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Results for "

EGFR inhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	EGFR (426) 5-HT Receptor (1) Ack1 (1) Akt (10) AMPK (1) Amyloid-β (1) Anaplastic lymphoma kinase (ALK) (8) Antibody-Drug Conjugates (ADCs) (1) Apoptosis (103) Aurora Kinase (2) Autophagy (42) Bacterial (1) Bcl-2 Family (2) Bcr-Abl (2) BMX Kinase (2) Btk (14) c-Kit (1) c-Met/HGFR (11) CaMK (2) Casein Kinase (3) Caspase (3) CDK (14) Checkpoint Kinase (Chk) (1) COX (2) Cytochrome P450 (1) Dihydrofolate reductase (DHFR) (3) Discoidin Domain Receptor (1) DNA-PK (1) DNA/RNA Synthesis (1) Drug Metabolite (8) Drug-Linker Conjugates for ADC (3) E1/E2/E3 Enzyme (1) Endogenous Metabolite (4) Enterovirus (1) Ephrin Receptor (1) Epigenetic Reader Domain (1) ERK (3) FAK (1) Ferroptosis (9) FGFR (4) FLT3 (1) GPR35 (1) HCV (2) HDAC (2) Histone Acetyltransferase (1) Histone Methyltransferase (2) HIV (1) HSP (3) IGF-1R (1) IKK (1) Influenza Virus (2) IRAK (2) Isotope-Labeled Compounds (14) Itk (3) JAK (8) JNK (3) MEK (1) mGluR (1) Microtubule/Tubulin (3) Mitochondrial Metabolism (1) Monoamine Oxidase (1) mTOR (4) Necroptosis (1) NF-κB (1) Orthopoxvirus (2) Oxidative Phosphorylation (1) p38 MAPK (4) PAK (1) Parasite (1) PARP (2) PDGFR (4) Phosphatase (3) Phosphodiesterase (PDE) (2) PI3K (4) PI4K (1) Pim (1) PKA (2) PKC (2) Polo-like Kinase (PLK) (1) Potassium Channel (1) PROTACs (11) Raf (7) Ras (1) Reactive Oxygen Species (3) RET (3) Reverse Transcriptase (1) ROR (1) SphK (2) Src (9) STAT (6) Survivin (1) TAM Receptor (1) TGF-beta/Smad (1) Thymidylate Synthase (2) Topoisomerase (5) Trk Receptor (4) Tyrosinase (1) VEGFR (24) Wnt (1)
By Research Areas:	Cancer (473) Cardiovascular Disease (5) Infection (6) Inflammation/Immunology (12) Metabolic Disease (3) Neurological Disease (4)
Click Chemistry:	Azide (1) Alkynes (21)

512

Inhibitors & Agonists

Screening Libraries

Fluorescent Dye

Biochemical Assay Reagents

Peptides

Inhibitory Antibodies

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

Targets Recommended: EGFR

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-13984

Mutant EGFR inhibitor	EGFR	Cancer
Mutant EGFR inhibitor is a potent and selective mutant *EGFR* inhibitor extracted from patent WO 2013014448 A1; inhibits EGFR ^L858R, EGFR ^{Exon 19 deletion} and EGFR ^T790M.

HY-157166

EGFR kinase inhibitor 2	EGFR	Cancer
EGFR kinase inhibitor 2 (compound A-7) is a potent *EGFR* inhibitor targeting EGFR ^{L858R/T790M/C797S} and EGFR ^{Del19/T790M/C797S} mutants. EGFR kinase inhibitor 2 has the potential to address acquired resistance in the treatment of non-small cell lung cancer .

HY-162300

EGFR kinase inhibitor 4	EGFR	Cancer
EGFR kinase inhibitor 4 (Compound 4) is a bivalent ATP-allosteric *EGFR* inhibitor (IC₅₀: 1.8 nM for mutant EGFR (LRTMCS)). EGFR kinase inhibitor 4 can be used for research of NSCLC .

HY-162299

EGFR kinase inhibitor 3	EGFR	Cancer
EGFR kinase inhibitor 3 (compound 2) is a bivalent ATP-allosteric *EGFR* kinase inhibitor with IC₅₀s of <10 nM, 1.5 nM, 0.059 nM, 0.064 nM for WT EGFR, EGFR-activating mutations L858R, L858R/T790M and L858R/T790M/C797S, respectively. EGFR kinase inhibitor 3 is a C-linked inhibitor .

HY-143246

EGFR kinase inhibitor 1	EGFR Apoptosis	Cancer
EGFR kinase inhibitor 1 is a potent *EGFR* inhibitor with IC₅₀s of 37, 1.7, >300 nM for WT, l885R/T790M, L858R/T790M/C797S, respectively. EGFR kinase inhibitor 1 induces apoptosis and cell cycle arrest at G0/G1-phase. EGFR kinase inhibitor 1 inhibits the cell motility. EGFR kinase inhibitor 1 shows antiproliferative and anti-tumor activity .

HY-156639

EGFR/ErbB-2 inhibitor-1

EGFR Cancer

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

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

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-157480

EGFR/AURKB-IN-1	EGFR Aurora Kinase	Cancer
EGFR/AURKB-IN-1 (compound 7) is a dual-targeted *EGFR/AURKB* inhibitor, and inhibits the phpsphorylations of ^L858R EGFR and AURKB with IC₅₀s of 0.07 and 1.1, respectively. EGFR/AURKB-IN-1 occupies the hydrophobic region I or the αC-helix out pocket of EGFR and the back pocket of AURKB, inhibiting the growth, division and metastasis of tumor cells, thus can be used for cancer research .

HY-161136

EGFR/STAT3-IN-1	EGFR STAT	Cancer
EGFR/STAT3-IN-1 (Compound 5k) is a dual inhibitor of EGFR/STAT3 with IC₅₀ values for *EGFR* and STAT3 are 41 and 3.34 nM, respectively. EGFR/STAT3-IN-1 has antitumor activity .

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-161269

EGFR-IN-101	EGFR	Cancer
EGFR-IN-101 (I-10) is a 2-phenylamino pyrimidine derivative. EGFR-IN-101 is a *EGFR* inhibitor. The IC₅₀ values for EGFR ^{L858R/T790M/C797S} and Ba/F3-EGFR ^{L858R/T790M/C797S} are 33.26 and 106.4 nM, respectively. EGFR-IN-101 can be used IN the study of non-small cell lung cancer (NSCLC) .

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-155200

EGFR-IN-84	EGFR	Cancer
EGFR-IN-84 (Compound 6g) is an *EGFR* inhibitor (IC₅₀: 24 nM). EGFR-IN-84 inhibits A549 cell growth (IC₅₀: 1.537 μM). EGFR-IN-84 can be used for research of lung cancer .

HY-163371

EGFR WT/T790M-IN-1	EGFR Apoptosis	Cancer
EGFR WT/T790M-IN-1 (Compound 16h) is a dual EGFR WT and EGFR T790 inhibitor. EGFR WT/T790M-IN-1 can arrest the cell cycle in G2/M phase and induce apoptosis. EGFR WT/T790M-IN-1 has anti-cancer activity .

HY-162099

VEGFR-IN-4	EGFR	Cancer
VEGFR-IN-4 (Compound 6e) is an epidermal growth factor receptor (EGFR) inhibitor. VEGFR-IN-4 has potent antiproliferative activity with an IC₅₀ value of 24.6nM against HCC827 cells .

HY-W423595

BEBT-109	EGFR	Cancer
BEBT-109 is a potent pan-mutant-selective *EGFR* inhibitor. BEBT-109 has improved pharmacokinetic properties. BEBT-109 can be used for multiple mutant-EGFR-driven non-small cell lung cancer (NSCLC) research .

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-157994

EGFR WT/T790M-IN-2	EGFR Apoptosis	Cancer
EGFR WT/T790M-IN-2 (Compound 7c) is a EGFR T790M/WT inhibitor with IC₅₀ values of 0.08 and 0.13 μM, respectively. EGFR WT/T790M-IN-2 induces apoptosis by blocking the G0-G1 phase (apoptosis). EGFR WT/T790M-IN-2 has antitumor activity .

HY-162254

EGFR/ACK1-IN-1	EGFR Ack1	Cancer
EGFR T790M/L858R/ACK1-IN-1 is a dual inhibitor of EGFR T790M/L858R and ACK1. IC₅₀ values are 23 and 263 nM, respectively. EGFR T790M/L858R/ACK1-IN-1 can inhibit cell proliferation and has antitumor activity .

HY-142512

EGFR-IN-24

EGFR Cancer

EGFR-IN-24, a potent EGFR inhibitor, shows inhibition against EGFR(del19/T790M/C797S) and EGFR(L858R/T790M/C797S), respectively .

EGFR-IN-24	EGFR	Cancer
EGFR-IN-24, a potent EGFR inhibitor, shows inhibition against EGFR(del19/T790M/C797S) and EGFR(L858R/T790M/C797S), respectively .

HY-P5314

OK2	EGFR STAT	Others
OK2, a specific inhibitor of the *CCN2/EGFR* interaction, efficiently blocks *CCN2/EGFR* interaction through binding to the CT domain of CCN2. OK2 can be used for kidney fibrosis and chronic kidney disease research .

HY-112412

PDGFR Tyrosine Kinase Inhibitor III PDGF Receptor Tyrosine Kinase inhibitor III	PDGFR	Neurological Disease
PDGFR Tyrosine Kinase Inhibitor III (PDGF Receptor Tyrosine Kinase Inhibitor III), a multikinase inhibitor, inhibits PDGFR, EGFR, FGFR, PKA, and PKC, respectively. PDGFR Tyrosine Kinase Inhibitor III can be used for the research of amyotrophic lateral sclerosis .

HY-162148

HNPMI	EGFR	Cancer
HNPMI is an inhibitor of *EGFR* and has cytotoxic effects on tumor cells. HNPMI can downregulate the protein levels of osteopontin, survivin and cathepsin S, leading to apoptosis. HNPMI also regulates BCL-2/BAX and p53 in CRC cell lines to inhibit tumorigenesis .

HY-147860

EGFR-IN-61	EGFR	Cancer
EGFR-IN-61 (compound 22a) is a potent *EGFR* kinase inhibitor, with IC₅₀ values of 42 nM (L858R/T790 M), 137 nM (L858R/T790 M/C797S), and 743 nM (WT), respectively. EGFR-IN-61 shows antiproliferative activity against A549 and H1975 cell lines, with IC₅₀ values of 2.14 and 1.82 μM, respectively .

HY-147862

EGFR-IN-62	EGFR Apoptosis	Cancer
EGFR-IN-62 (compound 9h) is a potent and reversible *EGFR* kinase inhibitor, with IC₅₀ values of 10 nM (L858R/T790 M), 29 nM (WT), and 242 nM (L858R/T790 M/C797S), respectively. EGFR-IN-62 shows antiproliferative activity against A549 and H1975 cell lines, with IC₅₀ values of 2.53 and 1.56 μM, respectively. EGFR-IN-62 induces dose-dependent apoptosis process, G1/G0-phase arrestation, and the inhibition of motility on A549 and/or H1975 cell lines .

HY-112823A

Almonertinib mesylate 3 Publications Verification HS-10296 mesylate	EGFR	Cancer
Almonertinib (HS-10296) mesylate is an orally available, irreversible, third-generation *EGFR* tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib mesylate shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC₅₀: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib mesylate is used for the research of the non-small cell lung cancer .

HY-163094

EGFR-IN-95	EGFR	Cancer
EGFR-IN-95 (compound 5j) is an 2,4-diaminonicotinamide derivative. EGFR-IN-95 has potent inhibitory activity against EGFR del19/T790M/C797S and L858R/T790M/C797S .

HY-145823

EGFR-IN-42	EGFR	Cancer
EGFR-IN-42 (Compound 17b) is a potent inhibitor of *EGFR* with single-digit nanomolar activity. EGFR-IN-42 connects tamoxifen or endoxifen with the EGFR-inhibitor gefitinib via a covalent linkage. EGFR-IN-42 retains both ER antagonist activity and EGFR inhibition. EGFR-IN-42 has superior anti-cancer activity .

HY-145824

EGFR-IN-43	EGFR	Cancer
EGFR-IN-43 (Compound 17c) is a potent inhibitor of *EGFR* with single-digit nanomolar activity. EGFR-IN-43 connects tamoxifen or endoxifen with the EGFR-inhibitor gefitinib via a covalent linkage. EGFR-IN-43 retains both ER antagonist activity and EGFR inhibition. EGFR-IN-43 has superior anti-cancer activity .

HY-142681

EGFR-IN-28

EGFR Cancer

EGFR-IN-28 is a potent EGFR inhibitor. EGFR-IN-28 has antitumor activity .

EGFR-IN-28	EGFR	Cancer
EGFR-IN-28 is a potent EGFR inhibitor. EGFR-IN-28 has antitumor activity .

HY-161145

EGFR/microtubule-IN-1	EGFR Apoptosis Microtubule/Tubulin	Cancer
EGFR/microtubule-IN-1 (Compound 10c) is a dual inhibitor targeting *EGFR* and tubulin. The IC₅₀ for inhibiting EGFR is 10.66 nM. EGFR/microtubule-IN-1 can reduce the phosphorylation levels of EGFR, AKT and ERK, hinder tubulin polymerization, and induce apoptosis .

HY-150611

EGFR-IN-70	EGFR	Cancer
EGFR-IN-70 (compound 18j) is a potent *EGFR* inhibitor with IC₅₀ values of 23.6 and 307.5 nM for EGFR ^LR/TM/CS and EGFR ^WT, respectively. EGFR-IN-70 has anti-proliferative activity and suppresses phosphorylation of the EGFR. EGFR-IN-70 can be used for cancer research .

HY-149695

EGFR-IN-91	EGFR	Cancer
EGFR-IN-91 (compound 9) is an orally available *EGFR* inhibitor with blood-brain barrier penetrability. EGFR-IN-91 inhibits EGFR ^L858R/C797S and EGFR ^{exon 19del/C797S}, inducing tumor regression in xenograft (PDX) mouse models. EGFR-IN-91 has the potential to inhibit localized and metastatic non-small cell lung cancer (NSCLC) driven by EGFR mutants .

HY-158018

EGFR-TK-IN-2

EGFR Cancer

EGFR-TK-IN-2 (compound 10b) is EGFR-TK inhibitor with the IC₅₀ of 0.16 μM. EGFR-TK-IN-2 inhibits cell growth .

EGFR-TK-IN-2	EGFR	Cancer
EGFR-TK-IN-2 (compound 10b) is *EGFR-TK* inhibitor with the IC₅₀ of 0.16 μM. EGFR-TK-IN-2 inhibits cell growth .

HY-144794

EGFR-IN-46	Apoptosis EGFR FAK	Cancer
EGFR-IN-46 is a potent *EGFR* and FAK dual inhibitor with IC₅₀s of 20.17 nM, 14.25 nM, respectively. EGFR-IN-46 significantly inhibits the growth of cancer cells. EGFR-IN-46 induces cell apoptosis .

HY-126320

EGFR-IN-8	EGFR c-Met/HGFR	Cancer
EGFR-IN-8 is a dual *EGFR* and c-Met inhibitor, compound 48. EGFR-IN-8 can be a promising candidate for further development to target EGFR TKI-resistant NSCLC .

HY-111452

EGFR-IN-85	EGFR	Cancer
EGFR-IN-85 (Compound 1) is an *EGFR* inhibitor. EGFR-IN-85 has IC₅₀ value of 0.19 μM for EGFRvⅢ phosphorylation. EGFR-IN-85 can suppress EGFR signaling within tumors. EGFR-IN-85 can be used for Glioblastoma (GBM) research .

HY-152098

HX103	EGFR	Cancer
HX103 is an epidermal growth factor receptor (EGFR)-tyrosine kinase inhibitor (TKI)-based fluorogenic probe. HX103 inhibits EGFR 19 del, EGFR L858R, EGFR wild type and EGFR T790M with IC₅₀s of 1.3, 1.5, 4.0 and 977 nM, respectively. HX103 can be used for quantifying active-EGFR to predict agent sensitivity in NSCLC patients with EGFR-activating mutations .

HY-155227

ALK/EGFR-IN-1	Anaplastic lymphoma kinase (ALK) EGFR Apoptosis	Cancer
ALK/EGFR-IN-1 (Compound 8l) is an *ALK/EGFR* dual inhibitor that blocks the phosphorylation of EGFR and ALK. ALK/EGFR-IN-1 inhibits ALK/EGFR mutants respectively, with IC₅₀ of 4.3 nM for EGFR L858R T790M in H1975 cells and EML4-ALK in BaF3 cells, respectively. and 3.6 nM. ALK/EGFR-IN-1 may be used in NSCLC research .

HY-17499

EGFR-IN-12	EGFR Apoptosis	Cancer
EGFR-IN-12 is a 4,6-disubstituted pyrimidine and is a potent, ATP-competitive, irreversible and highly selective *EGFR* inhibitor with an IC₅₀of 21 nM. EGFR-IN-12 also inhibits mutant EGFR ^L858R and EGFR ^L861Q with IC₅₀s of 63 nM and 4 nM, respectively. EGFR-IN-12 displays strong selectivity for *EGFR* over HER4 (IC₅₀ = 7640 nM) and a panel of 55 other kinases. EGFR-IN-12 induces cells apoptosis and has antitumor activity .

HY-151882

EGFR-IN-73

EGFR Cancer

EGFR-IN-73 (Compound 3f) is a potent inhibitor for the most common EGFR mutation EGFR Del19 with an IC₅₀ of 119 nM .

EGFR-IN-73	EGFR	Cancer
EGFR-IN-73 (Compound 3f) is a potent inhibitor for the most common EGFR mutation EGFR Del19 with an IC₅₀ of 119 nM .

HY-156741

EGFR-IN-87	EGFR	Cancer
EGFR-IN-87 is a *EGFR* tyrosine kinase inhibitor. EGFR-IN-87 has IC₅₀ value of 3.1 nM, 1.3 nM and 7.1 nM for EGFR_d746-750, EGFR_L858R/T790 and EGFR_WT in A431 cells, respectively. EGFR-IN-87 can be used for cancer diseases research .

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-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-163006

EGFR/c-Met-IN-1	EGFR c-Met/HGFR	Cancer
EGFR/c-Met-IN-1 (compound TS-41) is a dual-target inhibitor of *EGFR/c-Met. The IC₅₀ for inhibiting* EGFR ^L858R and c-Met is 68.1 nM and 0.26 nM respectively. . EGFR/c-Met-IN-1 induces apoptosis and cell cycle arrest in A549-P cells, downregulating the phosphorylation of EGFR, c-Met, and downstream AKT. EGFR/c-Met-IN-1 inhibits tumor growth in vitro and in vivo .

HY-19803

Naquotinib mesylate 4 Publications Verification ASP8273 mesylate	EGFR	Cancer
Naquotinib mesylate (ASP8273 mesylate) is an orally available, mutant-selective and irreversible *EGFR* inhibitor; with IC₅₀s of 8-33 nM toward EGFR mutants and 230 nM for EGFR.

HY-19729

Naquotinib 4 Publications Verification ASP8273	EGFR	Cancer
Naquotinib (ASP8273) is an orally available, mutant-selective and irreversible *EGFR* inhibitor; with IC₅₀s of 8-33 nM toward EGFR mutants and 230 nM for EGFR.

HY-138746

EGFR-IN-15

EGFR Cancer

EGFR-IN-15 (compound I-005) is a EGFR inhibitor with an IC₅₀ of 4 nM. EGFR-IN-15 can be used for oncological diseases 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 .
HY-147996

EGFR-IN-67

EGFR Cancer

EGFR-IN-67 (Compound 7d) is a potent EGFR inhibitor with an IC₅₀ of 0.34 μM. EGFR-IN-67 shows anticancer activity .

Cat. No.	Product Name

HY-L009

Kinase Inhibitor Library

3137 compounds

Kinase is an enzyme that adds phosphate groups to other molecules. This process is known as phosphorylation. Protein phosphorylation is a key aspect in the regulation of a large number of cellular processes including cellular division, metabolism, signal transduction, and so on. There are over 500 kinases encoded by the human genome and it has been estimated that kinases regulate approximately 50% of cellular functions. Kinases are a large group of drug targets in drug discovery. Kinase inhibitors are an important class of drugs that block certain enzymes involved in diseases such as cancer and inflammatory disorders.

Kinase inhibitor library designed by MCE contains 3137 kinase inhibitors and regulators mainly targeting protein kinases (VEGFR, EGFR, BTK, CDK, Akt, etc.), lipid kinases (PI3K, PI4K, SK, etc.) and carbohydrate kinases (Hexokinase), and is a useful tool for kinase drug discovery and related research.

HY-L016

Protein Tyrosine Kinase Compound Library

1055 compounds

Protein tyrosine kinases (PTKs) are key signaling molecules and important drug targets. Two classes of PTKs are present in cells: the transmembrane receptor PTKs (RTKs) and the nonreceptor PTKs. The RTK family includes the receptors for insulin and for many growth factors, such as EGFR, FGFR, PDGFR, VEGFR, and NGFR. RTKs are transmembrane glycoproteins that are activated by the binding of their ligands, and they transduce the extracellular signal to the cytoplasm by phosphorylating tyrosine residues on the receptors themselves (autophosphorylation) and on downstream signaling proteins. Their principal functions of PTKs involve the regulation of multicellular aspects of the organism. Cell to cell signals concerning growth, differentiation, adhesion, motility, and death are frequently transmitted through tyrosine kinases. In humans, tyrosine kinases have been demonstrated to play significant roles in the development of many disease states, including diabetes and cancers.

MCE designs a unique collection of 1055 compounds that act as a useful tool for PTKs-related drug screening and disease research.

HY-L177

Antibody Inhibitor Library

21 Compounds compounds

Antibody inhibitors are compounds with the same activity as the original therapeutic antibodies, which can be used as positive controls for drug efficacy evaluation and other studies. Antibody inhibitors can also assist in verifying the functional activity of the target protein. These antibody inhibitors are active in vivo and can achieve certain physiological functions by blocking or neutralizing target proteins, such as CD20, HER2, EGFR, VEGFR, TNF-α, etc. In drug screening, antibody inhibitor-based screening can be carried out to identify active compounds targeting target proteins and target diseases.

MCE can provide 21 antibody inhibitors that can be used for drug development in cancer, immunity, infection and other hot research areas.

HY-L008

JAK/STAT Compound Library

423 compounds

The Janus kinase (JAK)/signal transducer and activator of transcription (STAT) pathway is central to signaling by cytokine receptors, a superfamily of more than 30 transmembrane proteins that recognize specific cytokines, and is critical in blood formation and immune response. Canonical JAK/STAT signaling begins with the association of cytokines and their corresponding transmembrane receptors. Activated JAKs then phosphorylate latent STAT monomers, leading to dimerization, nuclear translocation, and DNA binding. In mammals, there are four JAKs (JAK1, JAK2, JAK3, TYK2) and seven STATs (STAT1, STAT2, STAT3, STAT4, STAT5a, STAT5b, STAT6). Since the JAK/STAT pathway plays a major role in many fundamental processes, such as apoptosis and inflammation, dysfunctional proteins in the pathway may lead to a number of diseases. For example, alterations in JAK/STAT signalling can result in cancer and diseases affecting the immune system, such as severe combined immunodeficiency disorder (SCID).

MCE provides 423 compounds that can be used in the study of the JAK/STAT signaling pathway and related diseases.

Cat. No.	Product Name	Target	Research Area

HY-P99041A

Panitumumab (anti-EGFR)	EGFR	Cancer
Panitumumab (anti-EGFR) is a fully human IgG2 anti-EGFR monoclonal antibody with anti-tumor activity. Panitumumab (anti-EGFR) inhibits tumor cell proliferation, survival and angiogenesis. Panitumumab (anti-EGFR) can be used in the research of cancers, such as colon cancer .

HY-P9969

Matuzumab

EMD 72000
EGFR Cancer

Matuzumab (EMD 72000) is a humanized anti-EGFR monoclonal antibody that blocks EGFR activation and downstream signaling, inhibits tumor growth .

HY-P9905

Cetuximab Maximum Cited Publications 25 Publications Verification C225	EGFR	Cancer
Cetuximab (C225) is a human IgG1 monoclonal antibody that inhibits epidermal growth factor receptor (EGFR), with a K_d of 0.201 nM for EGFR by SPR. Cetuximab has potent antitumor activity .

HY-P99849

Depatuxizumab ABT-806	EGFR	Cancer
Depatuxizumab is a brain-penetrant and humanized tumor-specific anti *EGFR* monoclonal antibody. Depatuxizumab inhibits the growth of xenograft models of mutant EGFRvIII and wild-type EGFR. Depatuxizumab can be used for research on cancer .

HY-P99041

Panitumumab 1 Publications Verification ABX-EGF	EGFR	Cancer
Panitumumab (ABX-EGF) is a fully human IgG2 anti-EGFR monoclonal antibody with anti-tumor activity. Panitumumab inhibits tumor cell proliferation, survival and angiogenesis. Panitumumab can be used in the research of cancers, such as colon cancer .

HY-P9977

Amivantamab 1 Publications Verification JNJ-61186372	EGFR	Cancer
Amivantamab (JNJ-61186372) is a human *EGFR-MET* bispecific antibody with immune anticancer activity. Amivantamab inhibits ligand binding, promotes endocytosis and degradation of receptor-antibody complexes, and induces Fc-dependent cytokinesis in macrophages and antibody-dependent cytotoxicity in natural killer cells .

HY-P99275

Patritumab 1 Publications Verification Human Anti-ERBB3 Recombinant Antibody	EGFR Akt ERK PARP Survivin	Cancer
Patritumab (Human Anti-ERBB3 Recombinant Antibody) is a neutralizing monoclonal antibody to ERBB3. Patritumab shows a synergy with Cetuximab (HY-P9905), potently inhibits the phosphorylation of *EGFR, HER2, HER3, ERK, and AKT. Patritumab also induces cell apoptosis* and suppresses the growth of pancreatic, non-small cell lung cancer, and colorectal cancer xenograft tumors .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-14596

Genistein Maximum Cited Publications 39 Publications Verification NPI 031L	Structural Classification Classification of Application Fields Anti-aging Source classification Plants Endogenous metabolite Human Gut Microbiota Metabolites Flavonoids Microorganisms Sunscreen Leguminosae Glycine max (L.) merr Phenols Polyphenols Cosmetic Research Disease Research Fields Glycyrrhiza uralensis Fisch. Isoflavones Cancer	EGFR Autophagy Apoptosis Endogenous Metabolite
Genistein, a soy isoflavone, is a multiple tyrosine kinases (e.g., *EGFR) inhibitor* which acts as a chemotherapeutic agent against different types of cancer, mainly by altering apoptosis, the cell cycle, and angiogenesis and inhibiting metastasis.

HY-13595

Chrysophanol 3 Publications Verification Chrysophanic acid	Quinones Structural Classification Classification of Application Fields Rheum palmatum L. Anthraquinones Polygonaceae Source classification Phenols Polyphenols Plants Disease Research Fields Cancer	EGFR
Chrysophanol (Chrysophanic acid) is a natural anthraquinone, which inhibits EGF-induced phosphorylation of *EGFR* and suppresses activation of AKT and mTOR/p70S6K.

HY-14596R

Genistein (Standard) Maximum Cited Publications 39 Publications Verification NPI 031L (Standard)	Structural Classification Classification of Application Fields Anti-aging Source classification Plants Endogenous metabolite Human Gut Microbiota Metabolites Flavonoids Sunscreen Leguminosae Glycine max (L.) merr Phenols Cosmetic Research Disease Research Fields Glycyrrhiza uralensis Fisch. Cancer	EGFR Autophagy Apoptosis Endogenous Metabolite
Genistein (Standard) is the analytical standard of Genistein. This product is intended for research and analytical applications. Genistein, a soy isoflavone, is a multiple tyrosine kinases (e.g., *EGFR) inhibitor* which acts as a chemotherapeutic agent against different types of cancer, mainly by altering apoptosis, the cell cycle, and angiogenesis and inhibiting metastasis.

HY-N0211

Cyasterone	Classification of Application Fields Labiatae Source classification Amaranthaceae Plants Laggera crispata (Vahl) Hepper & J. R. I. Wood Disease Research Fields Achyranthes bidentata Steroids Cancer	EGFR Apoptosis
Cyasterone, a natural *EGFR* inhibitor, mainly isolated from Ajuga decumbens Thunb (Labiatae). Cyasterone manifests anti-proliferation effect by induced apoptosis and cell cycle arrests. Cyasterone may serves as a therapeutic anti-tumor agent against human tumors .

HY-127067

Yuanhuadin	Structural Classification Terpenoids Thymelaeaceae Source classification Diterpenoids Plants Daphne genkwa Sieb. et Zucc.	Akt EGFR mTOR
Yuanhuadin, extracted from Genkwa Flos Daphne genkwa, has antitumor activity through inhibiting Akt/mTOR and *EGFR* pathways, induce cell-cycle arrest and abortion .

HY-13595R

Chrysophanol (Standard) Chrysophanic acid (Standard)	Quinones Structural Classification Classification of Application Fields Rheum palmatum L. Polygonaceae Source classification Phenols Plants Disease Research Fields Cancer	EGFR
Chrysophanol (Standard) is the analytical standard of Chrysophanol. This product is intended for research and analytical applications. Chrysophanol (Chrysophanic acid) is a natural anthraquinone, which inhibits EGF-induced phosphorylation of *EGFR* and suppresses activation of AKT and mTOR/p70S6K.

HY-N2450

Sulforaphene	Structural Classification Natural Products Classification of Application Fields Source classification Plants Brassicaceae Disease Research Fields Cancer Raphanus sativus Linn.	Apoptosis EGFR ERK NF-κB Microtubule/Tubulin
Sulforaphene, isolated from radish seeds, exhibits an ED₅₀ against velvetleaf seedlings approximately 2 x 10 ^-4 M. Sulforaphene promotes cancer cells apoptosis and inhibits migration via inhibiting *EGFR, p-ERK1/2, NF‐κB* and other signals .

HY-N2409

Delphinidin chloride	Cardiovascular Disease Structural Classification Classification of Application Fields Source classification Plants Anthocyans Flavonoids other families Microorganisms Solanum melongena L. Phenols Polyphenols Solanaceae Disease Research Fields Cancer	Apoptosis EGFR JAK STAT
Delphinidin chloride is an anthocyanin isolated from berries and red wine. Delphinidin chloride exhibits endothelium-dependent vasodilation and anticancer activity. Delphinidin chloride also modulates JAK/STAT3 and MAPK signaling, thereby inducing apoptosis in HCT116 cells. Delphinidin chloride is also a potent inhibitor of EGFR (IC₅₀: 1.3 μM), shutting down downstream signaling cascades .

HY-16558

Butein 3 Publications Verification 2’,3,4,4’-tetrahydroxy Chalcone	Structural Classification Chalcones Flavonoids other families Classification of Application Fields Anti-aging Source classification Phenols Polyphenols Plants Disease Research Fields Cancer	EGFR Autophagy Apoptosis Phosphodiesterase (PDE)
Butein is a cAMP-specific PDE inhibitor with an IC₅₀ of 10.4 μM for PDE4 . Butein is a specific protein tyrosine kinase inhibitor with IC₅₀s of 16 and 65 μM for *EGFR* and p60 ^c-src in HepG2 cells . Butein sensitizes HeLa cells to Cisplatin through AKT and ERK/p38 MAPK pathways by targeting FoxO3a . Butein is a SIRT1 activator (STAC).

HY-N2510

Myristicin Myristicine	Structural Classification Simple Phenylpropanols Source classification Myristicaceae Phenylpropanoids Plants Myristica fragrans Houtt.	5-HT Receptor EGFR ERK Apoptosis Bacterial
Myristicine is an orally bioavailable serotonin receptor antagonist and weak monoamine oxidase (MAO) inhibitor. Myristicine also exerts anti-cancer effects on gastric cancer cells by inhibiting the *EGFR/ERK* signaling pathway. Myristicine is the main component of nutmeg essential oil and has anti-cancer, anti-proliferative, antibacterial, anti-inflammatory and apoptosis-inducing effects. Myristicine abuse can produce hallucinogenic effects, organ damage, etc .

HY-N3634

Corylifol C	Structural Classification Leguminosae Source classification Phenols Polyphenols Psoralea corylifolia L. Plants	Others
Corylifol C is a potent protein kinase inhibitor with IC₅₀ valueS of 8.7, 3.0, 2.1, 6.4, 4.5, 6.2, 2.3, 1.2, 5.1 μg/ml for ARK5, Aurora-A, Aurora-B, AXL, B-RAF-VE, CDK4/CycD1, TIE2, EGF-R, EPHB4, respectively .

HY-N4201

β-Hydroxyisovalerylshikonin	Quinones Classification of Application Fields Source classification Phenols Polyphenols Plants Lithospermum erythrorhizon Sieb. et Zucc. Naphthalene Quinones Disease Research Fields Boraginaceae Cancer	EGFR Src
Beta-hydroxyisovalerylshikonin is a natural product isolated from Lithospermum erythrorhizon, acts as a potent inhibitor of protein tyrosine kinases (PTK), with IC₅₀s of 0.7μM and 1μM for EGFR and v-Src receptor, respectively. Beta-hydroxyisovalerylshikonin is effective against a wide variety of tumor cell lines, and most efficiently induces cell-death in NCI-H522 and DMS114 cells .

HY-108016

Peruvoside Encordin	Apocynaceae Triterpenes Structural Classification Terpenoids Source classification Thevetia peruviana (Pers.) K. Schum. Plants	Src PI3K JNK STAT EGFR Apoptosis Autophagy
Peruvoside is a potent inhibitor of Src, PI3K, JNK, STAT, and *EGFR. Peruvoside induces apoptosis* and autophagy and possesses a broad spectrum of anticancer activity in breast, lung, liver cancers and leukemia. Peruvoside is a broad-spectrum and potent antiviral activity against positive-sense RNA viruses. Peruvoside sensitizes Gefitinib (HY-50895)-resistant tumour cells (A549, PC9/gef and H1975) to Gefitinib .

HY-N0281

Daphnetin 2 Publications Verification 7,8-Dihydroxycoumarin	Classification of Application Fields Daphne Thymelaeaceae Source classification Coumarins Phenols Polyphenols Phenylpropanoids Plants Disease Research Fields Cancer	EGFR PKA PKC Autophagy Apoptosis AMPK Akt mTOR Reactive Oxygen Species Caspase Bcl-2 Family PARP Parasite
Daphnetin (7,8-dihydroxycoumarin), one coumarin derivative can be found in plants of the Genus Daphne, is a potent, oral active protein kinase inhibitor, with IC₅₀s of 7.67 μM, 9.33 μM and 25.01 μM for EGFR, PKA and PKC in vitro, respectively. Daphnetin triggers ROS-induced cell apoptosis and induces cytoprotective autophagy by modulating the AMPK/Akt/mTOR pathway. Daphnetin has anti-inflammation activitity and inhibits TNF-α, IL-1ß, ROS, and MDA production. Daphnetin has schizontocidal activity against malaria parasites. Daphnetin can be used for rheumatoid arthritis , cancer and anti-malarian research .

HY-108052

Delphinidin 3-glucoside chloride Delphinidin 3-O-glucoside chloride; Delphinidin 3-O-β-glucoside chloride	Malvaceae Structural Classification Anthocyans Flavonoids Microorganisms Classification of Application Fields Hibiscus sabdariffa Linn. Source classification Plants Disease Research Fields Cancer	EGFR Apoptosis Akt
Delphinidin 3-glucoside chloride (Delphinidin 3-O-glucoside chloride) is an active anthocyanin found in Hibiscus sabdariffa extract. Delphinidin 3-glucoside chloride induces a pro-apoptotic effect in B cell chronic lymphocytic leukaemia (B CLL) . Delphinidin 3-glucoside chloride exerts phytoestrogen activity by binding to ERβ, with an IC₅₀ of 9.7 μM . Delphinidin-3-O-glucoside chloride inhibits EGFR with an IC₅₀ of 2.37 µM . Delphinidin 3-glucoside chloride exhibits antitumor effects through pAKT/IRF1/HOTAIR pathway. Delphinidin 3-glucoside chloride exhibits efficacy against oxidative stress, inhibits platelet activation and endothelial dysfunction .

Cat. No.	Product Name	Chemical Structure

HY-50896S1

Erlotinib-13C6

Erlotinib- ¹³C₆ is a ¹³C-labeled Erlotinib. Erlotinib is a directly acting EGFR tyrosine kinase inhibitor, with an IC50 of 2 nM for human EGFR[1].

HY-15164AS

Icotinib-d4

Icotinib-d₄ is the deuterium-labeled Icotinib (HY-15164A). Icotinib-d₄ (BPI-2009) is a potent and specific EGFR inhibitor with an IC₅₀ of 5 nM; also inhibits mutant EGFR ^L858R, EGFR ^L858R/T790M, EGFR ^T790M and EGFR ^L861Q. Icotinib-d₄ is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-50896S

Erlotinib-d6
Erlotinib-d₆ (CP-358774 D6) is a deuterium labeled Erlotinib (CP-358774). Erlotinib is a directly acting inhibitor EGFR tyrosine kinase inhibitor with an IC50 of 2 nM for human EGFR[1]. Erlotinib-d6 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-50898S1

Lapatinib-d7 dihydrochloride
Lapatinib-d₇ (dihydrochloride) is the deuterium labeled Lapatinib dihydrochloride. Lapatinib (GW572016) dihydrochloride is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively[1].

HY-50898S2

Lapatinib-d5
Lapatinib-d₅ is deuterium labeled Lapatinib. Lapatinib (GW572016) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively[1].

HY-50898S3

Lapatinib-d4-1
Lapatinib-d₄-1 is deuterium labeled Lapatinib. Lapatinib (GW572016) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively[1].

HY-50898S

Lapatinib-d4
Lapatinib-d₄ is the deuterium labeled Lapatinib (HY-50898). Lapatinib is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively[1][2].

HY-50895S1

Gefitinib-d6
Gefitinib-d₆ is the deuterium labeled Gefitinib. Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity[1][2].

HY-15772S

Osimertinib-d6
Osimertinib-d₆ is a deuterium labeled osimertinib. Osimertinib is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer[1].

HY-142283AS

Dosimertinib mesylate
Dosimertinib-d₅ (mesylate) is a potent and orally active EGFR inhibitor. Dosimertinib-d₅ (mesylate) decreases the expression of p-EGFR and p-ERK protein levels. Dosimertinib-d₅ (mesylate) shows antiproliferative and anti-tumor activity. Dosimertinib-d₅ (mesylate) has the potential for the research of non-small-cell lung cancer (NSCLC)[1].

HY-B0793S1

AZ-5104-d2
AZ-5104-d₂ is the deuterium labeled AZ-5104. AZ-5104 is an EGFR inhibitor with IC50s of 1 nM, 6 nM, 1 nM, 25 nM and 7 nM for EGFRL858R/T790M, EGFRL858R, EGFRL861Q, EGFR and ErbB4, respectively[1].

HY-50895S2

Gefitinib-d3

Gefitinib-d₃ (ZD1839-d3) is the deuterium labeled Gefitinib. Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity[1][2].

HY-142283

Dosimertinib
Dosimertinib-d₃-d₃ is a potent and orally active EGFR inhibitor. Dosimertinib-d₃-d₃ decreases the expression of p-EGFR and p-ERK protein levels. Dosimertinib-d₃-d₃ shows antiproliferative and anti-tumor activity. Dosimertinib-d₃-d₃ has the potential for the research of non-small-cell lung cancer (NSCLC)[1].

HY-14596S

Genistein-d4
Genistein-d₄ is the deuterium labeled Genistein. Genistein, a soy isoflavone, is a multiple tyrosine kinases (e.g., EGFR) inhibitor which acts as a chemotherapeutic agent against different types of cancer, mainly by altering apoptosis, the cell cycle, and angiogenesis and inhibiting metastasis[1][2].

HY-32721S

Neratinib-d6
Neratinib-d₆ (HKI-272-d6) is the deuterium labeled Neratinib. Neratinib (HKI-272) is an orally available, irreversible tyrosine kinase inhibitor with IC50s of 59 nM and 92 nM for HER2 and EGFR, respectively.

HY-13272S2

Dacomitinib-d10 dihydrochloride
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
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-100064S

O-Desmethyl gefitinib-d8
O-Desmethyl gefitinib-d₈ is a deuterium labeled O-Desmethyl gefitinib. O-Desmethyl gefitinib is an active metabolite of Gefitinib in human plasma. The formation of O-desmethyl gefitinib is dependent on CYP2D6 activity. O-desmethyl gefitinib inhibits EGFR with an IC50 of 36 nM in subcellular assays[1][2].

HY-10261S1

Afatinib-d4
Afatinib-d₄ is the deuterium labeled Afatinib. Afatinib (BIBW 2992) is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively.

HY-100064S1

O-Desmethyl gefitinib-d6
O-Desmethyl gefitinib-d₆ is the deuterium labeled O-Desmethyl gefitinib. O-Desmethyl gefitinib is an active metabolite of Gefitinib in human plasma. The formation of O-desmethyl gefitinib is dependent on CYP2D6 activity. O-desmethyl gefitinib inhibits EGFR with an IC50 of 36 nM in subcellular assays[1][2].

HY-15772S1

Osimertinib-13C,d3
Osimertinib- ¹³C,d₃ is the deuterium and ¹³C labeled Osimertinib. Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively.

HY-13256AS

Desmethyl Erlotinib-d4

Desmethyl Erlotinib-d₄ is the deuterium labeled Desmethyl Erlotinib. Desmethyl Erlotinib (OSI-420 free base) is an active metabolite of Erlotinib. Erlotinib is a potent EGFR tyrosin kinase inhibitor[1][2]. Desmethyl Erlotinib-d4 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-10261AS

Afatinib-d6 dimaleate
Afatinib-d₆ (dimaleate) is the deuterium labeled Afatinib dimaleate. Afatinib dimaleate is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively[1][2].

HY-12008S1

Erlotinib-13C6 hydrochloride
Erlotinib- ¹³C₆ (hydrochloride) is the ¹³C labeled Erlotinib Hydrochloride[1]. Erlotinib Hydrochloride (CP-358774 Hydrochloride) inhibits purified EGFR kinase with an IC50 of 2 nM[2]. Erlotinib-13C6 (hydrochloride) 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-13653S

(+/-)-Epigallocatechin Gallate-13C3

(+/-)-Epigallocatechin Gallate- ¹³C₃ is the ¹³C-labeled (-)-Epigallocatechin Gallate. (-)-Epigallocatechin Gallate is a tea flavonoid with potent antioxidant, antiinflammatory, and anticarcinogenic properties. (-)-Epigallocatechin Gallate is reported to inhibit EGFR signaling and thereby exert anticancer effects[1]. (-)-Epigallocatechin Gallate (EGCG) is a glutamate dehydrogenase 1/2 (GDH1/2, GLUD1/2) inhibitor. Epigallocatechin-3-gallate induces oxidative phosphorylation (OXPHOS) by activating cytochrome c oxidase.

HY-10260S1

Vandetanib-d4
Vandetanib-d₄ is the deuterium labeled Vandetanib. Vandetanib (ZD6474) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM)[1][2].

HY-10260S

Vandetanib-d6
Vandetanib-d₆ is the deuterium labeled Vandetanib. Vandetanib (D6474) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM)[1].

Cat. No.	Product Name		Classification

HY-15164

Icotinib Hydrochloride 5+ Cited Publications BPI-2009H		Alkynes
Icotinib Hydrochloride (BPI-2009) is a potent and specific *EGFR* inhibitor with an IC₅₀ of 5 nM; also inhibits mutant EGFR ^L858R, EGFR ^L858R/T790M, EGFR ^T790M and EGFR ^L861Q. Icotinib (Hydrochloride) 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-15164A

Icotinib 5+ Cited Publications BPI-2009		Alkynes
Icotinib (BPI-2009) is a potent and specific *EGFR* inhibitor with an IC₅₀ of 5 nM; also inhibits mutant EGFR ^L858R, EGFR ^L858R/T790M, EGFR ^T790M and EGFR ^L861Q. Icotinib 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-50896S1

Erlotinib-13C6 CP-358774-¹³C₆; NSC 718781-¹³C₆; OSI-774-¹³C₆		Alkynes
Erlotinib- ¹³C₆ is a ¹³C-labeled Erlotinib. Erlotinib is a directly acting EGFR tyrosine kinase inhibitor, with an IC50 of 2 nM for human EGFR[1].

HY-150781

EGFR-IN-71		Alkynes
EGFR-IN-71 is a potent narrow spectrum *epidermal growth factor receptor (EGFR)* inhibitor with IC₅₀ values of 3.7 μM. EGFR-IN-71 can be used for researching chordoma . EGFR-IN-71 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-50896S

Erlotinib-d6 CP-358774-d₆; NSC 718781-d₆; OSI-774-d₆		Alkynes
Erlotinib-d₆ (CP-358774 D6) is a deuterium labeled Erlotinib (CP-358774). Erlotinib is a directly acting inhibitor EGFR tyrosine kinase inhibitor with an IC50 of 2 nM for human EGFR[1]. Erlotinib-d6 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-147858

PROTAC EGFR degrader 7		Alkynes
PROTAC EGFR degrader 7 (compound 13b) is a potent and selective CRBN-recruiting PROTAC EGFR ^L858R/T790M degrader, with a DC₅₀ of 13.2 nM. PROTAC EGFR degrader 7 inhibits NCI–H1975 cells proliferation, with an IC₅₀ of 46.82 nM. PROTAC EGFR degrader 7 significantly induces apoptosis and G2/M phase arrest in NCI–H1975 cell. PROTAC EGFR degrader 7 shows antitumor activity, and can be used for non-small cell lung cancer (NSCLC) research . PROTAC EGFR degrader 7 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-50896

Erlotinib Maximum Cited Publications 74 Publications Verification CP-358774; NSC 718781; OSI-774		Alkynes
Erlotinib (CP-358774) is a directly acting *EGFR* tyrosine kinase inhibitor, with an IC₅₀ of 2 nM for human EGFR. Erlotinib reduces EGFR autophosphorylation in intact tumor cells with an IC₅₀ of 20 nM. Erlotinib is used for the treatment of non-small cell lung cancer . Erlotinib is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-104066

Theliatinib Xiliertinib; HMPL-309		Alkynes
Theliatinib (Xiliertinib) is a potent, ATP-competitive, orally active and highly selective *EGFR* inhibitor with a K_i of 0.05 nM and an IC₅₀ of 3 nM. Theliatinib has an IC₅₀ of 22 nM for EGFR T790M/L858R mutant. Theliatinib shows >50-fold selectivity for *EGFR* than other kinases . Theliatinib 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-104066A

Theliatinib tartrate Xiliertinib tartrate; HMPL-309 tartrate		Alkynes
Theliatinib (Xiliertinib) tartrate is a potent, ATP-competitive, orally active and highly selective *EGFR* inhibitor with a K_i of 0.05 nM and an IC₅₀ of 3 nM. Theliatinib has an IC₅₀ of 22 nM for EGFR T790M/L858R mutant. Theliatinib shows >50-fold selectivity for *EGFR* than other kinases . Theliatinib (tartrate) 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-12008

Erlotinib Hydrochloride Maximum Cited Publications 74 Publications Verification CP-358774 hydrochloride; NSC 718781 hydrochloride; OSI-774 hydrochloride		Alkynes
Erlotinib Hydrochloride (CP-358774 Hydrochloride) inhibits purified *EGFR* kinase with an IC₅₀ of 2 nM. Erlotinib (Hydrochloride) 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-12008A

Erlotinib mesylate CP-358774 mesylate; NSC 718781 mesylate; OSI-774 mesylate		Alkynes
Erlotinib mesylate (CP-358774 mesylate) inhibits purified *EGFR* kinase with an IC₅₀ of 2 nM. Erlotinib (mesylate) 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-13256

Desmethyl Erlotinib hydrochloride 3 Publications Verification OSI-420; CP-373420 hydrochloride		Alkynes
Desmethyl Erlotinib hydrochloride (OSI-420) is an active metabolite of Erlotinib. Erlotinib is a potent EGFR tyrosin kinase inhibitor . Desmethyl Erlotinib (hydrochloride) 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-13256A

Desmethyl Erlotinib 3 Publications Verification OSI-420 free base; CP-373420		Alkynes
Desmethyl Erlotinib (OSI-420 free base) is an active metabolite of Erlotinib. Erlotinib is a potent EGFR tyrosin kinase inhibitor . Desmethyl Erlotinib 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-10223

CUDC-101 5+ Cited Publications		Alkynes
CUDC-101 is a potent inhibitor of HDAC, *EGFR, and HER2* with IC₅₀s of 4.4, 2.4, and 15.7 nM, respectively. CUDC-101 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-139300

Epitinib HMPL-813		Alkynes
Epitinib is an orally active and selective epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) designed for optimal brain penetration. Epitinib can be used for the research of cancer . Epitinib 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-13256AS

Desmethyl Erlotinib-d4		Alkynes
Desmethyl Erlotinib-d₄ is the deuterium labeled Desmethyl Erlotinib. Desmethyl Erlotinib (OSI-420 free base) is an active metabolite of Erlotinib. Erlotinib is a potent EGFR tyrosin kinase inhibitor[1][2]. Desmethyl Erlotinib-d4 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-139300A

Epitinib succinate HMPL-813 succinate		Alkynes
Epitinib succinate is an orally active and selective epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) designed for optimal brain penetration. Epitinib succinate can be used for the research of cancer . Epitinib (succinate) 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-12008S1

Erlotinib-13C6 hydrochloride CP-358774-¹³C₆ hydrochloride; NSC 718781-¹³C₆ hydrochloride; OSI-774-¹³C₆ hydrochloride		Alkynes
Erlotinib- ¹³C₆ (hydrochloride) is the ¹³C labeled Erlotinib Hydrochloride[1]. Erlotinib Hydrochloride (CP-358774 Hydrochloride) inhibits purified EGFR kinase with an IC50 of 2 nM[2]. Erlotinib-13C6 (hydrochloride) 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-150782

UNC-CA359		Alkynes
UNC-CA359 is a potent epidermal growth factor receptor (EGFR) inhibitor, with an IC₅₀ value of 18 nM. UNC-CA359 exhibits strong anti-tumor activity, can be used to Chordoma research . UNC-CA359 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-135699

TD52 1 Publications Verification		Alkynes
TD52, an Erlotinib (HY-50896) derivative, is an orally active, potent cancerous inhibitor of protein phosphatase 2A (CIP2A) inhibitor. TD52 mediates the apoptotic effect in triple-negative breast cancer (TNBC) cells via regulating the CIP2A/PP2A/p-Akt signalling pathway. TD52 indirectly reduced CIP2A by disturbing Elk1 binding to the CIP2A promoter. TD52 has less p-EGFR inhibition and has potent anti-cancer activity . TD52 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-135699A

TD52 dihydrochloride 1 Publications Verification		Alkynes
TD52 dihydrochloride, an Erlotinib (HY-50896) derivative, is an orally active, potent cancerous inhibitor of protein phosphatase 2A (CIP2A) inhibitor. TD52 dihydrochloride mediates the apoptotic effect in triple-negative breast cancer (TNBC) cells via regulating the CIP2A/PP2A/p-Akt signalling pathway. TD52 dihydrochloride indirectly reduced CIP2A by disturbing Elk1 binding to the CIP2A promoter. TD52 dihydrochloride has less p-EGFR inhibition and has potent anti-cancer activity . TD52 (dihydrochloride) 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-131088

N3-PEG8-Phe-Lys-PABC-Gefitinib		Azide
N3-PEG8-Phe-Lys-PABC-Gefitinib is a agent-linker conjugate for ADC with potent antitumor activity by using the anti-tumor agent, Gefitinib (orally active EGFR tyrosine kinase inhibitor), linked via the cleavable linker N3-PEG8-Phe-Lys-PABC. N3-PEG8-Phe-Lys-PABC-Gefitinib is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.

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