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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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 -
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 -
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 -
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 -
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 -
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 -
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 -
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 -
AG-18 (Tyrphostin 23)
Catalog No. A15940 -
DM1-SMCC
Catalog No. A15955 -
Lapatinib Ditosylate
Catalog No. A10514 -
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 -
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