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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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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最新产品
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 -
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 -
Nazartinib mesylate
Catalog No. A21741 covalent mutant-selective EGFR inhibitorNazartinib mesylate (EGF816 mesylate) is a novel, covalent mutant-selective EGFR inhibitor, with Ki and Kinact of 31 nM and 0.222 min?1 on EGFR(L858R/790M) mutant, respectively. 了解更多 -
Nazartinib S-enantiomer
Catalog No. A21747 EGFR inhibitorNazartinib S-enantiomer (EGF816 S-enantiomer) is the less active S-enantiomer of Nazartinib. Nazartinib (EGF816) is an EGFR inhibitor. 了解更多 -
Pyrotinib dimaleate
Catalog No. A21756 EGFR/HER2 dual inhibitorPyrotinib dimaleate (SHR-1258 dimaleate) is a potent and selective EGFR/HER2 dual inhibitor with IC50 s of 13 and 38 nM, respectively. 了解更多 -
Epertinib hydrochloride
Catalog No. A21950 EGFR, HER2 and HER4 inhibitorEpertinib hydrochloride is a potent, orally active, reversible, and selective tyrosine kinase inhibitor of EGFR, HER2 and HER4, with IC50s of 1.48 nM, 7.15 nM and 2.49 nM, respectively. Epertinib shows potent antitumor activity. 了解更多 -
Lifirafenib
Catalog No. A20988 Raf/EGFR inhibitorLifirafenib (BGB-283) is a novel and potent Raf Kinase and EGFR inhibitor with IC50 values of 23 and 29 nM for recombinant BRafV600E and EGFR, respectively. 了解更多 -
Pelitinib (EKB-569)
Catalog No. A10706 EGFR 抑制剂Pelitinib (EKB-569)是一种有效的,不可逆EGFR抑制剂,IC50为38.5 nM 了解更多 -
Neratinib (HKI-272)
Catalog No. A10638 -
Canertinib (CI-1033)
Catalog No. A10211 HER2/ErbB2 抑制剂Canertinib (CI-1033)是一种不可逆的酪氨酸激酶抑制剂,对EGFR(IC50 0.8 nM),HER-2(IC50 19 nM)和ErbB-4(IC50 7 nM)具有活性。 了解更多 -
BIBW2992 (Afatinib)
Catalog No. A10141 EGFR 抑制剂BIBW2992 (Afatinib)是酪氨酸激酶抑制剂(TKI),它不可逆地抑制人表皮生长因子受体2(Her2)和表皮生长因子受体(EGFR)激酶。 了解更多 -
AZD8931 (Sapitinib)
Catalog No. A10116 pan-EGFR/pan-erbB 抑制剂AZD8931 (Sapitinib)是ErbB1,ErbB2和ErbB3受体信号传导的等效抑制剂。 了解更多 -
Gefitinib (Iressa)
Catalog No. A10422 EGFR 抑制剂Gefitinib (Iressa)是一种EGFR抑制剂,可阻断靶细胞中表皮生长因子受体(EGFR)的信号传导。 了解更多 -
Erlotinib HCl
Catalog No. A10362 EGFR 抑制剂Erlotinib hydrochloride是一种可逆的酪氨酸激酶抑制剂,作用于表皮生长因子受体(EGFR)。 了解更多 -
Lapatinib Ditosylate
Catalog No. A10514 -
AG-1478 (Tyrphostin AG-1478)
Catalog No. A11022 EGFR 抑制剂AG-1478 (Tyrphostin AG-1478)是EGFR激酶的抑制剂,IC50值为3 nM。 了解更多 -
CUDC-101
Catalog No. A10246 -
WZ8040
Catalog No. A10992 -
WZ3146
Catalog No. A10990 -
PD153035 (HCl salt)
Catalog No. A10702 -
BMS 599626 (AC480)
Catalog No. A11209 EGFR 抑制剂BMS 599626 (AC480)是一种选择性的,高效效的HER1,HER2和HER4酪氨酸激酶抑制剂(IC50分别为22、32和190 nM),具有潜在的抗肿瘤活性。 了解更多 -
Arry-380 analog
Catalog No. A11027 HER2 抑制剂Arry-380 analog是一种ErbB-2抑制剂,可选择性结合并抑制ErbB-2的磷酸化,从而导致表达ErbB-2的肿瘤细胞的生长抑制和死亡。 了解更多 -
AEE788
Catalog No. A10043