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Pathways Recommended:	Protein Tyrosine Kinase/RTK

Results for "

EGFR tyrosine kinase inhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Btk (4) EGFR (154) Tyrosine Hydroxylase (2) ADC Antibody (1) Akt (6) Apoptosis (34) Autophagy (40) Bacterial (1) Bcr-Abl (2) BMX Kinase (1) c-Met/HGFR (2) CaMK (2) Casein Kinase (1) CDK (1) COX (1) DNA-PK (1) Drug Intermediate (1) Drug Metabolite (5) Drug-Linker Conjugates for ADC (4) Endogenous Metabolite (3) Enterovirus (1) Ephrin Receptor (1) Epigenetic Reader Domain (2) ERK (9) Ferroptosis (15) FGFR (6) GLUT (1) GPR35 (2) HCV (3) Histone Acetyltransferase (2) IGF-1R (2) Influenza Virus (3) IRAK (2) Isotope-Labeled Compounds (15) JAK (3) Mitosis (2) MMP (1) mTOR (1) p38 MAPK (3) PDGFR (5) Phosphatase (1) Phosphodiesterase (PDE) (2) PI3K (1) PKA (2) PKC (2) Ras (1) Reference Standards (24) RET (1) Ser/Thr Kinase (1) Src (7) STAT (4) TAM Receptor (1) TGF-β Receptor (1) Topoisomerase (1) Trk Receptor (2) TRP Channel (4) Tyrosinase (3) VEGFR (14)
By Research Areas:	Cancer (172) Cardiovascular Disease (4) Infection (18) Inflammation/Immunology (7) Metabolic Disease (10) Neurological Disease (8)
Click Chemistry:	ADC Synthesis (1) Azide (2) Alkynes (7)

184

Inhibitors & Agonists

Fluorescent Dyes

Biochemical Assay Reagents

Inhibitory Antibodies

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

GMP Molecules

Targets Recommended: EGFR Btk Syk Pyk2 TNK1 Tyrosine Hydroxylase DYRK BRK FAK FLT3 Anaplastic lymphoma kinase (ALK)

Art. -Nr.	Produktname	Target	Forschungsgebiete	Chemical Structure

HY-14596

Genistein Maximum Cited Publications 88 Publications Verification NPI 031L	EGFR Autophagy Apoptosis Endogenous Metabolite	Cancer
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-50896

Erlotinib 130+ Cited Publications CP-358774; NSC 718781; OSI-774	EGFR Autophagy	Cancer
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-50898

Lapatinib 90+ Cited Publications GW572016; GW2016	EGFR Autophagy Ferroptosis	Infection Neurological Disease Metabolic Disease Cancer
Lapatinib (GW572016) is a potent, orally active 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 .

HY-12000

AG490 160+ Cited Publications Tyrphostin AG490; Tyrphostin B42	EGFR STAT JAK Autophagy	Cancer
AG490 (Tyrphostin AG490) is a tyrosine kinase inhibitor that inhibits *EGFR, Stat-3* and JAK2/3.

HY-13524

AG-1478 45+ Cited Publications Tyrphostin AG-1478; NSC 693255	EGFR HCV Influenza Virus	Infection Cardiovascular Disease Metabolic Disease Cancer
AG-1478 (Tyrphostin AG-1478) is a selective *EGFR* tyrosine kinase inhibitor with IC₅₀ of 3 nM. AG-1478 has antiviral effects against HCV and encephalomyocarditis virus (EMCV).

HY-10260

Vandetanib 25+ Cited Publications ZD6474	VEGFR Autophagy Apoptosis	Neurological Disease Inflammation/Immunology Cancer
Vandetanib (D6474) is a potent, orally active, and blood-brain-barrier penetrate 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) .

HY-148810

Zongertinib 1 Publications Verification BI 1810631	c-Met/HGFR	Cancer
Zongertinib (BI 1810631) is a potent and selective HER2 and *EGFR* tyrosine kinase inhibitor with IC₅₀ values of 13 nM and 579 nM, respectively. Zongertinib has antitumor activity and can be used in the study of multiple solid tumors .

HY-19730

Olmutinib 10+ Cited Publications HM61713; BI 1482694	EGFR	Cancer
Olmutinib (HM61713; BI-1482694) is an orally active and irreversible third **EGFR tyrosine kinase** inhibitor that binds to a cysteine residue near the kinase domain. Olmutinib is used for NSCLC .

HY-101084

NSC 228155 15+ Cited Publications	EGFR Histone Acetyltransferase Epigenetic Reader Domain	Cancer
NSC 228155 is an activator of *EGFR, binds to the extracellular region of EGFR* and enhance tyrosine phosphorylation of EGFR . NSC 228155 is also a potent inhibitor of KIX-KID interaction, inhibits kinase-inducible domain (KID) from CREB and KID-interacting domain (KIX) from CBP, with an IC₅₀ of 0.36 μM .

HY-112299

Zipalertinib 3 Publications Verification TAS6417; CLN-081	EGFR Apoptosis	Cancer
Zipalertinib (TAS6417; CLN-081) is a highly effective, orally active and pan-mutation-selective EGFR tyrosine kinase inhibitor with a unique scaffold fitting into the ATP-binding site of the EGFR hinge region, with IC₅₀ values ranging from 1.1-8.0 nM .

HY-50898A

Lapatinib ditosylate 90+ Cited Publications GW572016 ditosylate; GW2016 ditosylate	EGFR Autophagy Ferroptosis	Infection Neurological Disease Metabolic Disease Cancer
Lapatinib ditosylate (GW572016 ditosylate) is a potent, orally active 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 .

HY-50895A

Gefitinib hydrochloride Maximum Cited Publications 200 Publications Verification ZD-1839 hydrochloride	EGFR	Cancer
Gefitinib hydrochloride (ZD1839 hydrochloride) is a potent, selective and orally active **EGFR tyrosine kinase** inhibitor with an IC₅₀ of 33 nM. Gefitinib hydrochloride selectively inhibits EGF-stimulated tumor cell growth (IC₅₀ of 54 nM) and that blocks EGF-stimulated *EGFR* autophosphorylation in tumor cells. Gefitinib hydrochloride also induces autophagy. Gefitinib hydrochloride has antitumour activity .

HY-50898B

Lapatinib ditosylate monohydrate 90+ Cited Publications GW572016 ditosylate monohydrate; GW2016 ditosylate monohydrate	EGFR Autophagy Ferroptosis	Infection Metabolic Disease Cancer
Lapatinib ditosylate monohydrate (GW572016 ditosylate monohydrate) is a potent, orally active 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 .

HY-10322

Falnidamol 4 Publications Verification BIBX 1382	EGFR	Cancer
Falnidamol (BIBX 1382) is an orally active, selective **EGFR tyrosine kinase** inhibitor with an IC₅₀ of 3 nM. Falnidamol displays > 1000-fold lower potency against ErbB2 (IC₅₀=3.4 μM) and a range of other related tyrosine kinases (IC₅₀>10 μM). Falnidamol is a pyrimido-pyrimidine compound and has anti-cancer activity .

HY-117155

PKI-166 1 Publications Verification	EGFR	Cancer
PKI-166 is a potent, selective and orally bioavailable **EGFR tyrosine kinase** inhibitor, with an IC₅₀ of 0.7 nM .

HY-19815

Olafertinib CK-101; RX518	EGFR	Cancer
Olafertinib (CK-101) is an orally available, third generation and irreversible epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI). Olafertinib selectively inhibits both EGFR-TKI-sensitizing and resistance mutations with minimal activity on wild-type EGFR. Olafertinib can be used in research for non-small cell lung cancer (NSCLC) with EGFR mutations and other advanced malignancies .

HY-112823A

Almonertinib mesylate 5+ Cited Publications 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-136430

JCN037 JGK037	EGFR	Cancer
JCN037 (JGK037) is non-covalent and BBB-penetrant *EGFR* tyrosine kinase inhibitor, with IC₅₀ values of 2.49 nM, 3.95 nM, 4.48 nM for EGFR, p-wtEGFR and pEGFRvⅢ, respectively .

HY-80002

BMX-IN-1 5+ Cited Publications 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-109189

Rezivertinib 1 Publications Verification BPI-7711	EGFR	Cancer
Rezivertinib (BPI-7711) is an orally active, highly selective and irreversible third-generation EGFR tyrosine kinase inhibitor (TKI). Rezivertinib exhibits high potency against the common activation EGFR and the resistance T790M mutations. Rezivertinib has excellent central nervous system (CNS) penetration and has antitumor activity .

HY-13896

PD168393 3 Publications Verification	EGFR Autophagy Apoptosis	Cancer
PD168393 is a potent, selective and cell-permeable inhibitor of **EGFR tyrosine kinase and ErbB2. PD168393 irreversiblely inactivates EGF receptor ( IC₅₀**=0.7 nM) and is inactive against insulin receptor, PDGFR, FGFR and PKC .

HY-18963

Lavendustin A 1 Publications Verification RG-14355	EGFR	Cancer
Lavendustin A (RG-14355) is a potent, selective and ATP-competitive inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase, with an IC₅₀ of 11 nM. Lavendustin A does not inhibit protein kinase A or C. Lavendustin A can suppress VEGF-induced angiogenesis .

HY-20878

Tyrphostin AG 879 3 Publications Verification AG 879	Trk Receptor EGFR Apoptosis	Cancer
Tyrphostin AG 879 (AG 879) is a tyrosine kinase inhibitor that inhibits TrKA phosphorylation (IC₅₀ of 10 μM), but not TrKB and TrKC. Tyrphostin AG 879 is also a selective ErbB2 tyrosine kinase inhibitor with an IC₅₀ of 1 μM, and has at least 500-fold higher selectivity to ErbB2 than EGFR. Tyrphostin AG 879 has anticancer activity .

HY-139300

Epitinib HMPL-813	EGFR	Cancer
Epitinib (HMPL-813) is a selective, orally active, blood-brain barrier-permeable *EGFR* tyrosine kinase inhibitor. Epitinib is applicable to research on EGFR ^T790M-positive non-small cell lung cancer with brain metastasis and advanced solid tumors .

HY-112412

PDGFR Tyrosine kinase-IN-1	PDGFR	Neurological Disease
PDGFR Tyrosine kinase-IN-1, a multikinase inhibitor, inhibits PDGFR, EGFR, FGFR, PKA, and PKC, respectively. PDGFR Tyrosine kinase-IN-1 can be used for the research of amyotrophic lateral sclerosis .

HY-108484

PP 3	EGFR	Cancer
PP 3 (Compound 3) is an **EGFR tyrosine kinase** inhibitor with an IC₅₀ of 2.7 μM .

HY-101820

Simotinib	EGFR	Cancer
Simotinib is a selective, specific, and orally bioavailable *EGFR* tyrosine kinase inhibitor, with an IC₅₀ of 19.9 nM. Antineoplastic activities .

HY-153110

Larotinib	EGFR IRAK Btk	Cancer
Larotinib is a potent broad-spectrum and orally active tyrosine kinase inhibitor (TKI) with *EGFR* as the main target with an IC₅₀ of 0.6 nM .

HY-12806

AG1557	EGFR	Cancer
AG1557 is a specific and ATP competitive inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase, has a pIC₅₀ value of 8.194 .

HY-118532

Tyrphostin AG30 1 Publications Verification AG30	EGFR	Cancer
Tyrphostin AG30 (AG30) is a potent and selective **EGFR tyrosine kinase** inhibitor. Tyrphostin AG30 (AG30) selectively inhibits self renewal induction by c-ErbB, and is able to inhibit activation of STAT5 by c-ErbB in primary erythroblasts .

HY-50898S4

Lapatinib-d7 GW572016-d₇; GW2016-d₇	Isotope-Labeled Compounds Autophagy EGFR Ferroptosis	Cancer
Lapatinib-d₇ (GW572016-d₇) is deuterium labeled Lapatinib. Lapatinib (GW572016) is a potent, orally active 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 .

HY-153110A

Larotinib mesylate hydrate	EGFR IRAK Btk	Cancer
Larotinib mesylate hydrate is a potent broad-spectrum and orally active tyrosine kinase inhibitor (TKI) with *EGFR* as the main target with an IC₅₀ of 0.6 nM .

HY-15772S3

Asandeutertinib asandeutertinibum; Osimertinib-d₃; AZD-9291-d₃	EGFR	Cancer
Asandeutertinib (Osimertinib-d3; AZD-9291-d3) is a epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, with antineoplastic effect .

HY-W013857

Lavendustin C	CaMK EGFR Src	Cancer
Lavendustin C is a potent *Ca ²⁺ calmodulin-dependent kinase* II (CaMK II)** inhibitor with an IC₅₀ of 0.2 µM. Lavendustin C inhibits *EGFR*-associated tyrosine kinase (IC₅₀=0.012 µM) and pp60 ^c-src(+) kinase (IC₅₀=0.5 µM) .

HY-156912

Tyrosine kinase-IN-7	EGFR	Cancer
Tyrosine kinase-IN-7 (compound 13h) is an inhibitor of the tyrosine kinase EGFR. The IC₅₀s for inhibiting EGFR(WT) and EGFR(T790M) are 0.630 μM and 0.956 μM respectively. Tyrosine kinase-IN-7 has antitumor activity against four cancer cell lines (HepG2, HCT-116, MCF-7, and A431) with IC₅₀s of 13.02 μM, 10.14 μM, 12.68 μM, and 47.05 μM, respectively .

HY-129510

4-Methyl erlotinib	EGFR Mitosis	Cancer
4-Methyl erlotinib, is a potent and selective epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor. 4-Methyl erlotinib potently inhibits EGF-mediated tumor cell mitosis by reducing EGFr-specific tyrosine phosphorylation. Using a mouse model of human tumor transplantation, 4-Methyl erlotinib demonstrated significant and sustained suppression of EGFr phosphotyrosine levels, resulting in significant growth inhibition of EGFr-dependent human cancers .

HY-156741A

EGFR-IN-87 hydrochloride	EGFR	Cancer
EGFR-IN-87 (Compound Example 2) hydrochloride is a *EGFR* tyrosine kinase inhibitor. EGFR-IN-87 hydrochloride 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 hydrochloride can be used for cancer diseases research .

HY-50898S1

Lapatinib-d7 dihydrochloride GW572016-d7 dihydrochloride; GW2016-d7 dihydrochloride	Isotope-Labeled Compounds EGFR Autophagy Ferroptosis	Cancer
Lapatinib-d₇ dihydrochloride is the deuterium labeled Lapatinib dihydrochloride. Lapatinib (GW572016) dihydrochloride is a potent, orally active 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 .

HY-10260B

Vandetanib hydrochloride ZD6474 hydrochloride	VEGFR Autophagy Apoptosis	Cancer
Vandetanib hydrochloride (D6474 hydrochloride) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC₅₀=40 nM). Vandetanib hydrochloride also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC₅₀=110 nM) and *EGFR/HER1* (IC₅₀=500 nM) .

HY-50898S

Lapatinib-d4 GW572016-d₄; GW2016-d₄	EGFR Autophagy Ferroptosis	Cancer
Lapatinib-d₄ is the deuterium labeled Lapatinib (HY-50898). Lapatinib is a potent, orally active 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 .

HY-117852

CGP-59326 TRX-13	EGFR Tyrosinase	Cancer
CGP-59326 (TRX-13) is a highly potent and selective epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (IC₅₀=0.027 μM). CGP-59326 blocks the EGFR signaling pathwa, demonstrating highly selective inhibition of EGFR-dependent tumor cells. CGP-59326 is promising for research of cancers .

HY-101958

Tyrphostin 25 AG82; Tyrphostin A 25; Tyrphostin AG 82; RG-50875	EGFR GPR35	Inflammation/Immunology Cancer
Tyrphostin 25 (AG82) is a specific inhibitor of the *EGFR* tyrosine kinase with an IC₅₀ value of 3 µM in A431 cells. Tyrphostin 25 is also a GPR35 agonist with an EC₅₀ of 5.3 µM .

HY-13524A

AG-1478 hydrochloride Tyrphostin AG-1478 hydrochloride; NSC 693255 hydrochloride	EGFR HCV Influenza Virus	Infection Cardiovascular Disease Metabolic Disease Cancer
AG-1478 hydrochloride (Tyrphostin AG-1478 hydrochloride) is a selective *EGFR* tyrosine kinase inhibitor with IC₅₀ of 3 nM. AG-1478 hydrochloride has antiviral effects against HCV and encephalomyocarditis virus (EMCV) .

HY-148871

Mc-Val-Cit-PAB-Gefitinib chloride	Drug-Linker Conjugates for ADC	Cancer
Mc-Val-Cit-PAB-Gefitinib chloride is a agent-linker conjugates for ADC. Mc-Val-Cit-PAB-Gefitinib chloride consists of Gefitinib (HY-50895) (an *EGFR* tyrosine kinase inhibitor) and the ADC linker Mc-Val-Cit-PAB .

HY-19730A

Olmutinib hydrochloride HM61713 hydrochloride; BI 1482694 hydrochloride	EGFR	Cancer
Olmutinib hydrochloride is an orally active and irreversible third **EGFR tyrosine kinase** inhibitor that binds to a cysteine residue near the kinase domain. Olmutinib hydrochloride is used for NSCLC .

HY-101820A

Simotinib hydrochloride	EGFR	Cancer
Simotinib hydrochloride is a selective, specific, and orally bioavailable *EGFR* tyrosine kinase inhibitor, with an IC₅₀ of 19.9 nM. Antineoplastic activities .

HY-144445

NSC114126	EGFR	Cancer
NSC114126 is a potent and orally active inhibitor of EGFR tyrosine kinase (EGFR-TK). NSC114126 has strong antiproliferative activities. NSC114126 has the potential for the research of cancer diseases .

HY-100636

Gefitinib N-oxide	EGFR	Cancer
Gefitinib N-oxide is the N-oxide derivative of Gefitinib. Gefitinib is an **EGFR tyrosine kinase** inhibitor, with IC₅₀ of 2-37 nM in NR6wtEGFR cells .

HY-W174279

Tyrphostin 8	EGFR Ras Phosphatase	Metabolic Disease
Tyrphostin 8 is a **tyrosine kinase, with an IC₅₀ of 560 μM for EGFR kinase. Tyrphostin 8 is also a GTPase** inhibitor. Tyrphostin 8 can inhibit the protein serine/threonine phosphatase calcineurin (IC₅₀=21 μM) .

HY-156741

EGFR-IN-87	EGFR	Cancer
EGFR-IN-87 (Compound Example 2) 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 .

Art. -Nr.	Produktname	Target	Research Area	Image

HY-P990947

Tilatamig AZD9592 Antibody	ADC Antibody EGFR	Cancer
Tilatamig (AZD9592 Antibody) is a human antibody of the Ig (G1-κ_G1-λ2) subtype that targets *EGFR/MET. Tilatamig conjugates with the Top1* inhibitor AZ14170133 (HY-145399) to form the antibody-drug conjugate (ADC) Tilatamig samrotecan (HY-171124) (AZD9592). Tilatamig accurately targets NSCLC models including EGFR-mutant, EGFR-wildtype, and EGFR tyrosine kinase inhibitor-treated ones, and its activity correlates with high expression of *EGFR, c-MET* and SLFN11. Tilatamig is available for in vivo anti-tumor studies in patient-derived xenograft models of non-small cell lung cancer (NSCLC) and head and neck squamous cell carcinoma (HNSCC) .

Art. -Nr.	Produktname	Category	Target	Chemical Structure

HY-14596

Genistein Maximum Cited Publications 88 Publications Verification NPI 031L	Classification of Application Fields Anti-aging Plants Endogenous metabolite Human Gut Microbiota Metabolites Flavonoids Microorganisms Leguminosae Glycine max (L.) merr Sunscreen Phenols Polyphenols Cosmetic Research Glycyrrhiza uralensis Fisch. Disease Research Fields Isoflavones Source Classification 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-16558

Butein 5+ Cited Publications 2’,3,4,4’-tetrahydroxy Chalcone	Chalcones Flavonoids other families Classification of Application Fields Anti-aging Phenols Polyphenols Plants Disease Research Fields Source Classification 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-14596R

Genistein (Standard) Maximum Cited Publications 88 Publications Verification NPI 031L (Standard)	Classification of Application Fields Anti-aging Plants Endogenous metabolite Human Gut Microbiota Metabolites Flavonoids Leguminosae Glycine max (L.) merr Sunscreen Phenols Cosmetic Research Glycyrrhiza uralensis Fisch. Disease Research Fields Source Classification Cancer	Reference Standards 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-18963

Lavendustin A 1 Publications Verification RG-14355	Microorganisms Classification of Application Fields Ketones, Aldehydes, Acids Phenols Polyphenols Disease Research Fields Source Classification Cancer	EGFR
Lavendustin A (RG-14355) is a potent, selective and ATP-competitive inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase, with an IC₅₀ of 11 nM. Lavendustin A does not inhibit protein kinase A or C. Lavendustin A can suppress VEGF-induced angiogenesis .

HY-N4201

β-Hydroxyisovalerylshikonin	Quinones Classification of Application Fields Phenols Polyphenols Plants Lithospermum erythrorhizon Sieb. et Zucc. Naphthalene Quinones Disease Research Fields Boraginaceae Cancer Source Classification	EGFR Src
Beta-hydroxyisovalerylshikonin is a natural product isolated from Lithospermum erythrorhizon, acts as a potent inhibitor of *protein tyrosine* kinases (PTK), with IC₅₀*s 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-N12726

Halociline	Microorganisms Marine natural products Phenols Marine microorganism Source Classification	p38 MAPK MMP
Halociline, a derivative of alkaloids, that can be isolated from the marine fungus Penicillium griseofulvum. Halociline targets MAPK1, MMP-9, and PIK3CA in gastric cancer cells, potentially mediated by diverse pathways including cancer, lipid metabolism, atherosclerosis, and EGFR tyrosine kinase inhibitor resistance. Halociline possesses antimicrobial, antioxidant and biofilm inhibitory activities .

HY-16558R

Butein (Standard) 2’,3,4,4’-tetrahydroxy Chalcone (Standard)	Structural Classification Chalcones Flavonoids other families Phenols Polyphenols Plants Source Classification	Reference Standards EGFR Autophagy Apoptosis Phosphodiesterase (PDE)
Butein (Standard) is the analytical standard of Butein. This product is intended for research and analytical applications. 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 p60c-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-N14635

Paeciloquinone A	Microorganisms Xanthones Phenols Source Classification	EGFR
Paeciloquinone A can inhibit *EGFR* protein tyrosine kinase. Paeciloquinone A inhibits the V-abl protein tyrosine kinase with an IC₅₀ of 0.59 μM .

HY-N14637

Paeciloquinone C	Microorganisms Xanthones Phenols Source Classification	EGFR
Paeciloquinone C can inhibit the *EGFR* protein tyrosine kinase. Paeciloquinone C inhibits the V-abl protein tyrosine *K_i*nase with an IC₅₀ of 0.56 μM .

HY-N14638

Paeciloquinone D	Microorganisms Xanthones Phenols Source Classification	EGFR
Paeciloquinone D can inhibit the *EGFR* protein tyrosine kinase .

HY-N14639

Paeciloquinone E	Microorganisms Xanthones Phenols Source Classification	EGFR
Paeciloquinone E can inhibit the *EGFR* protein tyrosine kinase .

HY-N14640

Paeciloquinone F	Microorganisms Xanthones Phenols Source Classification	EGFR
Paeciloquinone F can inhibit the *EGFR* protein tyrosine kinase .

HY-N14636

Paeciloquinone B	Microorganisms Xanthones Phenols Source Classification	EGFR
Paeciloquinone B can inhibit the *EGFR* protein tyrosine kinase .

HY-18963R

Lavendustin A (Standard) RG-14355 (Standard)	Structural Classification Microorganisms Ketones, Aldehydes, Acids Phenols Polyphenols Source Classification	Reference Standards EGFR
Lavendustin A (Standard) is the analytical standard of Lavendustin A. This product is intended for research and analytical applications. Lavendustin A (RG-14355) is a potent, selective and ATP-competitive inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase, with an IC50 of 11 nM. Lavendustin A does not inhibit protein kinase A or C. Lavendustin A can suppress VEGF-induced angiogenesis[1][2].

Art. -Nr.	Produktname	Chemical Structure

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 .

HY-50898S4

Lapatinib-d7
Lapatinib-d₇ (GW572016-d₇) is deuterium labeled Lapatinib. Lapatinib (GW572016) is a potent, orally active 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 .

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 . 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-15772S3

Asandeutertinib
Asandeutertinib (Osimertinib-d3; AZD-9291-d3) is a epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, with antineoplastic effect .

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 .

HY-50898S1

Lapatinib-d7 dihydrochloride
Lapatinib-d₇ dihydrochloride is the deuterium labeled Lapatinib dihydrochloride. Lapatinib (GW572016) dihydrochloride is a potent, orally active 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 .

HY-50898S

Lapatinib-d4
Lapatinib-d₄ is the deuterium labeled Lapatinib (HY-50898). Lapatinib is a potent, orally active 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 .

HY-50895S

Gefitinib-d8
Gefitinib-d₈ (ZD1839-d₈) is a deuterium labeled Gefitinib. Gefitinib is an EGFR tyrosine kinase inhibitor, with IC₅₀ of 2-37 nM in NR6wtEGFR cells .

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 .

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-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 .

HY-50898S2

Lapatinib-d5
Lapatinib-d₅ is deuterium labeled Lapatinib. Lapatinib (GW572016) is a potent, orally active 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 .

HY-50898S3

Lapatinib-d4-1
Lapatinib-d₄-1 is deuterium labeled Lapatinib. Lapatinib (GW572016) is a potent, orally active 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 .

HY-50898CS

Lapatinib-d4 tosylate
Lapatinib-d₄ (GW572016-d₄) tosylate is deuterium labeled Lapatinib (tosylate). Lapatinib (GW572016) tosylate is a potent, orally active 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 .

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) .

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) .

HY-10260S2

Vandetanib-13C6
Vandetanib- ¹³C₆ is a ¹³C labeled Vandetanib (HY-10260) . 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) .

HY-W777297

Lapatinib-13C2,15N Ditosylate
Lapatinib- ¹³C₂, ¹⁵N Ditosylate is the ¹³C- and ¹⁵N-labeled Lapatinib ditosylate (HY-50898A). Lapatinib ditosylate (GW572016 ditosylate) 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 .

HY-50896S3

Erlotinib-d8

Erlotinib-d₈ (CP-358774-d₈) is deuterium labeled Erlotinib. 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-50896S2

Erlotinib-d4

Erlotinib-d₄ (CP-358774-d₄) is deuterium labeled Erlotinib. 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-50898S5

Lapatinib-13C,d7
Lapatinib- ¹³C,d₇ (GW572016- ¹³C,d₇) is the deuterium and ¹³C-labeled Lapatinib (HY-50898). Lapatinib (GW572016) is a potent, orally active 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 .

HY-112823S

Almonertinib-d6

Almonertinib-d₆ (HS-10296-d₆) is the deuterium labeled Almonertinib (HY-112823). Almonertinib (HS-10296) is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib 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 is used for the research of the non-small cell lung cancer .

Art. -Nr.	Produktname		Classification

HY-50896

Erlotinib 130+ Cited Publications 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-139300

Epitinib HMPL-813		Alkynes
Epitinib (HMPL-813) is a selective, orally active, blood-brain barrier-permeable *EGFR* tyrosine kinase inhibitor. Epitinib is applicable to research on EGFR ^T790M-positive non-small cell lung cancer with brain metastasis and advanced solid tumors .

HY-131088

N3-PEG8-Phe-Lys-PABC-Gefitinib		ADC Synthesis 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 (HY-50895) (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. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN 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 . 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-129510

4-Methyl erlotinib		Alkynes
4-Methyl erlotinib, is a potent and selective epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor. 4-Methyl erlotinib potently inhibits EGF-mediated tumor cell mitosis by reducing EGFr-specific tyrosine phosphorylation. Using a mouse model of human tumor transplantation, 4-Methyl erlotinib demonstrated significant and sustained suppression of EGFr phosphotyrosine levels, resulting in significant growth inhibition of EGFr-dependent human cancers .

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-131088A

N3-PEG8-Phe-Lys-PABC-Gefitinib TFA		Azide
N3-PEG8-Phe-Lys-PABC-Gefitinib TFA is a agent-linker conjugate for ADC with potent antitumor activity by using the anti-tumor agent, Gefitinib (HY-50895) (orally active EGFR tyrosine kinase inhibitor), linked via the cleavable linker N3-PEG8-Phe-Lys-PABC. N3-PEG8-Phe-Lys-PABC-Gefitinib TFA 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. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN 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 .

HY-15661A

OSI-413 free base CP 373413		Alkynes
OSI-413 (free base) (CP 373413) is a major metabolite of Erlotinib (HY-50896). Erlotinib (CP-358774) is a directly acting EGFR tyrosine kinase inhibitor, with an IC₅₀ of 2 nM for human EGFR .

Targets Recommended: EGFR Btk Syk Pyk2 TNK1 Tyrosine Hydroxylase DYRK BRK FAK FLT3 Anaplastic lymphoma kinase (ALK)

Art. -Nr.	Produktname	Target	Forschungsgebiete	Chemical Structure

HY-50895G

Gefitinib ZD1839	EGFR Autophagy Apoptosis	Cancer
Gefitinib (ZD1839) (GMP) is Gefitinib (HY-50895) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Gefitinib is a potent, selective and orally active *EGFR* tyrosine kinase inhibitor .

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