EGFR/HER2
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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Neratinib (HKI-272)
Catalog No. A10638 -
Lapatinib Ditosylate
Catalog No. A10514 -
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 -
Chrysophanic acid (Chrysophanol)
Catalog No. A10210 -
XL647 (Tesevatinib)
Catalog No. A11057 EGFR, HER2 and VEGFR 抑制剂XL647 (Tesevatinib)是一种口服生物可利用的小分子RTK抑制剂,可结合并抑制在肿瘤细胞增殖和肿瘤血管形成中起主要作用的几种酪氨酸受体激酶,包括EGFR,HER2,ERBB2,VEGFR和EphB4。 了解更多 -
Mubritinib (TAK 165)
Catalog No. A10612 HER2/ErbB2 抑制剂Mubritinib (TAK 165)是一种有效的EGFR和p34cdc2抑制剂,IC50分别为6 nM和0.2 ?M。Mubritinib(TAK 165)也抑制p33cdk2和p33cdk5。 了解更多 -
Tyrphostin AG 879
Catalog No. A10053 -
BIBX 1382
Catalog No. A11334 -
AG-17
Catalog No. A11949 -
ARRY-543 (Varlitinib, ASLAN001)
Catalog No. A12868 ErbB 抑制剂ARRY-543 (Varlitinib,ASLAN001)是一种新型口服ErbB家族抑制剂,与批准的ErbB抑制剂不同,它直接或间接靶向ErbB家族的所有成员,包括ErbB3,在治疗通过多个ErbB家族成员发出信号的肿瘤方面具有潜在优势。 了解更多 -
CO-1686 (Rociletinib, AVL-301)
Catalog No. A13028 EGFR 抑制剂CO-1686是一种新型的口服靶向共价(不可逆)抑制剂,可抑制表皮生长因子受体(EGFR)的致癌突变形式,目前正在研究用于治疗非小细胞肺癌(NSCLC)。 了解更多 -
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 -
Compound 56
Catalog No. A14953 -
D-69491
Catalog No. A15457 -
CL-387785 (EKI-785)
Catalog No. A13146 -
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