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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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 -
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 -
(-)-Epigallocatechin gallate
Catalog No. A10005 Antioxidant, antiangiogenic, antitumor agent(-)-Epigallocatechin gallate是一种从绿茶中分离出来的强效抗氧化剂多酚类黄酮。 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 -
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 -
Genistin (Genistoside)
Catalog No. A10426 Genistin (Genistoside)是一种异黄酮,存在于许多饮食植物中,如大豆和葛根。显示出刺激体内雌激素依赖性乳腺癌细胞生长。 了解更多 -
BMS-690514
Catalog No. A11263 -
Lapatinib (free base)
Catalog No. A11752 Lapatinib (free base)是一种双重酪氨酸激酶抑制剂,是一种有效的EGFR和ErbB2抑制剂,在无细胞试验中IC50分别为10.2和9.8 nM。可阻断HER2生长受体途径。 了解更多 -
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