EGFR/ErbB1 选择性抑制剂 | 激活剂

目录号 产品名 产品描述 Selective / Pan IC50 / Ki
S8312 NSC228155

NSC228155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。

Selective
S6546 PD153035

PD153035 is a specific and potent inhibitor of the epidermal growth factor (EGF) receptor tyrosine kinase (Ki = 5.2 pM).

Selective EGFR, Ki: 5.2 pM
S1079 PD153035 HCl

PD153035 HCl是一种有效的,特异性EGFR抑制剂,无细胞试验中KiIC50分别为5.2 pM和29 pM;对PGDFR, FGFR, CSF-1, InsR和Src几乎无作用。

Selective EGFR, Ki: 5.2 pM
S7971 Zorifertinib (AZD3759)

AZD3759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。

Selective EGFR (L858R), IC50: 0.2 nM; EGFR (exon 19Del), IC50: 0.2 nM; EGFR (WT), IC50: 0.3 nM
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。

Selective EGFR, IC50: 370 pM
S7039 PD168393

PD168393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。

Selective EGFR, IC50: 0.70 nM
S1170 WZ3146

WZ3146是一种突变选择性的,不可逆EGFR(L858R)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。

Selective EGFR (E746_A750/T790M), IC50: 14 nM; EGFR (L858R/T790M), IC50: 5 nM; EGFR (L858R), IC50: 2 nM; EGFR (E746_A750), IC50: 2 nM
S7786 Erlotinib (OSI-774)

Erlotinib 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。

Selective EGFR, IC50: 2 nM
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。

Selective HER1/EGFR, IC50: 2 nM
S1173 WZ4002

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。

Selective EGFR (L858R/T790M), IC50: 8 nM; EGFR (L858R), IC50: 2 nM
S2205 OSI-420

OSI-420是Erlotinib的活性代谢产物(是一种EGFR抑制剂,IC50为2 nM)。

Selective EGFR, IC50: 2 nM
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。

Selective EGFR, IC50: 3 nM
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。Phase 2/3。

Selective EGFR, IC50: 66 nM; EGFR (L858R), IC50: 5 nM; EGFR (L861Q), IC50: 4 nM
S2867 WHI-P154

WHI-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。

Selective EGFR, IC50: 4 nM
S2922 Icotinib (BPI-2009H)

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)。Phase 4。

Selective EGFR, IC50: 5 nM
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。

Selective WT EGFR, IC50: 493.8 nM; L858R/T790M EGFR, IC50: 11.44 nM; Exon 19 deletion EGFR, IC50: 12.92 nM
S0070 Gefitinib-based PROTAC 3

Gefitinib-based PROTAC 3 conjugates an EGFR binding element to a VHL ligand via a linker and induces EGFR degradation with DC50 of 11.7 nM and 22.3 nM in HCC827(exon 19 del) and H3255 (L858R mutantion) cells, respectively.

Selective EGFR, DC50: 22.3 nM; EGFR, DC50: 11.7 nM
S5098 Gefitinib hydrochloride

Gefitinib (ZD1839) is an EGFR inhibitor with IC50s of 15.5 nM and 823.3 nM for WT EGFR and EGFR (858R/T790M), respectively.

Selective EGFR, IC50: 15.5 nM
S0360 EGFR Inhibitor

EGFR inhibitor is an inhibitor of EGFR that directly depolymerizes microtubules. EGFR inhibitor is used as a chemical probe to investigate both the EGFR pathway and microtubule dynamics.

Selective EGFR, IC50: 21 nM
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EGFRWTKi分别为21.5 nM和303.3 nM。Phase 2。

Selective EGFR (wt), Ki: 303.3 nM; EGFR (L858R/T790M), Ki: 21.5 nM
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。

Selective Tyr992 (NR6W cells), IC50: 57 nM; Tyr992 (NR6wtEGFR cells), IC50: 37 nM; Tyr1173 (NR6W cells), IC50: 26 nM; Tyr1173 (NR6wtEGFR cells), IC50: 37 nM
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。

Selective EGFR, IC50: 29 nM
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。

Selective EGFR, IC50: 38.5 nM
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。

Selective EGFR, IC50: 0.1 μM
S1046 Vandetanib (ZD6474)

Vandetanib (ZD6474)是一种有效的VEGFR2抑制剂,在无细胞试验中IC50为40 nM。同时,也抑制VEGFR3EGFR,IC50分别为110 nM 和500 nM。对PDGFRβ, Flt-1, Tie-2 和FGFR1作用效果不大,IC50为 1.1-3.6 μM, 对MEK, CDK2, c-Kit, erbB2, FAK, PDK1, Akt 和 IGF-1R几乎没有作用效果,IC50>10 μM。

Selective EGFR, IC50: 500 nM
S6525 AG 555

AG-555 (Tyrphostin B46) is an inhibitor of tyrosine kinase, interacts directly with topoisomerase I, thus preventing DNA relaxation. It inhibits EGFR with an IC50 of 0.7 μM.

Selective EGFR, IC50: 0.7 μM
S6509 AG 494

AG-494, a member of the tyrphostin family of tyrosine kinase inhibitors, is a potent inhibitor of EGF receptor autophosphorylation (IC50=1.2 μM) and EGF-dependent cell growth (IC50=6 μM).

Selective EGFR, IC50: 1.2 μM
S2115 RG 13022

RG 13022 (Tyrphostin RG13022) inhibits the autophosphorylation reaction of the EGF receptor in immunoprecipitates with IC50 of 4 µM.

Selective EGFR, IC50: 4 μM
S2554 Daphnetin

Daphnetin是天然香豆素衍生物,是一种蛋白激酶抑制剂,抑制EGFRPKA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。

Selective EGFR, IC50: 7.67 μM
S8009 AG-18

AG-18抑制EGFRIC50为35 μM。

Selective EGFR, IC50: 35 μM
S6809 SU5214

SU5214 is a inhibitor of VEGF receptor 2 (VEGFR2/FLK-1) with IC50 of 14.8 µM and EGFR with IC50 of 36.7 µm, respectively.

Selective EGFR, IC50: 36.7 μM
S2895 Tyrphostin 9

Tyrphostin 9 是第一个EGFR抑制剂,IC50为460 μM,作用于PDGFR更有效,IC50为0.5μM。

Selective EGFR, IC50: 460 μM
S6899 Licochalcone D

Licochalcone D (Lico D, LCD, LD), a flavonoid isolated from a Chinese medicinal plant Glycyrrhiza inflata, has antioxidant, anti-inflammatory and anti-cancer properties. Licochalcone D inhibit phosphorylation of NF-κB p65 in LPS signaling pathway. Licochalcone D inhibits JAK2, EGFR and Met (c-Met) activities and induces ROS-dependent apoptosis. Licochalcone D also induces caspases activation and poly (ADP-ribose) polymerase (PARP) cleavage.

Selective
S4667 Lidocaine hydrochloride

Lidocaine hydrochloride是一种局部麻醉剂及心脏抑制剂,被用作抗心律失常剂。

Selective
S1054 AG99

AG99 (Tyrphostin 46,Tyrphostin A46,Tyrphostin B40) is a potent and selective inhibitor of EGFR.

Selective
S1179 WZ8040

WZ8040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。

Selective
S5078 Osimertinib mesylate

Osimertinib mesylate (AZD9291) is the mesylate form of osimertinib, which is an oral, third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) drug.

Selective
S6868 Alflutinib (AST2818) mesylate

Alflutinib is an inhibitor of EGFR that targets both EGFR activating mutations and T790M, thus leading to tumor growth inhibition.

Selective
S8920 (Rac)-JBJ-04-125-02

JBJ-04-125-02 is a mutant-selective allosteric inhibitor of EGFR.

Selective
S8036 Butein

Butein,一种从漆树中分离的植物多酚,可以抑制酪氨酸激酶NF-κBSTAT3EGFR活化。

Selective
S9414 Cyasterone

Cyasterone is the main phytoecdysteroid component found in Cyathula capitata. It is a natural EGFR inhibitor and maybe a promising anti-cancer agent.

Selective
S3759 Norcantharidin

Norcantharidin (Endothall anhydride) is a synthetic anticancer compound which is a dual inhibitor for c-Met and EGFR in human colon cancers.

Selective
S6541 MTX-211

MTX-211 is a first-in-class dual inhibitor of PI3K and EGFR kinase.

Selective
S2406 Chrysophanic Acid

Chrysophanic Acid是Dianella longifolia中的一种天然蒽醌,是一种EGFR/mTOR通道抑制剂。

Selective
S6523 RG14620

RG14620 (Tyrphostin RG14620), an EGFR inhibitor of the tyrphostin family, directly inhibits the transport function of ABCG2/BCRP.

Selective
S1342 Genistein (NPI 031L)

Genistein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。

Selective
S9711 CH7233163

CH7233163 is a non-covalent ATP competitive inhibitor of EGFR-tyrosine kinase with antitumor activities against tumor with EGFR-Del19/T790M/C797S.

Selective
S0151 AG-1557

AG1557 is a specific and ATP competitive inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase with pIC50 of 8.194.

Selective
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。

Pan
S9786 BDTX-189

BDTX-189 is a potent and selective inhibitor of allosteric EGFR and HER2 oncogenic mutations with Kd of 0.2 nM, 0.76 nM, 13 nM and 1.2 nM for EGFR, HER2, BLK and RIPK2, reapectively. BDTX-189 exhibits anticancer activity.

Pan EGFR, Kd: 0.2 nM
S7810 Afatinib (BIBW2992) Dimaleate

Afatinib (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。

Pan EGFR (L858R/T790M), IC50: 10 nM; EGFR (wt), IC50: 0.5 nM; EGFR (L858R), IC50: 0.4 nM
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。

Pan EGFR (L858R/T790M), IC50: 10 nM; EGFR (L858R), IC50: 0.4 nM; EGFR (wt), IC50: 0.5 nM
S2185 Allitinib (AST-1306)

AST-1306是一种新型,不可逆的EGFRErbB2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。

Pan EGFR (T790M/L858R), IC50: 12 nM; EGFR, IC50: 0.5 nM
S7298 AZ5104

AZ5104,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。

Pan EGFR (wildtype), IC50: 25 nM; EGFR (L861Q) , IC50: 1 nM; EGFR (L858R), IC50: 6 nM; EGFR (L858R/T790M), IC50: <1 nM
S6897 Epertinib hydrochloride

Epertinib hydrochloride (S-222611 hydrochloride) is a potent, orally active, reversible, and selective tyrosine kinase inhibitor of EGFR, HER2 and HER4 with IC50 of 1.48 nM, 7.15 nM and 2.49 nM, respectively. Epertinib hydrochloride (S-222611 hydrochloride) exhibits antitumor activity.

Pan EGFR, IC50: 1.48 nM
S1019 Canertinib (CI-1033)

Canertinib (CI-1033)是一种泛ErbB抑制剂,作用于EGFRErbB2IC50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。

Pan EGFR, IC50: 1.5 nM
S1486 AEE788 (NVP-AEE788)

AEE788 (NVP-AEE788)是一种有效的EGFRHER2/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。

Pan EGFR, IC50: 2 nM
S8724 Lazertinib

Lazertinib (YH25448,GNS-1480) is a potent, highly mutant-selective and irreversible EGFR-TKI with IC50 values of 1.7 nM, 2 nM, 5 nM, 20.6 nM and 76 nM for Del19/T790M, L858R/T790M, Del19, L85R and Wild type EGFR respectively, showing much higher IC50 values aganist ErbB2 and ErbB4.

Pan WT EGFR, IC50: 76 nM; L858R/T790M EGFR, IC50: 2 nM
S1194 CUDC-101

CUDC-101是一种有效的,多靶点抑制剂,作用于HDACEGFR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。

Pan EGFR, IC50: 2.4 nM
S8584 Theliatinib (HMPL-309)

Theliatinib (HMPL-309) is a highly potent EGFR inhibitor with Ki value of 0.05 nM against the wild type EGFR and IC50 values of 3 nM and 22 nM against EGFR and EGFR T790M/L858R mutant. It demonstrats 50 fold greater selectivity for EGFR compared to 72 other kinases.

Pan WT EGFR, IC50: 3 nM
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。

Pan HER1, IC50: 3.2 nM
S2192 Sapitinib (AZD8931)

Sapitinib (AZD8931)是一种可逆的,ATP竞争性EGFRErbB2ErbB3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。

Pan EGFR, IC50: 4 nM
S8814 TAS6417

TAS6417 (CLN-081, TPC-064) is a novel EGFR inhibitor that targets EGFR exon 20 insertion mutations while sparing wild-type (WT) EGFR. IC50 values ranges from 1.1 ± 0.1 to 8.0 ± 1.1 nmol/L.

Pan EGFR WT, IC50: 8 nM; EGFR (L861Q), IC50: 5.5 nM; EGFR (T790M), IC50: 4.1 nM
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,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。

Pan EGFR, IC50: 6.0 nM
S6881 JND3229

JND3229 is a potent reversible inhibitor of EGFRC797S with an IC50 value of 5.8 nM. JND3229 also potently suppresses EGFRL858R/T790M and EGFRWT with IC50 values of 30.5 nM and 6.8 nM, respectively.

Pan EGFR WT, IC50: 6.8 nM
S2755 Varlitinib

Varlitinib是一种有效的,选择性ErbB1(EGFR)ErbB2(HER2)抑制剂,IC50分别为7 nM和2 nM。Phase 2。

Pan ErbB1, IC50: 7 nM
S0711 Canertinib dihydrochloride

Canertinib dihydrochloride is a potent and irreversible EGFR inhibitor. Canertinib dihydrochloride inhibits cellular EGFR and ErbB2 autophosphorylation with IC50 of 7.4 nM and 9 nM, respectively.

Pan EGFR, IC50: 7.4 nM
S2111 Lapatinib (GW-572016)

Lapatinib,以 Lapatinib Ditosylate的形式使用,是一种有效的EGFRErbB2抑制剂,在无细胞试验中IC50分别为10.2和9.8 nM。

Pan EGFR, IC50: 10.8 nM
S1028 Lapatinib (GW-572016) Ditosylate

Lapatinib (GW-572016) Ditosylate是一种有效的EGFRErbB2抑制剂,在无细胞试验中IC50分别为10.8和9.2 nM。

Pan EGFR, IC50: 10.8 nM
S8852 Pyrotinib (SHR-1258) dimaleate

Pyrotinib (SHR-1258, BLTN, Pyrroltinib) dimaleate is a potent and selective irreversible dual tyrosine kinase inhibitor of EGFR and HER2 with IC50 of 0.013 μM and 0.038 μM, respectively.

Pan EGFR, IC50: 0.013 μM
S7206 CNX-2006

CNX-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。

Pan mutant EGFR, IC50: <20 nM
S1056 AC480 (BMS-599626)

AC480 (BMS-599626)是一种选择性的,高效效的HER1HER2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。

Pan HER1, IC50: 20 nM
S2784 TAK-285

TAK-285是一种新型,HER2EGFR(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。

Pan EGFR/HER1, IC50: 23 nM
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。

Pan mutant EGFR, Ki: 0.031 μM
S2150 Neratinib (HKI-272)

Neratinib (HKI-272)是一种高度选择性的HER2EGFR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。

Pan EGFR, IC50: 92 nM
S6805 Tyrphostin AG-528

Tyrphostin AG-528 (Tyrphostin B66) is a potent inhibitor of epidermal growth factor receptors (EGFR) and ErbB2/HER2 with IC50 of 4.9 μM and 2.1 μM, respectively. Tyrphostin AG-528 exhibits anticancer activity.

Pan EGFR, IC50: 4.9 μM
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。

Pan
S6813 Mobocertinib (TAK788)

Mobocertinib (TAK788, AP32788), an investigational TKI, is a potent, selective preclinical inhibitor of epidermal growth factor receptor (EGFR) and HER2 mutations. Mobocertinib (TAK788) is an antineoplastic agent.

Pan
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telomeraseDNA methyltransferase, 阻滞EGF受体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。

Pan