769H, V842I, G309A induce gain-of-function over HER2 WT in MCF10A mammary epithelial cells. B, HER2 WT, L755S, and del.755–759 cells were grown in Matrigel in the presence of DMSO vehicle (0.5%), neratinib (0.5 μmol/L) or gefitinib (0.5 μmol/L). Phase contrast images were obtained as in A. C, MCF10A-HER2 WT or mutants were seeded in soft agar. After 7 days of growth, they were treated with DMSO vehicle (0.5%), lapatinib (0.5 μmol/L) or neratinib (0.5 μmol/L) for an additional week. Error bars represent 95% highest posterior density intervals. *, Significant difference between the HER2 mutant and HER2 WT; #, the effect of inhibitor treatment was significant (95% highest posterior density interval did not contain 0 for both). D, photomicrographs of the colonies in soft agar on day 12, magnification ×40. |
|
| 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。 |
(B–C) LNCaP (B) and LNCaP-AI (C) cells were transiently transfected with sPLA2-IIa(-800)-Luc (0.5 lg). The cells were then treated with Erlotinib (20 lM), Gefitinib (20 lM), Lapatinib (20 lM), CI-1033 (8 lM), LY294002 (20 lM) and Bortezomib (20 lM) without or with EGF (100 ng/ml) for 24 h. Luciferase assay was performed according to a standard protocol with Renilla luciferase as an internal control. Data are presented as the mean (±SD) of duplicate values of a representative experiment that was independently repeated for five times. |
|
| 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。Lapatinib 可诱导 ferroptosis 和细胞自噬。 |
Aberrantly activated PI3K/AKT pathway mediates lapatinib resistance in SK-BR-3-LR cells. (A and B) After drug treatment, phosphorylation of HER2, EGFR, AKT, and ERK1/2 was determined by Western blotting using specific antibodies. |
|
| 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。 |
IL6 normally induces WASF3 expression in MDA231 cells, but co-treatments
with AG490 (a pan-JAK inhibitor) show a dose-dependent reduction of both WASF3 levels and activated STAT3 levels.
|
|
| 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。 |
|
|
| S2727 |
Dacomitinib (PF-00299804)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。Dacomitinib 抑制 ERBB2 和 ERBB4 ，其对应的IC50值分别为45.7 nM和73.7 nM。Dacomitinib 可高效作用于携带EGFR或ERBB2突变型(耐Gefitinib)和携带EGFR T790M突变型的NSCLCs。Dacomitinib 可抑制细胞生长并诱导凋亡。Phase 2。 |
|
|
| 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. |
|
| 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。 |
|
|
| 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.
|
|
| 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.
|
|
| 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。 |
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). |
|
| 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。 |
HBMEC were preincubated with the indicated concentrations of either ErB1/2/4 inhibitor (Pelitinib; EKB-569), and cells were then infected for 4 h with the unencapsulated strain, MC58 siaD. The numbers of adherent (black bars) and invasive (gray bars) bacteria were determined in a gentamicin protection assay. The graphs show the percentages of adhesion and invasion of inhibitor-treated cells, relative to control cells (means 盨D of three independent experiments performed in duplicate). *, P < 0.05.
|
|
| 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。 |
Co-treatments of PI-103 and EGFR inhibitors enhance cytotoxicity in SUM149PT cells. Cells were treated with 0.3 uM of PI-103 in combination with different concentrations (0.1 and 1 uM) of EGFR inhibitors (BMS-599626) for -72 hrs. Cell viability was measured by MTT assay as described in Materials and methods. Data from two independent experiments performed in triplicate are shown as mean+SEM. *P < 0.05; **P < 0.01; ***P < 0.001. |
|
| 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. |
|
| 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. |
|
| 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. |
|
| 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.
|
|
| 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. |
|
| 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. |
|
| S2185 |
Allitinib (AST-1306)AST-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. |
|
| S7284 |
Rociletinib (CO-1686)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。 |
Western blot analysis of H1975 mock and H1975 EGFR cells treated with the indicated concentrations of EGF and rociletinib for phosphorylated (p-) and total (t-) EGFR, AKT, ERK1/2, and b-actin. |
|
| 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。 |
||
| 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。 |
|
|
| 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. |
|
| 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。 |
||
| 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. |
|
| 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.
|
|
| 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.
|
|
| 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。 |
||
| 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.
|
|
| S8009 |
AG-18AG-18抑制EGFR，IC50为35 μM。 |
||
| 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。 |
||
| S8724 |
LazertinibLazertinib (YH25448,GNS-1480)是一种有效的、对突变型具有高选择性的、不可逆的EGFR抑制剂，对Del19/T790M、L858R/T790M、Del19、L85R和野生型EGFR的IC50分别为1.7 nM, 2 nM, 5 nM, 20.6 nM和76 nM。对ErbB2和ErbB4的IC50值更高。 |
||
| 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。 |
Western blot analysis for total (t-) and phosphorylated (p-) EGFR, AKT, ERK1/2, and β actin in H1975 parental and resistant (COR#3, AZDR#1) cells. |
|
| 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. |
|
| S8362 |
Tucatinib (Irbinitinib, ONT-380)Tucatinib (Irbinitinib, ONT-380) 是一种具有口服活性、可逆的、ATP竞争性的的ErbB2（HER2）小分子抑制剂。在细胞实验中，ARRY-380对ErbB-2和p95 HER2的IC50s分别为8 nM和7 nM，对HER2的选择性是对EGFR的500倍。具有潜在的抗肿瘤活性。 |
||
| S8294 |
Olmutinib (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。 |
||
| 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。 |
|
|
| 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可诱导自噬。 |
Effects of combined treatment with erlotinib and NPS-1034 in HCC827/ER cells with AXL activation. Lysates were immunoprecipitated with an anti-AXL antibody and immunoblotted with antibodies for phosphotyrosine (p-Tyr) and AXL. HCC827/ER cells were treated with erlotinib. E, erlotinib; N, NPS-1034. **, P < 0.001 for the combination of erlotinib plus NPS-1034 versus either the control or drug alone. |
|
| S5098 |
Gefitinib hydrochlorideGefitinib is an EGFR inhibitor with IC50s of 15.5 nM and 823.3 nM for WT EGFR and EGFR (858R/T790M), respectively. |
||
| 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。 |
Inhibition of signaling pathway activation in lung tumor cell lines by kinase inhibitors. Lung tumor cells were cultured in 10% FBS until reaching ∼80% confluence and then the cells were starved in serum-free medium for overnight, followed by 4-hour treatment with the inhibitors. Cell lysates were then prepared and used for determination of the pathway activation signals by the CEER assay. |
|
| 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。 |
||
| 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。Poziotinib可诱导凋亡和G1细胞周期阻滞。Phase 2。 |
||
| 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.
|
|
| S5078 |
Osimertinib mesylateOsimertinib mesylate is the mesylate form of osimertinib, which is an oral, third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) drug. |
||
| 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。 |
||
| 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 |
|
| S7824 |
Nazartinib (EGF816)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。 |
||
| S3759 |
NorcantharidinNorcantharidin is a synthetic anticancer compound which is a dual inhibitor for c-Met and EGFR in human colon cancers. |
||
| S8584 |
Theliatinib (HMPL-309)Theliatinib (HMPL-309)是一种高效的EGFR抑制剂，对EGFR的Ki值为0.05 nM，对EGFR和EGFR T790M/L858R突变体的IC50值分别为3 nM和22 nM。它对EGFR的选择性是对其他72种激酶的50倍以上。 |
||
| 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。 |
|