target s/EGFR

By Targets:	EGFR (9) Apoptosis (2) Aurora Kinase (1) Autophagy (2) BMX Kinase (1) Btk (1) CDK (1) Ephrin Receptor (1) Necroptosis (1) Phosphodiesterase (PDE) (1) PROTACs (1) VEGFR (2)
By Research Areas:	Cancer (10)

Targets Recommended: EGFR Target Protein Ligand-Linker Conjugates Ligands for Target Protein for PROTAC

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-19985A

(3S,4S)-PF-06459988	EGFR	Cancer
(3S, 4S)-PF-06459988 is the S enantiomer of PF-06459988 with less active. PF-06459988 is a potent irreversible inhibitor of T790M mutant epidermal growth factor receptor (EGFR). PF-06459988 has excellent selectivity against *EGFR* wild-type while possessing a minimally reactive electrophile that reduces the propensity of off-target labeling .

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-146349

PROTAC EGFR degrader 4	PROTACs EGFR Autophagy	Cancer
PROTAC EGFR degrader 4 is a potent PROTAC targeting mutant *EGFR*.PROTAC EGFR degrader 4 induces EGFR ^del19 and EGFR ^L858R/T790M degradation with *DC₅₀s of 0.51 and 126 nM, respectively. PROTAC EGFR* degrader 4 significantly inhibits growth of HCC827 and H1975 cell lines with IC₅₀s of 0.83 and 203.1 nM, respectively. Induced EGFR degradation is related to autophagy .

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-161275

BI-4732	EGFR	Cancer
BI-4732 a potent inhibitor EGFR-activating (E19del and L858R) and T790M mutations, with high blood-brian barrier penetration, targeting a broad range of EGFR mutations, including C797S. BI-4732 has anti-tumor 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 *IC₅₀*s of 0.3, 16, 1.5, 8.7, and 1.4 nM.

HY-80002

BMX-IN-1 4 Publications Verification BMX kinase inhibitor	Btk BMX Kinase	Cancer
BMX-IN-1 is a selective, irreversible inhibitor of bone marrow tyrosine kinase on chromosome X (BMX) that targets Cys ⁴⁹⁶ in the BMX ATP binding domain with an IC₅₀ of 8 nM, also targets the related Bruton’s tyrosine kinase (BTK) with an IC₅₀ value of 10.4 nM, but is more than 47-656-fold less potent against Blk, JAK3, EGFR, Itk, or Tec activity.

HY-P99155

Zalutumumab	EGFR	Cancer
Zalutumumab is a high affinity, completely human IgG1 monoclonal antibody targeting *EGFR. Zalutumumab binds to domain III of the EGF receptor and acts by blocking the binding of EGF and by sterically interfering with the active conformation of the receptor. Zalutumumab binds with IgG and its Fab fragment with EC₅₀*s of 7 and 19 nM, respectively. Zalutumumab can be used for the research of cancer .

HY-16558

Butein 3 Publications Verification 2’,3,4,4’-tetrahydroxy Chalcone	EGFR Autophagy Apoptosis Phosphodiesterase (PDE)	Cancer
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-149407

Multi-kinase-IN-4	VEGFR CDK EGFR Necroptosis Apoptosis	Cancer
Multi-kinase-IN-4 (compound 5d) is multi-targeted kinase inhibitor, including VEGFR2, *EGFR, HER2, and CDK2, with IC₅₀* values of 0.33, 0.22, 0.18 and 2.09 μM, respectively. Multi-kinase-IN-4 shows broad-spectrum anti-cancer activities against HepG2, MCF-7, MDA-231, and HeLa cell lines (IC₅₀ = 1.94–7.1 µM), but exhibits lower toxicity in the WI-38 cells (IC₅₀ = 40.85 µM). Multi-kinase-IN-4 induces apoptosis and arrests cell cycle at S phase in HepG2 cells. Multi-kinase-IN-4 has the potential for the research of cancer .

Cat. No.	Product Name

HY-L075

Anti-Lung Cancer Compound Library	1835 compounds
Lung cancer is a major global health problem, as it is the leading cause of cancer-related deaths worldwide. Lung cancer is divided into two categories: small cell lung cancer and non-small cell lung cancer (NSCLC). Non-small cell lung cancer accounts for about 85 percent of lung cancers. As with all cancers, lung cancer may be treated with surgery, chemotherapy, radiation therapy, targeted therapy, immunotherapy or a combination thereof. Targeted therapy is one of the most exciting developments in lung cancer medicine, especially for NSCLC. Extensive genomic characterization of NSCLC has led to the identification of molecular subtypes of NSCLC that are oncogene addicted and exquisitely sensitive to targeted therapies. These include activating mutations in epidermal growth factor receptor (EGFR) and BRAF or echinoderm microtubule-associated protein-like 4 (EML4)-anaplastic lymphoma kinase (ALK) fusions and ROS1 receptor tyrosine kinase fusions. These are important targets for target therapy. MCE offers a unique collection of 1835 compounds with identified and potential anti-lung cancer activity. These compounds target lung cancer’s major targets and signaling pathways. MCE anti-lung cancer compound library is a useful tool for anti-lung cancer drugs screening and other related research.

Anti-Lung Cancer Compound Library

1835 compounds

Lung cancer is a major global health problem, as it is the leading cause of cancer-related deaths worldwide. Lung cancer is divided into two categories: small cell lung cancer and non-small cell lung cancer (NSCLC). Non-small cell lung cancer accounts for about 85 percent of lung cancers.

As with all cancers, lung cancer may be treated with surgery, chemotherapy, radiation therapy, targeted therapy, immunotherapy or a combination thereof. Targeted therapy is one of the most exciting developments in lung cancer medicine, especially for NSCLC. Extensive genomic characterization of NSCLC has led to the identification of molecular subtypes of NSCLC that are oncogene addicted and exquisitely sensitive to targeted therapies. These include activating mutations in epidermal growth factor receptor (EGFR) and BRAF or echinoderm microtubule-associated protein-like 4 (EML4)-anaplastic lymphoma kinase (ALK) fusions and ROS1 receptor tyrosine kinase fusions. These are important targets for target therapy.

MCE offers a unique collection of 1835 compounds with identified and potential anti-lung cancer activity. These compounds target lung cancer’s major targets and signaling pathways. MCE anti-lung cancer compound library is a useful tool for anti-lung cancer drugs screening and other related research.

Cat. No.	Product Name	Target	Research Area

HY-P99155

Zalutumumab	EGFR	Cancer
Zalutumumab is a high affinity, completely human IgG1 monoclonal antibody targeting *EGFR. Zalutumumab binds to domain III of the EGF receptor and acts by blocking the binding of EGF and by sterically interfering with the active conformation of the receptor. Zalutumumab binds with IgG and its Fab fragment with EC₅₀*s of 7 and 19 nM, respectively. Zalutumumab can be used for the research of cancer .

Cat. No.	Product Name	Category	Target	Chemical Structure

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).

MCE Japan Authorized Agent ナミキ商事株式会社コスモ・バイオ株式会社
Salutation			Country or Region *
Applicant Name *			Organization Name *
Department *
Email Address *			Product Name *
Cat. No.			Requested quantity *
Phone Number *
Remarks

Inhibitors & Agonists

Screening Libraries

Inhibitory Antibodies

Natural
Products