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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 (90) Apoptosis (20) Autophagy (26) Bcr-Abl (1) BMX Kinase (1) c-Met/HGFR (2) CaMK (2) Casein Kinase (1) CDK (1) COX (1) DNA-PK (1) Drug Metabolite (2) Drug-Linker Conjugates for ADC (3) Endogenous Metabolite (3) Enterovirus (1) Ephrin Receptor (1) Epigenetic Reader Domain (1) Ferroptosis (8) FGFR (4) GPR35 (1) HCV (2) Histone Acetyltransferase (1) IGF-1R (1) Influenza Virus (2) IRAK (2) Isotope-Labeled Compounds (7) JAK (2) mTOR (1) PDGFR (3) Phosphatase (1) Phosphodiesterase (PDE) (1) PI3K (1) PKA (1) PKC (1) Ras (1) ROR (1) Src (5) STAT (2) Topoisomerase (1) Trk Receptor (2) Tyrosinase (1) VEGFR (12)
By Research Areas:	Cancer (106) Cardiovascular Disease (2) Infection (3) Inflammation/Immunology (2) Metabolic Disease (3) Neurological Disease (1)
Click Chemistry:	Azide (1) Alkynes (5)

117

Inhibitors & Agonists

Fluorescent Dye

Biochemical Assay Reagents

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

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

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-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-108484

PP 3

EGFR Cancer

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

PP 3	EGFR	Cancer
PP 3 (Compound 3) is an **EGFR tyrosine kinase** inhibitor with an IC₅₀ of 2.7 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-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[1].

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-117155

PKI-166

EGFR Cancer

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

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

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

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-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-12000

AG490 95+ 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 .

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-50898

Lapatinib 60+ 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-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-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 .

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-50898A

Lapatinib ditosylate 60+ 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-50898B

Lapatinib ditosylate monohydrate 60+ 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-137433

Befotertinib D-0316	EGFR	Cancer
Befotertinib (D-0316) is the third-generation **EGFR tyrosine kinase** inhibitor. Befotertinib can be used for the research of EGFR T790M-positive non-small cell lung cancer (NSCLC) .

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-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-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-100636

Gefitinib N-oxide

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-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 .

Gefitinib N-oxide
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 .

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-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 5+ 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-137433A

Befotertinib mesylate D-0316 mesylate	EGFR	Cancer
Befotertinib (D-0316) mesylate is the third-generation **EGFR tyrosine kinase** inhibitor. Befotertinib (D-0316) mesylate can be used for the research of EGFR T790M-positive non-small cell lung cancer (NSCLC) .

HY-50895S

Gefitinib-d8

ZD1839-d8

Gefitinib-d₈ is a deuterium labeled Gefitinib. Gefitinib is an EGFR tyrosine kinase inhibitor, with IC50 of 2-37 nM in NR6wtEGFR cells[1][2].

Gefitinib-d8 ZD1839-d8
Gefitinib-d₈ is a deuterium labeled Gefitinib. Gefitinib is an EGFR tyrosine kinase inhibitor, with IC50 of 2-37 nM in NR6wtEGFR cells[1][2].

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-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) .

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-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-130616

EGFR-IN-11	EGFR Apoptosis	Cancer
EGFR-IN-11 is a fourth-generation *EGFR*-tyrosine kinase inhibitor (EGFR-TKI) with an IC₅₀ of 18 nM for triple mutant EGFR ^{L858R/T790M/C797S}. EGFR-IN-11 significantly suppresses the EGFR phosphorylation, induce the apoptosis, and arrest cell cycle at G0/G1 .

HY-18963

Lavendustin A RG-14355
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 35+ Cited Publications 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-50898S1

Lapatinib-d7 dihydrochloride GW572016-dd₇ dihydrochloride; GW2016-dd₇ dihydrochloride	Isotope-Labeled Compounds EGFR Autophagy Ferroptosis	Cancer
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 GW572016-d₅; GW2016-d₅	Isotope-Labeled Compounds EGFR Autophagy Ferroptosis	Cancer
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-20878

Tyrphostin AG 879 1 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-50898S3

Lapatinib-d4-1 GW572016-d₄-1; GW2016-d₄-1	Isotope-Labeled Compounds EGFR Autophagy Ferroptosis	Cancer
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-13524

AG-1478 30+ 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-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. Tyrphostin 25 is also a GPR35 agonist with an IC₅₀ of 0.94 µM and an EC₅₀** of 5.3 µM .

HY-112299

Zipalertinib 1 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-50898S

Lapatinib-d4 GW572016-d₄; GW2016-d₄	EGFR Autophagy Ferroptosis	Cancer
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-128893

MC-Sq-Cit-PAB-Gefitinib	Drug-Linker Conjugates for ADC	Cancer
MC-Sq-Cit-PAB-Gefitinib is a agent-linker conjugate for ADC with potent antitumor activity by using Gefitinib (an EGFR tyrosine kinase inhibitor), linked via the ADC linker MC-Sq-Cit-PAB.

HY-163377

AZ5385	Enterovirus EGFR	Infection
AZ5385 is an **EGFR-tyrosine kinase** inhibitor. AZ5385 is a HRV-2 virus blocker, with EC₅₀ of 0.35 µM. AZ5385 affects the late stage of viral life cycle .

HY-10260

Vandetanib 15+ Cited Publications ZD6474	VEGFR Autophagy Apoptosis	Cancer
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-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-10260A

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

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-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-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-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 .

Cat. No.	Product Name	Chemical Structure

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-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-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-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-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-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-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].

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-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].

Cat. No.	Product Name		Classification

HY-50896

Erlotinib 70+ 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[1].

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-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. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.

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