EGFR/HER2
Inhibitory Selectivity
Catalog No. | Inhibitor Name | EGFR/ErbB1 | HER2/ErbB2 | ErbB3 | ErbB4 | Other |
---|---|---|---|---|---|---|
A10362 | Erlotinib HCl | **** | ||||
A10422 | Gefitinib | ** | ||||
A10514 | Lapatinib Ditosylate | ** | ** | * | c-Src | |
A10141 | Afatinib | **** | ** | |||
A10638 | Neratinib | * | * | KDR,Src | ||
A10211 | Canertinib | **** | *** | |||
A11752 | Lapatinib | ** | ** | * | c-Src | |
A10047 | AG-490 | * | * | JAK2 | ||
A10242 | CP-724714 | ** | ||||
A11051 | Dacomitinib | *** | * | * | ||
A10991 | WZ4002 | **** | *** | |||
A10116 | Sapitinib | *** | *** | HDAC,HDAC1,HDAC6 | ||
A10246 | CUDC-101 | *** | ** | |||
A11022 | AG-1478 | *** | ||||
A10702 | PD153035 HCl | **** | Src,MEK/ERK,Raf | |||
A10706 | Pelitinib | * | * | c-Abl,FLT1,c-Fms | ||
A10043 | AEE788 | **** | *** | * | MEK,LCK,VEGFR2 | |
A11209 | AC480 | ** | * | * | ||
A10678 | OSI-420 | **** | ||||
A10990 | WZ3146 | **** | ||||
A11155 | AST-1306 | **** | *** | **** | ||
A13028 | Rociletinib | ** | ||||
A11158 | Varlitinib | *** | **** | |||
A13825 | Icotinib | *** | MEK1,Aurora B,LCK | |||
A11236 | TAK-285 | ** | ** | * | Src,VEGFR,JAK3 | |
A14049 | WHI-P154 | *** | ||||
A12725 | PD168393 | **** | ||||
A13755 | CNX-2006 | ** | PDGFR | |||
A11949 | Tyrphostin 9 | * | ||||
A15940 | AG-18 | * | ||||
A15551 | AZD3759 | **** | ||||
A14985 | Afatinib Dimaleate | **** | ** | |||
A13146 | CL-387785 | **** | ||||
A13044 | Poziotinib | *** | *** | ** | ||
A13681 | Osimertinib | ** | BLK,ACK1,BRK | |||
A15516 | AZ5104 | **** | *** | |||
A10992 | WZ8040 | topo II | ||||
A10426 | Genistein | |||||
A12448 | Butein | mTOR | ||||
A10210 | Chrysophanic Acid | |||||
A10053 | Tyrphostin AG 879 | * | Trk | |||
A10286 | Daphnetin | * | PKC, PKA | |||
A11027 | Irbinitinib (ARRY-380, ONT-380) | **** | ||||
A11028 | AV-412 | *** | * | |||
A11334 | BIBX 1382 | **** | * | |||
A12867 | CGP-52411 | * | ||||
A13588 | Tyrphostin AG 183 | * | ||||
A15509 | WHI-P180 | * | Cdk2 | |||
A10612 | Mubritinib (TAK 165) | **** | ||||
A16413 | ARRY-380 (Irbinitinib) | **** |
Notes:
1.Hover mouse over " " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.
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Poziotinib
Catalog No. A13044 EGFR 抑制剂Poziotinib是一种口服生物利用的,基于喹唑啉的泛表皮生长因子受体(EGFR或HER)抑制剂,具有潜在的抗肿瘤活性。 了解更多 -
EGFR Inhibitor
Catalog No. A13673 EGFR 抑制剂EGFR inhibitor是一种可透过细胞的4,6-二取代嘧啶化合物,可选择性抑制EGFR激酶,在体外的IC50值为21 nM,可阻断细胞中的受体自身磷酸化。 了解更多 -
Epidermal Growth Factor Receptor Peptide (985-996)
Catalog No. A14877 Epidermal Growth Factor Receptor Peptide (985-996)存在于细胞表面,并通过其特定配体(包括表皮生长因子和转化生长因子)的结合而被激活。 了解更多 -
Compound 56
Catalog No. A14953 -
Afatinib dimaleate
Catalog No. A14985 -
Erlotinib mesylate
Catalog No. A15081 -
Gefitinib hydrochloride
Catalog No. A15093 EGFR 抑制剂Gefitinib hydrochloride是一种EGFR抑制剂,可通过靶细胞中的表皮生长因子受体(EGFR)中断信号传导。因此,它仅在EGFR突变和过度活跃的癌症中有效。 了解更多 -
Vandetanib trifluoroacetate
Catalog No. A15272 -
WHI-P180
Catalog No. A15509 -
D-69491
Catalog No. A15457 -
AZD3759
Catalog No. A15551 -
ASP8273 (Naquotinib)
Catalog No. A14408 irreversible EGFR 抑制剂ASP8273 (Naquotinib)是不可逆的,第三代,选择性突变的表皮生长因子受体(EGFR)抑制剂,具有潜在的抗肿瘤活性。 了解更多 -
EGF816 (Nazartinib)
Catalog No. A14416 -
CL-387785 (EKI-785)
Catalog No. A13146 -
AG-18 (Tyrphostin 23)
Catalog No. A15940 -
DM1-SMCC
Catalog No. A15955 -
PD168393
Catalog No. A12725 -
EAI045
Catalog No. A16193 -
PD158780
Catalog No. A16254 -
ARRY-380 (Irbinitinib)
Catalog No. A16413 -
Avitinib (AC0010)
Catalog No. A16826 irreversible EGFR 抑制剂Avitinib (AC0010)是一种基于吡咯并嘧啶的不可逆EGFR抑制剂,对EGFR L858R/T790M双重突变具有突变选择性,IC50值为0.18 nM,效力比野生型EGFR(IC50值为7.68 nM)高近43倍。它具有可比的抗肿瘤活性和耐受的毒性。 了解更多 -
Lazertinib (YH25448,GNS-1480)
Catalog No. A16827 EGFR 抑制剂Lazertinib (YH25448,GNS-1480)是一种有效的,高度突变选择性和不可逆的EGFR-TKI,对于Del19/T790M,L858R/T790M,Del19,Del19,IC50值分别为1.7 nM,2 nM,5 nM,20.6 nM和76 nM。L85R和野生型EGFR分别显示出更高的IC50值,即抗药性ErbB2和ErbB4。 了解更多 -
Tyrphostin AG-528
Catalog No. A17072 -
Pyrotinib Racemate
Catalog No. A17068 -
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AG-494
Catalog No. A17142 -
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Lavendustin A
Catalog No. A17119 -
RG14620
Catalog No. A18327 -
Mutated EGFR-IN-2
Catalog No. A18565 EGFR 抑制剂Mutated EGFR-IN-2 (compound 91) is a mutant-selective EGFR inhibitor extracted from patent WO2017036263A1, which potently inhibits single-mutant EGFR (T790M) and double-mutant EGFR (including L858R/T790M (IC50=??1nM) and ex19del/T790M), and can suppress activity of single gain-of-function mutant EGFR (including L858R and ex19del) as well. Mutated EGFR-IN-2 shows anti-tumor antivity. 了解更多 -
NSC 228155
Catalog No. A16638 EGFR activatorNSC 228155 is an activator of EGFR, binds to the extracellular region of EGFR and enhance tyrosine phosphorylation of EGFR. 了解更多 -
CHMFL-EGFR-202
Catalog No. A12524 EGFR inhibitorCHMFL-EGFR-202 is a potent, irreversible inhibitor of epidermal growth factor receptor (EGFR) mutant kinase, with IC50s of 5.3 nM and 8.3 nM for drug-resistant mutant EGFR T790M and WT EGFR kinases, respectively. 了解更多 -
EGFR-IN-3
Catalog No. A15847 -
Canertinib dihydrochloride
Catalog No. A11344 EGFR inhibitorCanertinib dihydrochloride (CI-1033 dihydrochloride) is a potent and irreversible EGFR inhibitor; inhibits cellular EGFR and ErbB2 autophosphorylation with IC50s of 7.4 and 9 nM. 了解更多 -
Tarloxotinib bromide
Catalog No. A20849 EGFR/HER2 inhibitorTarloxotinib bromide (TH-4000) is an irreversible EGFR/HER2 inhibitor. 了解更多 -
Mutant EGFR inhibitor
Catalog No. A21144 EGFR inhibitorMutant EGFR inhibitor is a potent and selective mutant EGFR inhibitor extracted from patent WO 2013014448 A1; inhibits EGFRL858R, EGFRExon 19 deletion and EGFRT790M. 了解更多 -
HS-10296 hydrochloride
Catalog No. A21661 EGFR/T790M inhibitorHS-10296 hydrochloride is an orally available and third-Generation inhibitor of epidermal growth factor receptor (EGFR)-activating mutations and T790M-resistant mutation with limited activity against wild-type EGFR. 了解更多 -
AST2818 mesylate
Catalog No. A21666