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EGFR phosphorylation

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46

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1

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3

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1

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4

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1

Isotope-Labeled Compounds

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-150611
    EGFR-IN-70

    		EGFR Cancer
    EGFR-IN-70 (compound 18j) is a potent EGFR inhibitor with IC50 values of 23.6 and 307.5 nM for EGFR LR/TM/CS and EGFR WT, respectively. EGFR-IN-70 has anti-proliferative activity and suppresses phosphorylation of the EGFR. EGFR-IN-70 can be used for cancer research .
    EGFR-IN-70
  • HY-12283
    Rostafuroxin
    1 Publications Verification

    PST 2238

    		 Na+/K+ ATPase RSV Cardiovascular Disease
    Rostafuroxin (PST 2238), a digitoxigenin derivative, is an orally active and potent Na +,K +-ATPase (ATP1A1) antognist. Rostafuroxin binds specifically to the ATP1A1 extracellular domain and blocks respiratory syncytial virus (RSV)-triggered EGFR Tyr845 phosphorylation. Rostafuroxin has antihypertensive and anti-RSV activity .
    Rostafuroxin
  • HY-112474
    Tyrphostin AG 112

    		EGFR Cancer
    Tyrphostin AG 112 is an EGFR phosphorylation inhibitor .
    Tyrphostin AG 112
  • HY-155358
    Os30

    		EGFR Apoptosis Cancer
    Os30, a potent fourth-generation EGFR inhibitor, is a potent EGFRC797S-TK inhibitor with IC50 values of 18 nM and 113 nM for EGFRDel19/T790M/C797S TK and EGFRL858R/T790M/C797S TK, respectively. Os30 can suppress EGFR phosphorylation, arrest at G1 phase and induce the apoptosis of KC-0116 (BaF3-EGFRDel19/T790M/C797S) cells. Os30 shows potent antitumor efficacy on non-small cell lung cancer (NSCLC) with EGFmRC797S mutation .
    Os30
  • HY-161408
    GePhos1

    		EGFR Apoptosis Cancer
    GePhos1, a EGFR-targeting PhosTAC (phosphorylation targeting chimera), induces EGFR dephosphorylation. GePhos1 induces apoptosis .
    GePhos1
  • HY-111452
    EGFR-IN-85

    		EGFR Cancer
    EGFR-IN-85 (Compound 1) is an EGFR inhibitor. EGFR-IN-85 has IC50 value of 0.19 μM for EGFRvⅢ phosphorylation. EGFR-IN-85 can suppress EGFR signaling within tumors. EGFR-IN-85 can be used for Glioblastoma (GBM) research .
    EGFR-IN-85
  • HY-161145
    EGFR/microtubule-IN-1

    		EGFR Apoptosis Microtubule/Tubulin Cancer
    EGFR/microtubule-IN-1 (Compound 10c) is a dual inhibitor targeting EGFR and tubulin. The IC50 for inhibiting EGFR is 10.66 nM. EGFR/microtubule-IN-1 can reduce the phosphorylation levels of EGFR, AKT and ERK, hinder tubulin polymerization, and induce apoptosis .
    EGFR/microtubule-IN-1
  • HY-12029
    WZ8040

    		EGFR Cancer
    WZ8040 is an irreversible mutated EGFR T790M inhibitor and inhibits EGFR phosphorylation. WZ8040 displays 100-fold greater activity against the mutated EGFR than the normal .
    WZ8040
  • 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 .
    EGFR-IN-11
  • HY-155227
    ALK/EGFR-IN-1

    		Anaplastic lymphoma kinase (ALK) EGFR Apoptosis Cancer
    ALK/EGFR-IN-1 (Compound 8l) is an ALK/EGFR dual inhibitor that blocks the phosphorylation of EGFR and ALK. ALK/EGFR-IN-1 inhibits ALK/EGFR mutants respectively, with IC50 of 4.3 nM for EGFR L858R T790M in H1975 cells and EML4-ALK in BaF3 cells, respectively. and 3.6 nM. ALK/EGFR-IN-1 may be used in NSCLC research .
    ALK/EGFR-IN-1
  • HY-103443
    HKI-357

    		EGFR Cancer
    HKI-357 is an irreversible dual inhibitor of EGFR and ERBB2 with IC50s of 34 nM and 33 nM, respectively. HKI-357 suppresses EGFR autophosphorylation (at Y1068), and AKT and MAPK phosphorylation .
    HKI-357
  • HY-149889
    EGFR-IN-78

    		Apoptosis EGFR Cancer
    EGFR-IN-78 (compound A5)，a 2-aminopyrimidine derivative，is a reversible inhibitor of EGFR C797S-TK，and also an inducer of apoptosis. EGFR-IN-78 shows anti-proliferative activity，inhibits EGFR phosphorylation and arrests cell cycle at G2/M phase .
    EGFR-IN-78
  • 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 .
    NSC 228155
  • 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 .
    Sacibertinib
  • HY-19816A
    Avitinib maleate
    2 Publications Verification

    Abivertinib maleate; AC0010 maleate

    		 EGFR Btk Apoptosis Cancer
    Avitinib (Abivertinib) maleate is a third-generation, irreversible and orally active selective EGFR inhibitor, with IC50 values of 0.18 nM, 0.18 nM, 7.68 nM and against EGFR L858R, EGFR T790M and wild-type EGFR. Avitinib maleate is also a BTK inhibitor that induces apoptosis and inhibits phosphorylation of BTK in mantle cell lymphoma. Avitinib maleate shows anticancer effects .
    Avitinib maleate
  • HY-19816
    Avitinib
    2 Publications Verification

    Abivertinib; AC0010

    		 EGFR Btk Apoptosis Cancer
    Avitinib (Abivertinib) is a third-generation, irreversible and orally active selective EGFR inhibitor, with IC50 values of 0.18 nM, 0.18 nM, 7.68 nM and against EGFR L858R, EGFR T790M and wild-type EGFR. Avitinib is also a BTK inhibitor that induces apoptosis and inhibits phosphorylation of BTK in mantle cell lymphoma. Avitinib shows anticancer effects .
    Avitinib
  • HY-163006
    EGFR/c-Met-IN-1

    		EGFR c-Met/HGFR Cancer
    EGFR/c-Met-IN-1 (compound TS-41) is a dual-target inhibitor of EGFR/c-Met. The IC50 for inhibiting EGFR L858R and c-Met is 68.1 nM and 0.26 nM respectively. . EGFR/c-Met-IN-1 induces apoptosis and cell cycle arrest in A549-P cells, downregulating the phosphorylation of EGFR, c-Met, and downstream AKT. EGFR/c-Met-IN-1 inhibits tumor growth in vitro and in vivo .
    EGFR/c-Met-IN-1
  • HY-13595
    Chrysophanol
    3 Publications Verification

    Chrysophanic acid

    		 EGFR Cancer
    Chrysophanol (Chrysophanic acid) is a natural anthraquinone, which inhibits EGF-induced phosphorylation of EGFR and suppresses activation of AKT and mTOR/p70S6K.
    Chrysophanol
  • 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 .
    pp60 (v-SRC) Autophosphorylation Site, Phosphorylated
  • HY-113599
    Isoprocurcumenol

    		EGFR ERK Akt Others
    Isoprocurcumenol is a guaiane type sesquiterpene, that can be isolated from Curcuma comosa. Isoprocurcumenol can activate EGFR signaling. Isoprocurcumenol increases the phosphorylation of ERK and AKT. Isoprocurcumenol promotes the proliferation of keratinocytes .
    Isoprocurcumenol
  • HY-147183
    JBJ-09-063

    		EGFR Cancer
    JBJ-09-063 is a mutant-selective allosteric EGFR inhibitor with IC50s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 can be used for researching EGFR-mutant lung cancer .
    JBJ-09-063
  • HY-147183A
    JBJ-09-063 TFA

    		EGFR Cancer
    JBJ-09-063 TFA is a mutant-selective allosteric EGFR inhibitor with IC50s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 TFA effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 TFA is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 TFA can be used for researching EGFR-mutant lung cancer .
    JBJ-09-063 TFA
  • HY-147183B
    JBJ-09-063 hydrochloride

    		EGFR Cancer
    JBJ-09-063 hydrochloride is a mutant-selective allosteric EGFR inhibitor with IC50s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 hydrochloride effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 hydrochloride is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 hydrochloride can be used for researching EGFR-mutant lung cancer .
    JBJ-09-063 hydrochloride
  • HY-124674A
    CCT365623 hydrochloride

    		Monoamine Oxidase EGFR Akt TGF-beta/Smad Cancer
    CCT365623 hydrochloride is an orally active lysyl oxidase (LOX) inhibitor, with an IC50 of 0.89 μM. CCT365623 hydrochloride suppresses EGFR (pY1068) and AKT phosphorylation driven by EGF. CCT365623 hydrochloride is extremely well tolerated, and has good pharmacokinetic properties .
    CCT365623 hydrochloride
  • HY-13595R
    Chrysophanol (Standard)

    Chrysophanic acid (Standard)

    		 EGFR Cancer
    Chrysophanol (Standard) is the analytical standard of Chrysophanol. This product is intended for research and analytical applications. Chrysophanol (Chrysophanic acid) is a natural anthraquinone, which inhibits EGF-induced phosphorylation of EGFR and suppresses activation of AKT and mTOR/p70S6K.
    Chrysophanol (Standard)
  • HY-103441
    JNJ28871063 hydrochloride

    		EGFR Cancer
    JNJ28871063 hydrochloride is an orally active, highly selective and ATP competitive pan-ErbB kinase inhibitor with IC50 values of 22 nM, 38 nM, and 21 nM for ErbB1, ErbB2, and ErbB4, respectively. JNJ28871063 hydrochloride inhibits phosphorylation of functionally important tyrosine residues in both EGFR and ErbB2. JNJ28871063 hydrochloride crosses the blood-brain barrier and has antitumor activity in human tumor xenograft models that overexpress EGFR and ErbB2 .
    JNJ28871063 hydrochloride
  • HY-137191
    CH7233163

    		EGFR Cancer
    CH7233163 is a noncovalent ATP-competitive inhibitor for EGFR-Del19/T790M/C797S. CH7233163 can overcome Osimertinib (HY-15772)-Resistant EGFR-Del19/T790M/C797S mutation. CH7233163 blocks the EGFR phosphorylation in the Del19/T790M/C797S_NIH3T3 cells. CH7233163 has antitumor activities .
    CH7233163
  • HY-146672
    ITK inhibitor 6

    		Itk Cancer
    ITK inhibitor 6 (compound 43) is a potent and selective ITK inhibitor with IC50s of 4 nM, 133 nM, 320 nM, 2360 nM, 155 nM for ITK, BTK, JAK3, EGFR, LCK, respectively. ITK inhibitor 6 inhibits phosphorylation of PLCγ1 and ERK1/2. ITK inhibitor 6 shows antiproliferative activities .
    ITK inhibitor 6
  • HY-115452
    G5-7

    		JAK Apoptosis Cancer
    G5-7, an orally active and allosteric JAK2 inhibitor, selectively inhibits JAK2 mediated phosphorylation and activation of EGFR (Tyr 1068) and STAT3 by binding to JAK2. G5-7 induces cell cycle arrest, apoptosis and possesses antiangiogenic effect. G5-7 has the potential for glioma study .
    G5-7
  • 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 .
    Tyrphostin AG 879
  • 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 .
    CGP77675
  • HY-P99275
    Patritumab
    1 Publications Verification

    Human Anti-ERBB3 Recombinant Antibody

    		 EGFR Akt ERK PARP Survivin Cancer
    Patritumab (Human Anti-ERBB3 Recombinant Antibody) is a neutralizing monoclonal antibody to ERBB3. Patritumab shows a synergy with Cetuximab (HY-P9905), potently inhibits the phosphorylation of EGFR, HER2, HER3, ERK, and AKT. Patritumab also induces cell apoptosis and suppresses the growth of pancreatic, non-small cell lung cancer, and colorectal cancer xenograft tumors .
    Patritumab
  • HY-105226
    CI-988

    PD134308

    		 Cholecystokinin Receptor Neurological Disease Cancer
    CI-988 (PD134308) is a potent, selective and orally active CCK2R (cholecystokinin 2 receptor) antagonist with an IC50 of 1.7 nM for mouse cortex CCK2. CI-988 shows >1600-fold selectivity for CCK2 over CCK1 receptor. CI-988 has anxiolytic and anti-tumor effects .
    CI-988
  • HY-105226B
    CI-988 hemihydrate

    PD134308 hemihydrate

    		 Cholecystokinin Receptor Neurological Disease Cancer
    CI-988 hemihydrate (PD134308) is a potent, selective and orally active CCK2R (cholecystokinin 2 receptor) antagonist with an IC50 of 1.7 nM for mouse cortex CCK2. CI-988 hemihydrate shows >1600-fold selectivity for CCK2 over CCK1 receptor. CI-988 hemihydrate has anxiolytic and anti-tumor effects .
    CI-988 hemihydrate
  • 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 .
    CGP77675 hydrate
  • HY-13653S
    (+/-)-Epigallocatechin Gallate-13C3

    		Oxidative Phosphorylation Autophagy Reactive Oxygen Species HIV Ferroptosis Mitochondrial Metabolism Endogenous Metabolite Cancer
    (+/-)-Epigallocatechin Gallate- 13C3 is the 13C-labeled (-)-Epigallocatechin Gallate. (-)-Epigallocatechin Gallate is a tea flavonoid with potent antioxidant, antiinflammatory, and anticarcinogenic properties. (-)-Epigallocatechin Gallate is reported to inhibit EGFR signaling and thereby exert anticancer effects[1]. (-)-Epigallocatechin Gallate (EGCG) is a glutamate dehydrogenase 1/2 (GDH1/2, GLUD1/2) inhibitor. Epigallocatechin-3-gallate induces oxidative phosphorylation (OXPHOS) by activating cytochrome c oxidase.
    (+/-)-Epigallocatechin Gallate-13C3
  • HY-111553
    TAS0728

    		EGFR Cancer
    TAS0728 is a potent, selective, orally active, irreversible and covalent-binding HER2 inhibitor, with an IC50 of 13 nM. TAS0728 also shows IC50s of 4.9, 8.5, 31, 65, 33, 25 and 86 nM for BMX、HER4、BLK、EGFR、JAK3、SLK and LOK respectively. Furthermore, TAS0728 exhibits robust and sustained inhibition of the phosphorylation of HER2HER3, and downstream effectors .
    TAS0728
  • HY-17408
    Mevastatin
    5+ Cited Publications

    Compactin; ML236B

    		 HMG-CoA Reductase (HMGCR) Bacterial Autophagy Apoptosis Antibiotic Infection Cardiovascular Disease Neurological Disease Metabolic Disease Cancer
    Mevastatin (Compactin) is a first HMG-CoA reductase inhibitor that belongs to the statins class. Mevastatin is a lipid-lowering agent, and induces apoptosis, arrests cancer cells in G0/G1 phase. Mevastatin also increases endothelial nitric oxide synthase (eNOS) mRNA and protein levels. Mevastatin has antitumor activity and has the potential for cardiovascular diseases treatment .
    Mevastatin
  • HY-100434
    PD-161570

    PD-161570 is a potent and ATP-competitive human FGF-1 receptor inhibitor with an IC50 of 39.9 nM and a Ki 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 .
    PD-161570
  • HY-13302
    CP-547632

    		VEGFR FGFR Cancer
    CP-547632 is an orally active, ATP-competitive and potent VEGFR-2 and FGF kinases inhibitor with IC50s of 11 nM and 9 nM, respectively. CP-547632 is selective for VEGFR2 and bFGF over EGFR, PDGFRβ, and related tyrosine kinases (TKs). CP-547632 has antitumor efficacy .
    CP-547632
  • HY-13302B
    CP-547632 hydrochloride

    		VEGFR FGFR Cancer
    CP-547632 hydrochloride is an orally active, ATP-competitive and potent VEGFR-2 and FGF kinases inhibitor with IC50s of 11 nM and 9 nM, respectively. CP-547632 hydrochloride is selective for VEGFR2 and bFGF over EGFR, PDGFRβ, and related tyrosine kinases (TKs). CP-547632 hydrochloride has antitumor efficacy .
    CP-547632 hydrochloride
  • HY-13302C
    CP-547632 TFA

    		VEGFR FGFR Cancer
    CP-547632 TFA is an orally active, ATP-competitive and potent VEGFR-2 and FGF kinases inhibitor with IC50s of 11 nM and 9 nM, respectively. CP-547632 TFA is selective for VEGFR2 and bFGF over EGFR, PDGFRβ, and related tyrosine kinases (TKs). CP-547632 TFA has antitumor efficacy .
    CP-547632 TFA
  • HY-116624
    MAZ51
    2 Publications Verification

    		 VEGFR Apoptosis Cancer
    MAZ51 is a selective inhibitor of VEGFR-3 (Flt-4) tyrosine kinase. MAZ51 inhibits VEGF-C-induced activation of VEGFR-3 without blocking VEGF-C-mediated stimulation of VEGFR2. MAZ51 had no effect on ligand-induced autophosphorylation of EGFR, IGF-1R and PDGFRβ. MAZ51 blocks proliferation and induces apoptosis in a wide variety of tumor cells. Antitumor activity .
    MAZ51
  • HY-P1845
    PACAP-38 (31-38), human, mouse, rat

    		ERK EGFR Reactive Oxygen Species Calcium Channel Neurological Disease
    PACAP-38 (31-38), human, mouse, rat is a PAC1 receptor activator and increases the α-secretase activity. PACAP-38 (31-38), human, mouse, rat elevates cytosolic Ca 2+, increases proliferation and increases phosphorylation of extracellular regulates kinase (ERK) and the epidermal growth factor receptor (EGFR). PACAP-38 (31-38), human, mouse, rat demonstrates potent, efficacious, and sustained stimulatory effects on sympathetic neuronal NPY and catecholamine production. PACAP-38 (31-38), human, mouse, rat can be used for neurotrophic and neuroprotective research .
    PACAP-38 (31-38), human, mouse, rat
  • HY-P1845A
    PACAP-38 (31-38), human, mouse, rat TFA

    		ERK EGFR Reactive Oxygen Species Calcium Channel Neurological Disease
    PACAP-38 (31-38), human, mouse, rat TFA is a PAC1 receptor activator and increases the α-secretase activity. PACAP-38 (31-38), human, mouse, rat TFA elevates cytosolic Ca 2+, increases proliferation and increases phosphorylation of extracellular regulates kinase (ERK) and the epidermal growth factor receptor (EGFR). PACAP-38 (31-38), human, mouse, rat TFA demonstrates potent, efficacious, and sustained stimulatory effects on sympathetic neuronal NPY and catecholamine production. PACAP-38 (31-38), human, mouse, rat TFA can be used for neurotrophic and neuroprotective research .
    PACAP-38 (31-38), human, mouse, rat TFA
  • HY-50895
    Gefitinib
    Maximum Cited Publications
    114 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 .
    Gefitinib

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