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Results for "

autophosphorylation kinase

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Anaplastic lymphoma kinase (ALK) (1) Apoptosis (23) Autophagy (15) Bcr-Abl (6) Btk (1) c-Kit (3) Caspase (3) CDK (1) Drug Metabolite (3) EGFR (18) Ephrin Receptor (1) FAK (4) FGFR (4) FLT3 (10) Fungal (1) Insulin Receptor (1) IRE1 (8) Isotope-Labeled Compounds (3) JAK (3) Ligands for Target Protein for PROTAC (3) LRRK2 (3) Mitophagy (6) Organoid (1) PDGFR (10) Prostaglandin Receptor (1) RET (2) RIP kinase (1) SARS-CoV (1) Src (6) STAT (1) TGF-β Receptor (2) VEGFR (8)
By Research Areas:	Cancer (59) Cardiovascular Disease (3) Infection (1) Inflammation/Immunology (2) Metabolic Disease (2) Neurological Disease (5)
Click Chemistry:	Alkynes (2)

Inhibitors & Agonists

Screening Libraries

Peptides

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-107594

Benzene hexabromide	JAK	Cancer
Benzene hexabromide, a bromohydrocarbon, is a potent inhibitor of JAK2 tyrosine kinase autophosphorylation.

HY-15841

CEP-37440	Anaplastic lymphoma kinase (ALK) FAK	Cancer
CEP-37440 is a potent, orally active dual FAK/ALK inhibitor with IC₅₀ values of 2.3 nM and 3.5 nM for FAK and ALK, respectively. CEP-37440 decreases the cell proliferation by blocking the autophosphorylation kinase activity of FAK1 (Tyr 397) .

HY-100434

PD-161570	FGFR PDGFR EGFR Src TGF-β Receptor	Cardiovascular Disease Cancer
PD-161570 is a potent and ATP-competitive human FGF-1 receptor inhibitor with an IC₅₀ of 39.9 nM and a K_i of 42 nM. PD-161570 also inhibits the PDGFR, EGFR and c-Src tyrosine kinases with IC₅₀ values of 310 nM, 240 nM, and 44 nM, respectively. PD-161570 inhibits PDGF-stimulated autophosphorylation and FGF-1 receptor phosphorylation with IC₅₀s of 450 nM and 622 nM, respectively . PD-161570 is also a bone morphogenetic proteins (BMPs) and TGF-β signaling inhibitor .

HY-13012

RepSox 15+ Cited Publications E-616452; SJN 2511	Organoid TGF-β Receptor	Metabolic Disease
RepSox (E-616452) is a potent and selective *transforming growth factor-beta receptor I/activin like kinase* 5 (TGF-β-RI/ALK5)** inhibitor. RepSox inhibits ALK5 autophosphorylation with an IC₅₀ value of 4 nM. RepSox can be used for the research of obesity and associated metabolic diseases such as type 2 diabetes .

HY-101957

AG 1295 3 Publications Verification	PDGFR	Cardiovascular Disease
AG 1295 is a selective platelet-derived growth factor receptor (PDGFR) tyrosine-kinase inhibitor. AG1295 abolishes autophosphorylation of the PDGFR whereas not affects the autophosphorylation of the EGF receptor .

HY-101429

RG13022 Tyrphostin RG13022	EGFR	Cancer
RG13022 is a tyrosine kinase inhibitor; inhibits the autophosphorylation reaction of the EGF receptor with an IC₅₀ of 4 μM.

HY-10255A

Sunitinib 55+ Cited Publications SU 11248	VEGFR PDGFR IRE1 Mitophagy Autophagy Apoptosis	Cancer
Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC₅₀s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively . Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation .

HY-101962

HNMPA	Insulin Receptor	Metabolic Disease
HNMPA is a membrane impermeable insulin receptor tyrosine kinase inhibitor. HNMPA inhibits serine and tyrosine autophosphorylation by the human insulin receptor. HNMPA has no effect on protein kinase C or cyclic AMP-dependent protein kinase activities

HY-P2548

pp60 (v-SRC) Autophosphorylation Site, Phosphorylated	EGFR	Others
pp60 (v-SRC) Autophosphorylation Site, Phosphorylated is the phosphorylated peptide of an EGFR substrate. pp60 (v-SRC) Autophosphorylation Site, Phosphorylated can be used for the screening of EGFR Kinase inhibitors via phosphorylated-substrate quantification .

HY-P10609

Btk substrate peptide	Btk	Others
Btk substrate peptide is a peptide substrate corresponding to residues 217-229 of human Bruton’s tyrosine kinase (Btk), of which the tyrosine at residue 223 is the major autophosphorylation site of Btk. Btk substrate peptide is used as a substrate in in vitro kinase assays to evaluate the activity of Btk or other tyrosine kinases .

HY-15002

AST 487 4 Publications Verification NVP-AST 487	RET FLT3 VEGFR c-Kit Bcr-Abl	Cancer
AST 487 is a RET kinase inhibitor with IC₅₀ of 880 nM, inhibits RET autophosphorylation and activation of downstream effectors, also inhibits Flt-3 with IC₅₀ of 520 nM.

HY-12444

Y15 15+ Cited Publications FAK Inhibitor 14	FAK	Cancer
Y15 is a potent and specific inhibitor of focal adhesion kinase (FAK) that inhibits its autophosphorylation activity, decreases the viability of cancer cells, and blocks tumor growth.

HY-10255

Sunitinib Malate 55+ Cited Publications SU 11248 Malate	PDGFR VEGFR IRE1 Mitophagy Autophagy Apoptosis	Cancer
Sunitinib Malate (SU 11248 Malate) is a multi-targeted receptor tyrosine kinase inhibitor with IC₅₀s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively . Sunitinib Malate, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation .

HY-10255AS

Sunitinib-d10 SU 11248-d₁₀	VEGFR PDGFR IRE1 Mitophagy Autophagy Apoptosis	Cancer
Sunitinib-d₁₀ is a deuterium labeled Sunitinib. Sunitinib is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively[1]. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation[2].

HY-10255AS1

Sunitinib-d4	Isotope-Labeled Compounds VEGFR PDGFR IRE1 Mitophagy Autophagy Apoptosis	Cancer
Sunitinib-d₄ is the deuterium labeled Sunitinib. Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively[1]. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation[2].

HY-18509

IRE1α kinase-IN-2	IRE1	Cancer
IRE1α kinase-IN-2 is a potent IRE1α kinase inhibitor, with an EC₅₀ of 0.82 μM. IRE1α kinase-IN-2 inhibits IRE1α kinase autophosphorylation (IC₅₀=3.12 μM). IRE1α kinase-IN-2 inhibits XBP1 mRNA splicing in the WT cell lines .

HY-13258A

NVP-BHG712 4 Publications Verification BHG712	Ephrin Receptor	Cancer
NVP-BHG712 is an oral active EphB4 kinase autophosphorylation inhibitor, with IC₅₀ values of 3.3 nM and 3.0 nM for EphA2 and EphB4, respectively .

HY-149413

FHND5071	RET	Others Cancer
FHND5071 is a potent and selective RET kinase inhibitor, FHND5071 can exert antitumor effects by inhibiting RET autophosphorylation. FHND5071 can be used for tumor diseases research .

HY-10255AR

Sunitinib (Standard)	VEGFR PDGFR IRE1 Mitophagy Autophagy Apoptosis	Cancer
Sunitinib (Standard) is the analytical standard of Sunitinib. This product is intended for research and analytical applications. Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC₅₀s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively . Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation .

HY-10255R

Sunitinib Malate (Standard)	PDGFR VEGFR IRE1 Mitophagy Autophagy Apoptosis	Cancer
Sunitinib (Malate) (Standard) is the analytical standard of Sunitinib (Malate). This product is intended for research and analytical applications. Sunitinib Malate (SU 11248 Malate) is a multi-targeted receptor tyrosine kinase inhibitor with IC₅₀s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively . Sunitinib Malate, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation .

HY-15463S1

Imatinib-d4 STI571 d₄; CGP-57148B d₄	Bcr-Abl PDGFR c-Kit SARS-CoV Autophagy	Cancer
Imatinib-d₄ is a deuterium labeled Imatinib (STI571). Imatinib is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity[1][2].

HY-18899

Nec-3a	RIP kinase	Cancer
Nec-3a is a Necrostatin-3 analogue. Nec-3a is a RIP1 inhibitor (IC₅₀: 0.44 μM). Nec-3a inhibits the autophosphorylation activity of the RIP1 kinase domain .

HY-14674

CP-724714 4 Publications Verification	EGFR Apoptosis	Cancer
CP-724714 is a potent, selective and orally active ErbB2 (HER2) tyrosine kinase inhibitor, with an IC₅₀ of 10 nM. CP-724714 displays a marked selectivity against EGFR kinase (IC₅₀=6400 nM). CP-724714 potently inhibits ErbB2 receptor autophosphorylation in intact cells. Antitumor activities .

HY-108263

3-Hydroxy Midostaurin CGP52421	FLT3	Cancer
3-Hydroxy Midostaurin (CGP 52421), a metabolite of PKC412, effectively inhibits *FMS-like tyrosine kinase-3 (FLT3)* autophosphorylation with IC₅₀s of approximately 132 nM and 9.8 μM in culture medium and plasma, respectively. 3-Hydroxy Midostaurin is less selective but more cytotoxic than PKC412 .

HY-108263S

3-Hydroxy Midostaurin-d5 CGP52421-d₅	Isotope-Labeled Compounds FLT3	Cancer
3-Hydroxy Midostaurin-d₅ is a deuterium labeled 3-Hydroxy Midostaurin. 3-Hydroxy Midostaurin is a metabolite of PKC412, which effectively inhibits FMS-like tyrosine kinase-3 (FLT3) autophosphorylation with IC50s of approximately 132 nM and 9.8 μM in culture medium and plasma, respectively[1].

HY-144448

FAK-IN-2	FAK Apoptosis	Cancer
FAK-IN-2 is a potent and orally active focal adhesion kinase (FAK) inhibitor, with anticancer activity (FAK IC₅₀= 35 nM). FAK-IN-2 covalently inhibits the autophosphorylation of FAK in a dose-dependent manner, and inhibits the clone formation and migration of tumor cells, inducing apoptosis .

HY-15480

NSC 42834 1 Publications Verification JAK2 Inhibitor V; Z3	JAK	Cancer
NSC 42834 (JAK2 Inhibitor V), a novel specific inhibitor of Jak2, inhibits Jak2-V617F and Jak2-WT autophosphorylation in a dose-dependent manner but was not cytotoxic to cells at concentrations that inhibited kinase activity.

HY-101450

PF-6274484	EGFR	Cancer
PF-6274484 is a potent EGFR inhibitor with K_is of 0.14 nM and 0.18 nM for EGFR-L858R/T790M and WT EGFR, respectively. PF-6274484 inhibits EGFR-L858R/T790M autophosphorylation in H1975 tumor cells and EGFR WT in A549 tumor cells with IC₅₀s of 6.6 and 5.8 nM, respectively .

HY-103274

PD180970	Bcr-Abl Src c-Kit Apoptosis	Neurological Disease Cancer
PD180970 is a highly potent and ATP-competitive p210 ^Bcr-Abl kinase inhibitor, with an IC₅₀ of 5 nM for inhibiting the autophosphorylation of p210 ^Bcr-Abl. PD180970 also inhibits Src and KIT kinase with IC₅₀s of 0.8 nM and 50 nM, respectively. PD180970 indcues apoptosis of K562 leukemic cells, and can be used for chronic myelogenous leukemia research .

HY-136735

IRE1α kinase-IN-1	IRE1	Neurological Disease Cancer
IRE1α kinase-IN-1 is a highly selective IRE1α (ERN1) inhibitor, with an IC₅₀ of 77 nM. IRE1α kinase-IN-1 displays 100-fold selectivity for IRE1α over the IRE1β isoform. IRE1α kinase-IN-1 inhibits ER stress-induced IRE1α oligomerization and autophosphorylation, and also inhibits IRE1α RNase activity (IC₅₀=80 nM) .

HY-12282

GNE-9605	LRRK2	Neurological Disease
GNE-9605 is a potent, orally active, selective *Leucine-rich repeat kinase* 2 (LRRK2) inhibitor with an IC₅₀** value of 18.7 nM. GNE-9605 inhibits LRRK2 Ser1292 autophosphorylation. GNE-9605 can be used in research of Parkinson's disease (PD) .

HY-50895A

Gefitinib hydrochloride Maximum Cited Publications 129 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-131257

Gefitinib impurity 1	Drug Metabolite	Others Cancer
Gefitinib impurity 1 is the impurity of 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-133779

Gefitinib impurity 5	Drug Metabolite	Others Cancer
Gefitinib impurity 5 is the impurity of 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-118304

AKN-028	FLT3 Apoptosis Caspase	Cancer
AKN-028, a novel *tyrosine kinase* (TK) inhibitor, is a potent, orally active FMS-like receptor tyrosine kinase 3 (FLT3) inhibitor with an IC₅₀** value of 6 nM. AKN-028 inhibits FLT3 autophosphorylation. AKN-028 induces dose-dependent cytotoxic response (mean IC₅₀=1 μM). AKN-028 induces apoptosisby activation of caspase 3. AKN-028 can be used in research of acute myeloid leukemia (AML) .

HY-118304B

AKN-028 acetate	FLT3 Apoptosis Caspase	Cancer
AKN-028 acetate, a novel tyrosine kinase (TK) inhibitor, is a potent, orally active FMS-like receptor tyrosine kinase 3 (FLT3) inhibitor with an IC50 value of 6 nM. AKN-028 acetate inhibits FLT3 autophosphorylation. AKN-028 acetate induces dose-dependent cytotoxic response (mean IC50=1 μM). AKN-028 acetate induces apoptosisby activation of caspase 3. AKN-028 acetate can be used in research of acute myeloid leukemia (AML).

HY-136895

AZ12672857	Prostaglandin Receptor	Cancer
AZ12672857 is an orally active inhibitor of EphB4 (IC₅₀=1.3 nM) and Src kinases. AZ12672857 shows good inhibition of proliferation of c-Src transfected 3T3 cells (IC₅₀=2 nM) as well as autophosphorylation of EphB4 in transfected CHO-K1 cells (IC₅₀=9 nM) .

HY-50895

Gefitinib Maximum Cited Publications 129 Publications Verification ZD1839	EGFR Autophagy Apoptosis	Cancer
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 and cell apoptosis, which can be used for cancer related research, such as Lung cancer and breast cancer .

HY-W062835

CGP77675	Src	Cancer
CGP77675 is an orally active and potent inhibitor of Src family kinases. CGP77675 inhibits phosphorylation of peptide substrates and autophosphorylation of purified Src (IC₅₀s of 5-20 and 40 nM, respectively), and also inhibits Src, EGFR, KDR, v-Abl, and Lck with IC₅₀s of 5-20, 40, 20, 150, 1000, 310, and 290 nM, respectively. Anticancer activity .

HY-100663

Gefitinib impurity 2	EGFR	Others Cancer
Gefitinib impurity 2 is the impurity of Gefitinib. Gefitinib (ZD1839; HY-50895) 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-50895S1

Gefitinib-d6 ZD1839-d₆	EGFR Autophagy	Cancer
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-145652

Narmafotinib AMP-945	FAK	Cancer
Narmafotinib (AMP-945) is an inhibitor of the enzyme focal adhesion kinase (FAK, K_D=0.21 nM). Narmafotinib inhibits autophosphorylation of 397Y-FAK in MDA-MB-231 cells with an IC₅₀=7 nM and exhibits low general cellular toxicity (IC₅₀=2.7 μM, MDA-MB-231 cells) .

HY-50895B

Gefitinib dihydrochloride ZD 1839 dihydrochloride	EGFR Autophagy Apoptosis	Cancer
Gefitinib (ZD 1839) dihydrochloride is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC₅₀ of 33 nM. Gefitinib dihydrochloride selectively inhibits EGF-stimulated tumor cell growth (IC₅₀ of 54 nM) and blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib dihydrochloride also induces autophagy and cell apoptosis, which can be used for cancer related research, such as Lung cancer and breast cancer .

HY-50896S

Erlotinib-d6 CP-358774-d₆; NSC 718781-d₆; OSI-774-d₆	EGFR	Cancer
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-50896

Erlotinib 85+ 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-W062835A

CGP77675 hydrate	Src	Cancer
CGP77675 hydrate is an orally active and potent inhibitor of Src family kinases. CGP77675 hydrate inhibits phosphorylation of peptide substrates and autophosphorylation of purified Src (IC₅₀s of 5-20 and 40 nM, respectively),and also inhibits Src, EGFR, KDR, v-Abl, and Lck with IC₅₀s of 0.02, 0.15, 1.0, 0.31, and 0.29 μM, respectively. Anticancer activity .

HY-112345

PD-089828	FGFR PDGFR EGFR Src	Cancer
PD-089828 is an ATP competitive inhibitor of FGFR-1, PDGFR-β and EGFR (IC₅₀s=0.15, 1.76, and 5.47 µM, respectively) and a noncompetitive inhibitor of c-Src tyrosine kinase (IC₅₀=0.18 µM). PD-089828 also inhibits MAPK with an IC₅₀ of 7.1 µM. PD-089828 inhibits PDGF-, EGF- and bFGF-mediated tyrosine kinase receptor autophosphorylation in vitro. PD-089828 has a long-lasting cellular activity .

HY-118304A

AKN-028 TFA	FLT3 Apoptosis Caspase	Cancer
AKN-028 TFA, a novel *tyrosine kinase* (TK) inhibitor, is a potent, orally active FMS-like receptor tyrosine kinase 3 (FLT3) inhibitor with an IC₅₀** value of 6?nM. AKN-028 TFA inhibits FLT3 autophosphorylation. AKN-028 TFA induces dose-dependent cytotoxic response (mean IC₅₀=1?μM). AKN-028 TFA induces apoptosisby activation of caspase 3. AKN-028 TFA can be used in research of acute myeloid leukemia (AML) .

HY-50895S2

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

HY-156618

Irpagratinib ABSK011	FGFR	Cancer
Irpagratinib (ABSK011) is an orally active inhibitor of fibroblast growth factor receptor (FGFR) tyrosine kinase, targeting to FGFR4 (IC50<10 nM). Irpagratinib inhibits the auto-phosphorylation of FGFR4 and blocks signal transduction from FGFR4 to downstream pathway activation. Irpagratinib exhibits high exposure in PK study in mouse, rat and dog, and also shows antineoplastic/anti-tumor activity in subcutaneous xenograft tumor models .

Cat. No.	Product Name

HY-L016

Protein Tyrosine Kinase Compound Library

1,140 compounds

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

MCE designs a unique collection of 1,140 compounds that act as a useful tool for PTKs-related drug screening and disease research.

Cat. No.	Product Name	Target	Research Area

HY-P2548

pp60 (v-SRC) Autophosphorylation Site, Phosphorylated	EGFR	Others
pp60 (v-SRC) Autophosphorylation Site, Phosphorylated is the phosphorylated peptide of an EGFR substrate. pp60 (v-SRC) Autophosphorylation Site, Phosphorylated can be used for the screening of EGFR Kinase inhibitors via phosphorylated-substrate quantification .

HY-P10609

Btk substrate peptide	Btk	Others
Btk substrate peptide is a peptide substrate corresponding to residues 217-229 of human Bruton’s tyrosine kinase (Btk), of which the tyrosine at residue 223 is the major autophosphorylation site of Btk. Btk substrate peptide is used as a substrate in in vitro kinase assays to evaluate the activity of Btk or other tyrosine kinases .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-131257

Gefitinib impurity 1	Classification of Application Fields Disease Research Fields Cancer	Drug Metabolite
Gefitinib impurity 1 is the impurity of 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-133779

Gefitinib impurity 5	Classification of Application Fields Disease Research Fields Cancer	Drug Metabolite
Gefitinib impurity 5 is the impurity of 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-100663

Gefitinib impurity 2	Classification of Application Fields Disease Research Fields Cancer	EGFR
Gefitinib impurity 2 is the impurity of Gefitinib. Gefitinib (ZD1839; HY-50895) 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-108485

Damnacanthal	Structural Classification Classification of Application Fields Source classification Plants Infection Quinones Monophenols Anthraquinones Morinda citrifolia Linn. Rubiaceae Phenols Inflammation/Immunology Disease Research Fields	Src Apoptosis Fungal
Damnacanthal is an anthraquinone isolated from the root of Morinda citrifolia. Damnacanthal is a highly potent, selective inhibitor of p56 ^lck tyrosine kinase activity. Natural Damnacanthal inhibits p56 ^lck autophosphorylation and phosphorylation of exogenous substrates with IC₅₀s of 46 nM and 220 nM, respectively. Damnacanthal is a potent inducer of apoptosis with anticancer activity. Damnacanthal also has antinociceptive, anti-inflammatory effects in mice and anti-fungal activity against *Candida albicans* .

HY-149413

FHND5071	Classification of Application Fields Disease Research Fields Cancer	RET
FHND5071 is a potent and selective RET kinase inhibitor, FHND5071 can exert antitumor effects by inhibiting RET autophosphorylation. FHND5071 can be used for tumor diseases research .

Cat. No.	Product Name	Chemical Structure

HY-10255AS

Sunitinib-d10
Sunitinib-d₁₀ is a deuterium labeled Sunitinib. Sunitinib is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively[1]. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation[2].

HY-15463S1

Imatinib-d4
Imatinib-d₄ is a deuterium labeled Imatinib (STI571). Imatinib is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity[1][2].

HY-50895S1

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

HY-10255AS1

Sunitinib-d4
Sunitinib-d₄ is the deuterium labeled Sunitinib. Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively[1]. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation[2].

HY-149413

FHND5071
FHND5071 is a potent and selective RET kinase inhibitor, FHND5071 can exert antitumor effects by inhibiting RET autophosphorylation. FHND5071 can be used for tumor diseases research .

HY-108263S

3-Hydroxy Midostaurin-d5
3-Hydroxy Midostaurin-d₅ is a deuterium labeled 3-Hydroxy Midostaurin. 3-Hydroxy Midostaurin is a metabolite of PKC412, which effectively inhibits FMS-like tyrosine kinase-3 (FLT3) autophosphorylation with IC50s of approximately 132 nM and 9.8 μM in culture medium and plasma, 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-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 85+ 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-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.

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autophosphorylation kinase

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