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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Chrysophanic acid (Chrysophanol)
Catalog No. A10210 -
PF299804 (Dacomitinib, PF299)
Catalog No. A11051 EGFR 抑制剂PF299804是一种有效的,可口服的酪氨酸激酶人表皮生长因子受体(HER)1(EGFR),HER2和HER4不可逆抑制剂。 了解更多 -
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 -
ARRY334543 (Varlitinib)
Catalog No. A11158 EGFR 抑制剂ARRY334543 (Varlitinib)是一种有效的EGFR和ErbB-2口服活性小分子抑制剂。 了解更多 -
BMS-690514
Catalog No. A11263 -
Tyrphostin AG 879
Catalog No. A10053 -
BIBX 1382
Catalog No. A11334 -
AG-17
Catalog No. A11949 -
PKC 412 (Midostaurin)
Catalog No. A12650 PKC 抑制剂PKC 412 (Midostaurin)是一种广谱蛋白激酶抑制剂。抑制常规PKC亚型α/β/γ,PDFRβ,VEGFR2,Syk,Flk-1,Flt3,Cdk1/B,PKA,c-Kit,c-Fgr,c-Src,VEGFR1和EGFR。显示有效的抗肿瘤活性。 了解更多 -
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 -
Icotinib Hydrochloride
Catalog No. A13718 EGFR 抑制剂Icotinib hydrochloride是一种有效的特异性表皮生长因子受体(EGFR)酪氨酸激酶抑制剂(TKI),IC(50)为5 nM,包括EGFR(L858R),EGFR(L861Q),EGFR(T790M)和EGFR的突变体(T790M,L858R)。 了解更多 -
AZD-9291 (Osimertinib)
Catalog No. A13681 EGFR 抑制剂AZD-9291 (Osimertinib)是第三代EGFR抑制剂,在临床前研究中显示出希望,并为已对现有EGFR抑制剂产生耐药性的晚期肺癌患者提供了希望。 了解更多 -
Tyrphostin AG 183
Catalog No. A13588 -
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 -
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