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EGFR-IN-2

" in MedChemExpress (MCE) Product Catalog:

By Targets:	EGFR (54) Akt (1) Anaplastic lymphoma kinase (ALK) (1) Apoptosis (8) Btk (1) c-Met/HGFR (1) CDK (10) Dihydrofolate reductase (DHFR) (2) Ephrin Receptor (1) ERK (1) HSP (1) IKK (1) Isotope-Labeled Compounds (2) Necroptosis (1) PARP (1) PROTACs (1) SphK (2) Survivin (1) Thymidylate Synthase (2) Topoisomerase (1) VEGFR (5)
By Research Areas:	Cancer (58) Cardiovascular Disease (1) Inflammation/Immunology (1)

Inhibitors & Agonists

Inhibitory Antibodies

Isotope-Labeled Compounds

Targets Recommended: EGFR AIM2 NEKs

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-100520

EGFR-IN-2

EGFR Cancer

EGFR-IN-2 is a a noncovalent, irreversible, mutant-selective second generation EGFR inhibitor.

*EGFR-IN-2*	EGFR	Cancer
EGFR-IN-2 is a a noncovalent, irreversible, mutant-selective second generation *EGFR* inhibitor.

HY-128860

Mutated EGFR-IN-2	EGFR	Cancer
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 .

HY-155227A

ALK/EGFR-IN-2	Anaplastic lymphoma kinase (ALK)	Cancer
ALK/EGFR-IN-2 is a potent dual inhibitor of ALK and *EGFR*. ALK/EGFR-IN-2 induces apoptosis and G0/G1 cell cycle arrest in cancer cells. ALK/EGFR-IN-2 significantly inhibits the cell proliferation of H1975, PC9, and Baf3-EML4-ALK cancer cell lines with IC₅₀s of 0.0034, 0.0065, and 0.0018 μM, respectively .

HY-151573

EGFR/CDK2-IN-1	EGFR CDK	Cancer
EGFR/CDK2-IN-1 (Compound 3b) is an *EGFR/CDK2* inhibitor. EGFR/CDK2-IN-1 shows good cytotoxicity against MCF7 and HepG2 cells. EGFR/CDK2-IN-1 can be used in cancer research .

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-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-144304

PROTAC EGFR degrader 2	PROTACs EGFR	Cancer
PROTAC EGFR degrader 2 is a potent PROTAC *EGFR* degrader. PROTAC EGFR degrader 2 exhibits excellent antiproliferative activity with IC₅₀ of 4.0 nM and good EGFR degradation activity with DC50 of 36.51 nM. PROTAC EGFR degrader 2 can be used for the synthesis of nitroreductase (NTR)-responsive PROTAC .

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-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-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-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-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-155005

EGFR mutant-IN-2	EGFR	Cancer
EGFR mutant-IN-2 (Compound D51) is an *EGFR* mutant inhibitor. EGFR mutant-IN-2 inhibits the EGFR ^{L858R/T790M/C797S} mutant with an IC₅₀ value of 14 nM. EGFR mutant-IN-2 inhibits the EGFR ^{del19/T790M/C797S} mutant with an IC₅₀ value of 62 nM. EGFR mutant-IN-2 has favorable PK parameters, safety properties, in vivo stability, and antitumor activity .

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-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-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-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-156114

EGFR/CDK2-IN-2	EGFR CDK	Cancer
EGFR/CDK2-IN-2 (compound 6a) is a dual inhibitor of EGFR and CDK-2 with IC₅₀s of 19.6 and 87.9 nM, respectively. EGFR/CDK2-IN-2 induces apoptosis in MCF-7 cells and arrests the cell cycle in the S phase. EGFR/CDK2-IN-2 has significant anti-cancer cell toxicity and inhibits MCF-7 with an IC₅₀ of 0.39 μM .

HY-156115

EGFR/CDK2-IN-3	EGFR CDK	Cancer
EGFR/CDK2-IN-3 (compound 4b) is a dual inhibitor of EGFR and CDK-2 with IC₅₀s of 71.7 and 113.7 nM, respectively. EGFR/CDK2-IN-3 induces apoptosis in MCF-7 cells and arrests the cell cycle in the S phase. EGFR/CDK2-IN-3 has significant anti-cancer cell toxicity and inhibits MCF-7 with an IC₅₀ of 3.16 μM .

HY-156116

EGFR/CDK2-IN-4	EGFR CDK	Cancer
EGFR/CDK2-IN-4 (compound 4c) is a dual inhibitor of EGFR and CDK-2 with IC₅₀s of 89.6 and 165.4 nM, respectively. EGFR/CDK2-IN-4 induces apoptosis in MCF-7 cells and arrests the cell cycle in the S phase. EGFR/CDK2-IN-4 has significant anti-cancer cell toxicity and inhibits MCF-7 with an IC₅₀ of 2.74 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-150905

*EGFR ligand-2*	EGFR	Cancer
EGFR ligand-2 (compound C4), a covalent *EGFR* ligand, is a EGFR mutant inhibitor with IC₅₀s of 21 nM and 48 nM for EGFR ^L858R and EGFR ^L858R/T790M, respectively. EGFR ligand-2 can be used to synthesize PROTAC .

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-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-156639

EGFR/ErbB-2 inhibitor-1

EGFR Cancer

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

EGFR/ErbB-2 inhibitor-1	EGFR	Cancer
EGFR/ErbB-2 inhibitor-1 is a ErbB2/HER2 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-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-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-10333

BMS-690514 2 Publications Verification	EGFR VEGFR	Cardiovascular Disease Cancer
BMS-690514 is a potent and orally active inhibitor of *EGFR* and VEGFR; has IC₅₀s of 5, 20 and 60 nM for EGFR, HER 2 and HER 4, respectively.

HY-18609

PD158780

1 Publications Verification

EGFR Cancer

PD158780 is a potent EGFR family inhibitor with IC₅₀s of 8 pM, 49, 52, 52 nM for EGFR, ErbB2, ErbB3, and ErbB4, respectively.

PD158780 1 Publications Verification	EGFR	Cancer
PD158780 is a potent *EGFR* family inhibitor with IC₅₀s of 8 pM, 49, 52, 52 nM for EGFR, ErbB2, ErbB3, and ErbB4, respectively.

HY-13050

Sapitinib 5+ Cited Publications AZD-8931	EGFR	Cancer
Sapitinib (AZD-8931) is a reversible, ATP competitive *EGFR* inhibitor of with IC₅₀s of 4, 3 and 4 nM for EGFR, ErbB2 and ErbB3 in cells, respectively.

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-13272

Dacomitinib Maximum Cited Publications 17 Publications Verification PF-00299804; PF-299804	EGFR Apoptosis	Cancer
Dacomitinib (PF-00299804) is a specific and irreversible inhibitor of the ERBB family of kinases with IC₅₀s of 6 nM, 45.7 nM and 73.7 nM for *EGFR, ERBB2*, and ERBB4, respectively .

HY-103440

EGFR/ErbB-2/ErbB-4 inhibitor-3	EGFR	Cancer
EGFR/ErbB-2/ErbB-4 inhibitor-3 (compound 29) is a potent tyrosine kinase inhibitor with IC₅₀s of 0.3, 1.1, 0.5, 2.5, 24 nM for erbB1, erbB2, erbB4, EGF, HER, respectively . EGFR/ErbB-2/ErbB-4 inhibitor-3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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-112420

EGFR/ErbB-2/ErbB-4 inhibitor-2

EGFR Cancer

EGFR/ErbB-2/ErbB-4 inhibitor-2 (Compound 5) is a EGFR and ErbB inhibitor with IC₅₀s of 0.017 μM, 0.08 μM, 1.91 μM .
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/ErbB-2/ErbB-4 inhibitor-2	EGFR	Cancer
EGFR/ErbB-2/ErbB-4 inhibitor-2 (Compound 5) is a *EGFR* and ErbB inhibitor with IC₅₀s of 0.017 μM, 0.08 μM, 1.91 μM .

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-13272S2

Dacomitinib-d10 dihydrochloride PF-00299804-d₁₀ dihydrochloride; PF-299804-d₁₀ dihydrochloride	Isotope-Labeled Compounds EGFR Apoptosis	Cancer
Dacomitinib-d₁₀ (dihydrochloride) is the deuterium labeled Dacomitinib dihydrochloride. Dacomitinib (PF-00299804) dihydrochloride is a specific and irreversible inhibitor of the ERBB family of kinases with IC50s of 6 nM, 45.7 nM and 73.7 nM for EGFR, ERBB2, and ERBB4, respectively[1].

HY-13272S3

Dacomitinib-d10 PF-00299804-d₁₀; PF-299804-d₁₀	Isotope-Labeled Compounds EGFR Apoptosis	Cancer
Dacomitinib-d₁₀ is deuterium labeled Dacomitinib. Dacomitinib (PF-00299804) is a specific and irreversible inhibitor of the ERBB family of kinases with IC50s of 6 nM, 45.7 nM and 73.7 nM for EGFR, ERBB2, and ERBB4, respectively[1].

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 ^[2].

HY-135815B

Mobocertinib mesylate TAK-788 mesylate; AP32788 mesylate	EGFR	Cancer
Mobocertinib (TAK-788) mesylate is an orally active and irreversible *EGFR/HER2* inhibitor. Mobocertinib mesylate potently inhibits oncogenic variants containing activating EGFRex20ins mutations with selectivity over wild-type *EGFR*. Mobocertinib mesylate can be used in NSCLC research ^[2].

HY-135815A

Mobocertinib succinate 5+ Cited Publications TAK-788 succINate; AP32788 succINate	EGFR	Cancer
Mobocertinib (TAK-788) succinate is an orally active and irreversible *EGFR/HER2* inhibitor. Mobocertinib succinate potently inhibits oncogenic variants containing activating EGFRex20ins mutations with selectivity over wild-type *EGFR*. Mobocertinib succinate can be used in NSCLC research ^[2].

HY-161141

EGFR/c-Met-IN-2	c-Met/HGFR	Cancer
EGFR/ C-Met-in-2 (Compound H-22) is a dual inhibitor of *EGFR/c-Met. EGFR/c-Met-IN-2 inhibits cell proliferation by arresting G2/M phase. EGFR*/c-Met-IN-2 has antitumor activity .

HY-13314

Tesevatinib 4 Publications Verification XL-647; EXEL-7647; KD-019	EGFR VEGFR Ephrin Receptor	Cancer
Tesevatinib (XL-647; EXEL-7647; KD-019) is an orally available, multi-target tyrosine kinase inhibitor; inhibits *EGFR, ErbB2*, KDR, Flt4 and EphB4 kinase with IC₅₀s of 0.3, 16, 1.5, 8.7, and 1.4 nM.

HY-103439

GW583340 dihydrochloride	EGFR	Cancer
GW 583340 dihydrochloride is a potent dual *EGFR/ErbB2* tyrosine kinase inhibitor (IC₅₀: 0.01 and 0.014 μM respectively). GW 583340 dihydrochloride reverses ABCG2- and ABCB1-mediated drug resistance. GW 583340 dihydrochloride has anti-cancer activity ^[2] .

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