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EGFR/HER2 inhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	EGFR (71) Akt (4) Apoptosis (11) Autophagy (6) Btk (3) c-Met/HGFR (5) CDK (6) Dihydrofolate reductase (DHFR) (3) ERK (1) HDAC (1) Isotope-Labeled Compounds (1) Itk (1) JAK (1) Necroptosis (1) p38 MAPK (3) PARP (1) PI4K (1) Potassium Channel (1) Raf (1) Survivin (1) Thymidylate Synthase (2) Trk Receptor (1) VEGFR (3)
By Research Areas:	Cancer (72) Cardiovascular Disease (1)
Click Chemistry:	Alkynes (1)

Inhibitors & Agonists

Screening Libraries

Inhibitory Antibodies

Isotope-Labeled Compounds

Click Chemistry

Targets Recommended: EGFR

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-153111

EGFR/HER2-IN-9

EGFR Cancer

EGFR/HER2-IN-9 (Compound 1) is an EGFR and HER2 inhibitor with IC₅₀s of 3.2, 8.3 and 14 nM against EGFR, EGFR T790M and HER2, respectively .

EGFR/HER2-IN-9	EGFR	Cancer
EGFR/HER2-IN-9 (Compound 1) is an *EGFR* and *HER2* inhibitor with IC₅₀s of 3.2, 8.3 and 14 nM against EGFR, EGFR T790M and HER2, respectively .

HY-151161

EGFR/HER2-IN-8	EGFR	Cancer
EGFR/HER2-IN-8 (compound 34) is a *EGFR/HER2* and DHFR inhibitor. EGFR/HER2-IN-8 inhibits EGFR kinase, HER2 kinase and DHFR with IC₅₀s of 0.45, 0.244 and 5.669 μM, respectively. EGFR/HER2-IN-8 shows anticancer activity against several cancer cell lines with high safety profile and selectivity indices. EGFR/HER2-IN-8 can be used for the research of cancer .

HY-151156

EGFR/HER2-IN-6	EGFR Apoptosis	Cancer
EGFR/HER2-IN-6 (compound 43) is an *EGFR/HER2* and DHFR inhibitor. EGFR/HER2-IN-6 inhibits EGFR kinase, HER2 kinase and DHFR with IC₅₀s of 0.122, 0.078 and 0.585 μM, respectively. EGFR/HER2-IN-6 shows anticancer activity against several cancer cell lines with high safety profile and selectivity indices. EGFR/HER2-IN-8 can be used for the research of cancer .

HY-157399

EGFR/HER2-IN-10	EGFR	Cancer
EGFR/HER2-IN-10 (compound 9F) is a potent and selective dual *EGFR/HER2* inhibitor with IC₅₀s of 2.3 nM and 234 nM for EGFR and HER2, respectively. EGFR/HER2-IN-10 shows an effective antiproliferative action against prostate carcinoma .

HY-115952

EGFR/HER2-IN-3

EGFR Cancer

EGFR/HER2-IN-3 (Compound ZINC21942954) is a dual inhibitor of EGFR and HER2 .

EGFR/HER2-IN-3	EGFR	Cancer
EGFR/HER2-IN-3 (Compound ZINC21942954) is a dual inhibitor of *EGFR* and *HER2* .

HY-115951

EGFR/HER2-IN-2	EGFR	Cancer
EGFR/HER2-IN-2 (Compound ZINC35560729) is a dual inhibitor of *EGFR* and *HER2* with IC₅₀ values of 5.02 µM and 0.83 µM against EGFR and HER2, respectively .

HY-153557

HER2-IN-13

EGFR Potassium Channel Cancer

HER2-IN-13 (Compound 33) is an HER2 inhibitor with an IC₅₀ of 8 nM. HER2-IN-13 also inhibits wt-EGFR with an IC₅₀ of 0.40 μM .
HY-153557A

HER2-IN-14

EGFR Cancer

HER2-IN-14 (Compound 34) is an HER2 inhibitor with an IC₅₀ of 18 nM. HER2-IN-14 also inhibits wt-EGFR with an IC₅₀ of 6.3 μM .

HER2-IN-13	EGFR Potassium Channel	Cancer
HER2-IN-13 (Compound 33) is an *HER2* inhibitor with an IC₅₀ of 8 nM. HER2-IN-13 also inhibits *wt-EGFR* with an IC₅₀ of 0.40 μM .

HER2-IN-14	EGFR	Cancer
HER2-IN-14 (Compound 34) is an *HER2* inhibitor with an IC₅₀ of 18 nM. HER2-IN-14 also inhibits *wt-EGFR* with an IC₅₀ of 6.3 μM .

HY-146238

EGFR/HER2/TS-IN-1	EGFR Thymidylate Synthase Apoptosis	Cancer
EGFR/HER2/TS-IN-1 (Compound 4d) is an *EGFR, HER2* and TS (Thymidylate synthase) inhibitor with IC₅₀ values of 0.203, 0.088 and 0.168 μM against EGFR, HER2 and TS, respectively. EGFR/HER2/TS-IN-1 induces MCF7 cell apoptosis .

HY-151158

EGFR/HER2-IN-7	EGFR	Cancer
EGFR/HER2-IN-7 is a potent anticancer agent with high selectivity against MCF-7 breast cancer cells. EGFR/HER2-IN-7 is a *EGFR/HER2* kinase and DHFR inhibitor, with IC₅₀s of 0.18 μM (EGFR), 0.146 μM (HER2), respectively. EGFR/HER2-IN-7 shows moderate inhibition on DHFR (IC₅₀=0.907 μM) .

HY-160682

EGFR/HER2-IN-12	EGFR	Others
EGFR/HER2-IN-12 (compound 14b) is a dual inhibitor of EGFR and HER2 with 81% and 51% inhibition at 10 μM. The toxicity of EGFR/HER2-IN-12 to cancer cells A431 and MDA-MB-361 was not significant .

HY-143734

HER2-IN-6	EGFR	Cancer
HER2-IN-6 is a potent inhibitor of *HER2. HER2-IN-6 has the potential for the research of wild and/or mutant EGFR* and/or HER2 kinase mediated tumor (extracted from patent WO2021164697A1, compound 11) .

HY-144053

EGFR-IN-36	EGFR	Cancer
EGFR-IN-36 is a potent *EGFR* inhibitor with IC₅₀s of 19.09 nM, 120.01 nM, 2.35 nM for EGFR (WT), HER2 (WT), HER2 (A775_G776insYVMA), respectively. EGFR-IN-36 has potential for wild and/or mutant EGFR and/or HER2 kinase mediated tumors research .

HY-149633

EGFR/HER2/DHFR-IN-3	EGFR Dihydrofolate reductase (DHFR) Apoptosis	Cancer
EGFR/HER2/DHFR-IN-3 (compound 4c) is a potent dual inhibitor of *EGFR/HER2, with IC₅₀s of 0.138 and 0.092 μM, respectively. EGFR/HER2/DHFR-IN-3 also inhibits* DHFR, with an IC₅₀ of 0.193 M. EGFR/HER2/DHFR-IN-3 causes arrest at the S phase of the cell cycle and induces apoptosis in MCF7 breast cancer cells .

HY-136789

Tuxobertinib BDTX-189	EGFR	Cancer
Tuxobertinib (BDTX-189) is a potent, orally active and selective inhibitor of allosteric *EGFR* and *HER2* oncogenic mutations, including EGFR/HER2 exon 20 insertion mutants. Tuxobertinib shows K_Ds of 0.2, 0.76, 13 and 1.2 nM for EGFR, HER2, BLK and RIPK2, reapectively. Anticancer activity .

HY-13501

Mubritinib

5+ Cited Publications

TAK-165
EGFR Cancer

Mubritinib (TAK-165) is a potent and selective EGFR2/HER2 inhibitor with an IC₅₀ of 6 nM.

Mubritinib 5+ Cited Publications TAK-165	EGFR	Cancer
Mubritinib (TAK-165) is a potent and selective *EGFR2/HER2* inhibitor with an IC₅₀ of 6 nM.

HY-147797

EGFR/HER2/CDK9-IN-2	EGFR CDK	Cancer
EGFR/HER2/CDK9-IN-2 (Compound 9) is a potent inhibitor of EGFR/HER2/CDK9 with IC₅₀*s of 145.35, 129.07, and 117.13 nM, respectively. EGFR/HER2/CDK9-IN-2 exhibits remarkable antitumor activity .*

HY-147798

EGFR/HER2/CDK9-IN-3	EGFR CDK	Cancer
EGFR/HER2/CDK9-IN-3 (Compound 10) is a potent inhibitor of EGFR/HER2/CDK9 with IC₅₀*s of 191.08, 132.65, and 113.98 nM, respectively. EGFR/HER2/CDK9-IN-3 exhibits remarkable antitumor activity .*

HY-147796

EGFR/HER2/CDK9-IN-1	EGFR CDK	Cancer
EGFR/HER2/CDK9-IN-1 (Compound 4) is a potent inhibitor of EGFR/HER2/CDK9 with IC₅₀*s of 90.17, 131.39, and 67.04 nM, respectively. EGFR/HER2/CDK9-IN-1 exhibits remarkable antitumor activity .*

HY-147992

EGFR/HER2-IN-4	EGFR	Cancer
EGFR/HER2-IN-4(compound 6d) is an orally active irreversible dual inhibitor. EGFR/HER2-IN-4 inhibits *EGFR* with an IC₅₀ value of 0.6 nM and demonstrates potent *EGFR* kinase inhibitory activities on L858R and T790M mutations. EGFR/HER2-IN-4 has potent antitumor efficacy in vivo and can be used for lung cancer research .

HY-147994

EGFR/HER2-IN-5	EGFR	Cancer
EGFR/HER2-IN-5 (compound 6h) is an orally active irreversible dual inhibitor. EGFR/HER2-IN-5 inhibits *EGFR* with an IC₅₀ value of 1.01 nM and demonstrates potent *EGFR* kinase inhibitory activities on L858R and T790M mutations. EGFR/HER2-IN-5 has potent antitumor efficacy in vivo and can be used for lung cancer research .

HY-137786

EGFR-IN-16

EGFR Cancer

EGFR-IN-16 (compound 3) is a potent EGFR inhibitor with pIC₅₀ of 4.85 and 4.74 for EGFR and HER-2, respectively .

EGFR-IN-16	EGFR	Cancer
EGFR-IN-16 (compound 3) is a potent *EGFR* inhibitor with pIC₅₀ of 4.85 and 4.74 for EGFR and HER-2, respectively .

HY-151154

EGFR/HER2/DHFR-IN-1	EGFR	Cancer
EGFR/HER2/DHFR-IN-1 is a potent anticancer agent with high selectivity against MCF-7 breast cancer cells. EGFR/HER2/DHFR-IN-1 is a multiple inhibitor of *EGFR/HER2* kinase and DHFR, with IC₅₀s of 0.153 μM, 0.108 μM, 0.291 μM, respectively. EGFR/HER2/DHFR-IN-1 arrests cell cycle at G1/S and induces cells apoptosis .

HY-160613

EGFR/HER2-IN-11	EGFR	Cancer
EGFR/HER2-IN-11 (compound 20) is an orally active dual inhibitor for human epidermal growth factor receptor 2 (HER2) and epidermal growth factor receptor (EGFR), with IC₅₀s of 7.7 and 22 nM, respectively. EGFR/HER2-IN-11 exhibits antitumor efficacy and inhibits proliferation against cancer cells BT-474 with GI₅₀ of 601 nM .

HY-156639

EGFR/ErbB-2 inhibitor-1

EGFR Cancer

EGFR/ErbB-2 inhibitor-1 is a ErbB2/HER2 inhibitor .

EGFR/ErbB-2 inhibitor-1	EGFR	Cancer
EGFR/ErbB-2 inhibitor-1 is a ErbB2/HER2 inhibitor .

HY-146239

EGFR/HER2/TS-IN-2	EGFR Thymidylate Synthase	Cancer
EGFR/HER2/TS-IN-2 (compound 17) is a potent *EGFR/HER2* and TS (Thymidylate synthase) inhibitor, with IC₅₀ values of 0.173, 0.125, and 1.12 μM, respectively. EGFR/HER2/TS-IN-2 shows cytotoxic activity against MDA-MB-231 cancer cell lines, with an IC₅₀ of 1.69 µM .

HY-143319

SPH5030	Others	Cancer
SPH5030 is a selective and irreversible *HER2* inhibitor. SPH5030 inhibits HER2 ^WT and EGFR ^WT with IC₅₀s of 3.51 and 8.13 nM, respectively. SPH5030 shows excellent activities against HER2 mutants. SPH5030 can be used for the research of cancer .

HY-17632

Tarloxotinib bromide

1 Publications Verification

TH-4000
EGFR Cancer

Tarloxotinib bromide (TH-4000) is an irreversible EGFR/HER2 inhibitor.

Tarloxotinib bromide 1 Publications Verification TH-4000	EGFR	Cancer
Tarloxotinib bromide (TH-4000) is an irreversible *EGFR/HER2* inhibitor.

HY-149632

EGFR/HER2/DHFR-IN-2	EGFR Dihydrofolate reductase (DHFR)	Cancer
EGFR/HER2/DHFR-IN-2 (Compound 4b) is an inhibitor of *EGFR, HER2, and DHFR* (IC₅₀: 0.248, 0.156, 0.138 μM respectively). EGFR/HER2/DHFR-IN-2 has anticancer activities against a panel of cancer cells (IC₅₀: 9.14, 7.33, 14.18, 24.87, 20.07, 6.16 μM for Hep G2, HeLa, HEp-2, HCT 116, PC-3, MCF7 cells). EGFR/HER2/DHFR-IN-2 reduce breast cancer tumor growth .

HY-163453

HER2-IN-19	EGFR	Cancer
HER2-IN-19 (Compound 10e) is a potent inhibitor of *HER2* and *EGFR* with IC₅₀ values of 0.87 respectively and 3.5 nM. HER2-IN-19 has potent inhibitory activity against tumor cells, IC₅₀ ^NCI-N87 = 1.63 nM, IC₅₀ ^BT474= 15.17 nM, IC₅₀ ^{BaF3-HER2YVMA} = 1.49 nM .

HY-108931

AG 1406

EGFR Cancer

AG 1406 (compound M19) is a HER2 inhibitor, with an IC₅₀ of 10.57 μM for HER2 in BT474 cell and >50 μM for EGFR in EGF-3T3 cell .

AG 1406	EGFR	Cancer
AG 1406 (compound M19) is a *HER2* inhibitor, with an IC₅₀ of 10.57 μM for HER2 in BT474 cell and >50 μM for EGFR in EGF-3T3 cell .

HY-112293

GW2974	EGFR	Cancer
GW2974 is a potent dual inhibitor of *EGFR* and *HER2* with IC₅₀ value of 0.007 μM and 0.016 μM, respectively. GW2974 demonstrates in vitro inhibition of the *EGFR* and *HER2* and inhibits the growth of tumor cell. GW2974 can be used for glioblastoma multiforme (GBM) disease research .

HY-157229

STX-721

EGFR Others

STX-721 is a mutant-selective inhibitor of EGFR and HER2 Exon 20 insertion (ex20ins) mutants .

STX-721	EGFR	Others
STX-721 is a mutant-selective inhibitor of EGFR and HER2 Exon 20 insertion (ex20ins) mutants .

HY-147303

Sacibertinib	Trk Receptor EGFR	Cancer
Sacibertinib is a tyrosine kinase (Trk) inhibitor with EC₅₀ value of 110 nM and 244 nM for *EGFR-TK* phosphorylation and *HER2*, respectively. Antineoplastic activity .

HY-132842

Sunvozertinib 1 Publications Verification DZD9008	EGFR Btk	Cancer
Sunvozertinib (DZD9008) is a potent ErbBs (EGFR, Her2, especially mutant forms) and BTK inhibitor. Sunvozertinib shows IC₅₀s of 20.4, 20.4, 1.1, 7.5, and 80.4 nM for EGFR exon 20 NPH insertion, EGFR exon 20 ASV insertion, EGFR L858R and T790M mutations, and Her2 Exon20 YVMA, and EGFR WT A431, respectively (patent WO2019149164A1, example 52) .

HY-104065

Pyrotinib

10+ Cited Publications

SHR-1258
EGFR Cancer

Pyrotinib (SHR-1258) is a potent and selective EGFR/HER2 dual inhibitor with IC₅₀s of 13 and 38 nM, respectively .
HY-104065A

(Rac)-Pyrotinib

(Rac)-SHR-1258
Others Cancer

(Rac)-Pyrotinib ((Rac)-SHR-1258) is the racemate of Pyrotinib (HY-104065). Pyrotinib is a potent and selective EGFR/HER2 dual inhibitor.

Pyrotinib 10+ Cited Publications SHR-1258	EGFR	Cancer
Pyrotinib (SHR-1258) is a potent and selective *EGFR/HER2* dual inhibitor with IC₅₀s of 13 and 38 nM, respectively .

(Rac)-Pyrotinib (Rac)-SHR-1258	Others	Cancer
(Rac)-Pyrotinib ((Rac)-SHR-1258) is the racemate of Pyrotinib (HY-104065). Pyrotinib is a potent and selective *EGFR/HER2* dual inhibitor.

HY-32721

Neratinib 15+ Cited Publications HKI-272	EGFR	Cancer
Neratinib (HKI-272) is an orally available, irreversible, highly selective *HER2* and *EGFR* inhibitor with IC₅₀s of 59 nM and 92 nM, respectively .

HY-32721B

Neratinib maleate 15+ Cited Publications HKI-272 maleate	EGFR	Cancer
Neratinib (HKI-272) maleate is an orally available, irreversible, highly selective *HER2* and *EGFR* inhibitor with IC₅₀s of 59 nM and 92 nM, respectively .

HY-146262

LDC0496	EGFR	Cancer
LDC0496 is a potent and selective *EGFR* inhibitor. LDC0496 possesses intense inhibitory potency toward EGFR and Her2 exon20 insertion mutations, as well as selectivity over wild type EGFR and within the kinome .

HY-104065B

Pyrotinib dimaleate 10+ Cited Publications SHR-1258 dimaleate	EGFR	Cancer
Pyrotinib dimaleate (SHR-1258 dimaleate) is a potent and selective *EGFR/HER2* dual inhibitor with IC₅₀s of 13 and 38 nM, respectively .

HY-10261

Afatinib Maximum Cited Publications 53 Publications Verification BIBW 2992	EGFR Autophagy Apoptosis c-Met/HGFR Akt p38 MAPK	Cancer
Afatinib (BIBW 2992) is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and *HER2), with IC₅₀* values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR ^wt, EGFR ^L858R, EGFR ^L858R/T790M and HER2, respectively. Afatinib can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .

HY-10261A

Afatinib dimaleate Maximum Cited Publications 53 Publications Verification BIBW 2992MA2	EGFR Autophagy Apoptosis c-Met/HGFR Akt p38 MAPK	Cancer
Afatinib (BIBW 2992) dimaleate is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and *HER2), with IC₅₀* values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR ^wt, EGFR ^L858R, EGFR ^L858R/T790M and HER2, respectively. Afatinib dimaleate can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .

HY-10261D

Afatinib oxalate BIBW 2992 oxalate	EGFR Autophagy Apoptosis c-Met/HGFR Akt	Cancer
Afatinib (BIBW 2992) oxalate is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and *HER2), with IC₅₀* values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR ^wt, EGFR ^L858R, EGFR ^L858R/T790M and HER2, respectively. Afatinib oxalate can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .

HY-15732

BGB-102

JNJ-26483327
EGFR Cancer

BGB-102 is a potent multi-kinase inhibitor against EGFR, HER2, and HER4 with IC₅₀s of 9.6 nM, 18 nM and 40.3 nM, respectively.

BGB-102 JNJ-26483327	EGFR	Cancer
BGB-102 is a potent multi-kinase inhibitor against *EGFR, HER2, and HER4* with IC₅₀s of 9.6 nM, 18 nM and 40.3 nM, respectively.

HY-10530

Varlitinib 1 Publications Verification ASLAN001; ARRY-334543	EGFR	Cancer
Varlitinib (ASLAN001) is a potent, reversible, small molecule pan-EGFR inhibitor with IC₅₀s of 7, 2, 4 nM for HER1, HER2 and HER4, respectively .

HY-10530A

Varlitinib tosylate ASLAN001 tosylate; ARRY-334543 tosylate	EGFR	Cancer
Varlitinib (ASLAN001) tosylate is a potent, reversible, small molecule pan-EGFR inhibitor with IC₅₀s of 7, 2, 4 nM for HER1, HER2 and HER4, respectively .

HY-111553

TAS0728	EGFR	Cancer
TAS0728 is a potent, selective, orally active, irreversible and covalent-binding *HER2* inhibitor, with an IC₅₀ of 13 nM. TAS0728 also shows IC₅₀s of 4.9, 8.5, 31, 65, 33, 25 and 86 nM for *BMX、HER4、BLK、EGFR、JAK3、SLK* and LOK respectively. Furthermore, TAS0728 exhibits robust and sustained inhibition of the phosphorylation of HER2HER3, and downstream effectors .

HY-10261E

(R)-Afatinib (R)-BIBW 2992	EGFR c-Met/HGFR p38 MAPK	Cancer
(R)-Afatinib ((R)-BIBW 2992) is the Afatinib isomer. Afatinib (HY-10261) is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR* and HER2),* with IC₅₀ values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR ^wt, EGFR ^L858R, EGFR ^L858R/T790M and HER2, respectively. Afatinib can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .

HY-135815

Mobocertinib 5+ Cited Publications TAK-788; AP32788	EGFR	Cancer
Mobocertinib (TAK-788) is an orally active and irreversible *EGFR/HER2* inhibitor. Mobocertinib potently inhibits oncogenic variants containing activating EGFRex20ins mutations with selectivity over wild-type *EGFR*. Mobocertinib can be used in NSCLC research .

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