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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 (131) Apoptosis (26) Autophagy (39) Bcr-Abl (1) BMX Kinase (1) c-Met/HGFR (2) CaMK (2) Casein Kinase (1) CDK (1) COX (1) DNA-PK (1) Drug Intermediate (1) Drug Metabolite (4) Drug-Linker Conjugates for ADC (3) Endogenous Metabolite (3) Enterovirus (1) Epigenetic Reader Domain (1) ERK (2) Ferroptosis (14) FGFR (5) GLUT (1) GPR35 (2) HCV (3) Histone Acetyltransferase (1) IGF-1R (1) Influenza Virus (3) IRAK (2) Isotope-Labeled Compounds (13) JAK (2) Mitosis (2) MMP (1) mTOR (1) p38 MAPK (1) PDGFR (4) Phosphatase (1) Phosphodiesterase (PDE) (2) PI3K (1) PKA (2) PKC (2) Ras (1) Reference Standards (13) RET (1) Ser/Thr Kinase (1) Src (6) STAT (2) TAM Receptor (1) TGF-β Receptor (1) Topoisomerase (1) Trk Receptor (2) Tyrosinase (2) VEGFR (13)
By Research Areas:	Cancer (150) Cardiovascular Disease (4) Infection (11) Inflammation/Immunology (4) Metabolic Disease (4) Neurological Disease (1)
Click Chemistry:	Azide (1) Alkynes (7)

161

Inhibitors & Agonists

Fluorescent Dye

Biochemical Assay Reagents

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

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

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-112823A

Almonertinib mesylate 5 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-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-164718

Sevabertinib	EGFR	Cancer
Sevabertinib is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor with antitumor activity .

HY-N14635

Paeciloquinone A	EGFR	Infection
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	EGFR	Infection
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	EGFR	Infection
Paeciloquinone D can inhibit the *EGFR* protein tyrosine kinase .

HY-N14639

Paeciloquinone E	EGFR	Infection
Paeciloquinone E can inhibit the *EGFR* protein tyrosine kinase .

HY-N14640

Paeciloquinone F	EGFR	Infection
Paeciloquinone F can inhibit the *EGFR* protein tyrosine kinase .

HY-N14636

Paeciloquinone B	EGFR	Infection
Paeciloquinone B can inhibit the *EGFR* protein tyrosine kinase .

HY-169755

Tyrphostin 63	EGFR	Cancer
Tyrphostin 63 (compound 13) is an epidermal growth factor receptor (EGFR) inhibitor with IC₅₀ and K_i values are 375 and 123 μM, respectively .

HY-108484

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

HY-50896S1

Erlotinib-13C6 CP-358774-¹³C₆; NSC 718781-¹³C₆; OSI-774-¹³C₆	Isotope-Labeled Compounds EGFR Autophagy	Cancer
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-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-120857

BPIQ-II hydrochloride PD 158294	EGFR	Others
BPIQ-II is a linear imidazoloquinazoline that potently inhibits the tyrosine kinase activity of the epidermal growth factor receptor (EGFR; IC₅₀=8 pM). It is selective for EGFR over an assortment of other tyrosine and serine/threonine kinases. Cellular studies indicate that BPIQ-II can enter cells and very selectively shut down EGF-stimulated signal transmission by binding competitively at the ATP site of EGFR.

HY-110328

PKI-166 hydrochloride	EGFR	Cancer
PKI-166 hydrochloride is a potent, selective and orally active **EGFR tyrosine kinase** inhibitor, with an IC₅₀ of 0.7 nM .

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-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-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-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-12000

AG490 135+ 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-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-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-144444

NSC381467	EGFR	Cancer
NSC381467 is a potent and orally active inhibitor of EGFR tyrosine kinase (EGFR-TK). NSC381467 has strong antiproliferative activities. NSC381467 has the potential for the research of cancer diseases .

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-118175

RG 14921	EGFR	Others
RG 14921 is a compound structurally related to Erbstatin (HY-113549) and has inhibitory activity against *EGFR* tyrosine kinase and CAMP-dependent kinase activity. RG 14921 inhibits EGF receptor kinase activity as a noncompetitive inhibitor.

HY-147303

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

HY-50898

Lapatinib 80+ Cited Publications GW572016; GW2016	EGFR Autophagy Ferroptosis	Cancer
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 .

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-112405

BPIQ-I PD 159121	EGFR	Cancer
BPIQ-I (PD 159121) is a potent and ATP-competitive **EGFR tyrosine kinase** inhibitor.. BPIQ-I shows anti-proliferative actively .

HY-19730

Olmutinib 5+ 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-50898B

Lapatinib ditosylate monohydrate 80+ Cited Publications GW572016 ditosylate monohydrate; GW2016 ditosylate monohydrate	EGFR Autophagy Ferroptosis	Cancer
Lapatinib ditosylate monohydrate (GW572016 ditosylate monohydrate) 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-50898C

Lapatinib tosylate GW572016 tosylate; GW2016 tosylate	EGFR Ferroptosis Autophagy	Cancer
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-50898A

Lapatinib ditosylate 80+ Cited Publications GW572016 ditosylate; GW2016 ditosylate	EGFR Autophagy Ferroptosis	Cancer
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-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-145844

EGFR-IN-44	EGFR Apoptosis	Cancer
EGFR-IN-44 (Compound 6a) is a potent, orally active *EGFR* tyrosine kinase inhibitor with an IC₅₀ of 4.11 nM. EGFR-IN-44 induces cell apoptosis and shows an oral bioavailability value of 33.57%. EGFR-IN-44 can be studied for non-small-cell lung cancers .

HY-15661A

OSI-413 free base CP 373413	Drug Metabolite	Cancer
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 .

HY-161866

EGFR-IN-118	EGFR	Cancer
EGFR-IN-118 (Compound 4a) is an inhibitor for the tyrosine kinase *EGFR. EGFR-IN-118 demonstrates anti-cancer property, inhibiting* the proliferation of MCF-7 and PC3 with IC₅₀ of 2.53 and 3.25 µg/ml. EGFR-IN-118 exhibits antioxidant efficacy, inhibiting the DPPH free radicals with IC₅₀ of 10.04 µg/ml .

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-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-50895S

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

HY-100636A

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

HY-101084

NSC 228155 10+ 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-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 .

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-164413

CLM3	VEGFR EGFR RET Apoptosis	Cancer
CLM3, a pyrazolopyrimidine derivative, is a multiple *tyrosine* kinase inhibitor. CLM3 shows antiproliferative and proapoptotic activity on endothelial and cancer cells, synergistically enhanced by SN38 (HY-13704). These effects are mainly due to its inhibition of phosphorylation of VEGFR-2, *EGFR* and RET tyrosine kinases and their related signaling pathways .

HY-142680

EGFR-IN-23	EGFR	Cancer
EGFR-IN-23 is a potent *EGFR* TKI (tyrosine kinase inhibitor) with an IC₅₀ of 8.05 nM for BaF3/EGFR-DEL19/T790M/C797S cell (WO2021244502A1, compound 8) .

HY-137433A

Befotertinib mesylate D-0316 mesylate	EGFR	Cancer
Befotertinib (D-0316) mesylate is an orally active **EGFR tyrosine kinase** inhibitor. Befotertinib mesylate can inhibit the proliferation of tumor cells. Befotertinib mesylate can be used in the research of EGFR T790M-positive non-small cell lung cancer (NSCLC) .

HY-137433

Befotertinib 1 Publications Verification D-0316	EGFR	Cancer
Befotertinib (D-0316) is an orally active **EGFR tyrosine kinase** inhibitor. Befotertinib can inhibit the proliferation of tumor cells. Befotertinib can be used in the research of EGFR T790M-positive non-small cell lung cancer (NSCLC) .

HY-18963

Lavendustin A 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 .

Cat. No.	Product Name	Type

HY-50895G

Gefitinib (GMP) ZD1839 (GMP)	Fluorescent Dye
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 .

Cat. No.	Product Name	Type

HY-50895G

Gefitinib (GMP) ZD1839 (GMP)	Biochemical Assay Reagents
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 .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-18963

Lavendustin A RG-14355	Structural Classification Microorganisms Classification of Application Fields Ketones, Aldehydes, Acids Source classification Phenols Polyphenols Disease Research Fields 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-14596

Genistein Maximum Cited Publications 65 Publications Verification NPI 031L	Structural Classification Classification of Application Fields Anti-aging Source classification 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 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-14596R

Genistein (Standard) Maximum Cited Publications 65 Publications Verification NPI 031L (Standard)	Structural Classification Classification of Application Fields Anti-aging Source classification Plants Endogenous metabolite Human Gut Microbiota Metabolites Flavonoids Leguminosae Glycine max (L.) merr Sunscreen Phenols Cosmetic Research Glycyrrhiza uralensis Fisch. Disease Research Fields 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-N14635

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

HY-N14639

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

HY-N14640

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

HY-N14636

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

HY-18963R

Lavendustin A (Standard) RG-14355 (Standard)	Structural Classification Microorganisms Ketones, Aldehydes, Acids Source classification Phenols Polyphenols	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].

HY-N12726

Halociline	Structural Classification Microorganisms Marine natural products Source classification Phenols Marine microorganism	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-16558

Butein 4 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-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 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-16558R

Butein (Standard) 2’,3,4,4’-tetrahydroxy Chalcone (Standard)	Structural Classification Chalcones Flavonoids other families Source classification Phenols Polyphenols Plants	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).

Cat. No.	Product Name	Chemical Structure

HY-50895S

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

HY-15772S3

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

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 .

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-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 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-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 .

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 .

HY-50898S4

Lapatinib-d7
Lapatinib-d₇ (GW572016-d₇) 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 .

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-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-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-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-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-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-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-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.

Cat. No.	Product Name		Classification

HY-50896

Erlotinib 105+ 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-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-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-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-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 .

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-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-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. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.

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