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gastrointestinal stromal tumor

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製品番号 製品名 Target 研究分野 構造式
  • HY-13001
    Quizartinib
    Maximum Cited Publications
    45 Publications Verification

    AC220

    FLT3 Apoptosis PDGFR c-Kit Cancer
    Quizartinib (AC220) is an orally active, potent and selective FLT3 inhibitor. Quizartinib inhibits kinase activity of mutant-FLT3, -PDGFRA and -KIT isoforms and inhibits autophosphorylation. Quizartinib inhibits cellular proliferation, induces apoptosis in cancer cells. Quizartinib can be used for the research of cancer .
    Quizartinib
  • HY-156619

    EVT-8565072; THB335

    c-Kit PDGFR Metabolic Disease Inflammation/Immunology
    Labuxtinib (EVT-8565072; THB335) is a potent dual inhibitor of c-Kit and PDGFR. Labuxtinib exhibits potent inhibitory activity against wild-type c-Kit (IC50 = 0.005 μM). Labuxtinib inhibits SCF-dependent and PDGF-dependent cell proliferation, and blocks the proliferation of cells dependent on c-Kit or PDGFR signaling pathways. In animal models of skin allergy, Labuxtinib depletes skin mast cells and significantly alleviates anaphylactic shock responses. Labuxtinib can be used in research on mast cell-related diseases, respiratory diseases, inflammatory diseases, fibrotic diseases, metabolic diseases, and other related conditions .
    Labuxtinib
  • HY-B0523A
    Anagrelide hydrochloride
    3 Publications Verification

    BL4162A

    Phosphodiesterase (PDE) Apoptosis Cardiovascular Disease Cancer
    Anagrelide hydrochloride (BL4162A) is a potent inhibitor of phosphodiesterase type III (PDE3) (IC50=36 nM). Anagrelide hydrochloride, an imidazoquinazoline derivative, acts as an inhibitor of platelet aggregation. Anagrelide hydrochloride inhibits bone marrow megakaryocytopoiesis. Anagrelide hydrochloride decreases gastrointestinal stromal tumor (GIST) cell proliferation and promotes their apoptosis in vitro. Anagrelide hydrochloride is a platelet-lowering agent and plays in the antithrombopoietic action .
    Anagrelide hydrochloride
  • HY-G0017
    N-Desmethyl imatinib
    1 Publications Verification

    Norimatinib; Imatinib metabolite N-Desmethyl imatinib; CGP 74588

    Drug Metabolite P-glycoprotein Apoptosis Neurological Disease Cancer
    N‑Desmethyl imatinib (Norimatinib) is an active metabolite of Imatinib (HY-15463), a selective c‑Abl inhibitor, and a substrate of P‑glycoprotein. N-Desmethyl imatinib binds to the c-Abl catalytic domain to prevent substrate phosphorylation, inhibits c-Abl-mediated α-synuclein activation and downstream inflammatory signaling pathways. N-Desmethyl imatinib induces apoptosis in K562 human leukemia cells. N-Desmethyl imatinib shows significantly elevated plasma levels in gastrointestinal stromal tumor (GIST) models with mild SARS-CoV-2 infection. N-Desmethyl imatinib can be used for the research of Parkinson’s disease, gastrointestinal stromal tumor, and chronic myeloid leukemia .
    N-Desmethyl imatinib
  • HY-B0523
    Anagrelide
    3 Publications Verification

    Phosphodiesterase (PDE) Apoptosis Cardiovascular Disease Cancer
    Anagrelide is a potent inhibitor of phosphodiesterase type III (PDE3) (IC50=36 nM). Anagrelide, an imidazoquinazoline derivative, acts as an inhibitor of platelet aggregation. Anagrelide inhibits bone marrow megakaryocytopoiesis. Anagrelide decreases gastrointestinal stromal tumor (GIST) cell proliferation and promotes their apoptosis in vitro. Anagrelide is a platelet-lowering agent and plays in the antithrombopoietic action .
    Anagrelide
  • HY-162730

    Molecular Glues Phosphodiesterase (PDE) Cancer
    OPB-171775 is an orally active molecular glue. OPB-171775 forms ternary complex with phosphodiesterase 3A (PDE3A) and schlafen family member 12 (SLFN12). OPB-171775 causes SLFN12 RNase-mediated cell death, activates SLFN12 RNase-associated GCN2 signaling pathway. OPB-171775 exhibits significant efficacy against gastrointestinal stromal tumor .
    OPB-171775
  • HY-112802

    c-Kit Cancer
    AZD3229 is a potent pan-KIT mutant inhibitor for the treatment of gastrointestinal stromal tumors. AZD3229 inhibits c-KIT with an IC50 value of 223.3 nM .
    AZD3229
  • HY-177578

    Antibody-Drug Conjugates (ADCs) c-Kit Apoptosis Microtubule/Tubulin ERK Akt Caspase Cancer
    NN3201 is a c-Kit-targeting antibody-drug conjugate (ADC) with high affinity (KD = 0.19 pM). NN3201 is composed of 4-(3-Tosyl-2-(tosylmethyl)propanoyl)benzoic acid-glu(PEG24-Me)-val-cit-NH-benzyloxyformic acid-MMAE (HY-178219) and an anti-c-Kit human monoclonal antibody NN2101 (HY-P991293). NN3201 rapidly internalizes and inhibits stem cell factor (SCF)-driven signaling, thereby delivering its payload to induce cell cycle arrest and apoptosis. NN3201 exhibits no Fc-mediated effector functions antibody-dependent cell-mediated cytotoxicity (ADCC)/complement-dependent cytotoxicity (CDC) due to reduced FcγR binding. NN3201 exhibits significant c-Kit-dependent anti-tumor efficacies in various tumor models. NN3201 can be used in small cell lung cancer (SCLC) and gastrointestinal stromal tumor (GIST) and acute myeloid leukemia (AML) research [1][2].
    NN3201
  • HY-G0017S

    Norimatinib-d8; Imatinib metabolite N-Desmethyl imatinib-d8; CGP 74588-d8

    Isotope-Labeled Compounds Drug Metabolite P-glycoprotein Apoptosis Neurological Disease Cancer
    N-Desmethyl imatinib-d8 is a deuterium labeled Imatinib metabolite N-Desmethyl Imatinib (HY-G0017). N‑Desmethyl imatinib (Norimatinib) is an active metabolite of Imatinib (HY-15463), a selective c‑Abl inhibitor, and a substrate of P‑glycoprotein. N-Desmethyl imatinib binds to the c-Abl catalytic domain to prevent substrate phosphorylation, inhibits c-Abl-mediated α-synuclein activation and downstream inflammatory signaling pathways. N-Desmethyl imatinib induces apoptosis in K562 human leukemia cells. N-Desmethyl imatinib exhibits significantly elevated plasma levels in gastrointestinal stromal tumor (GIST) settings following mild SARS CoV 2 infection. N-Desmethyl imatinib can be used for the research of Parkinson’s disease, gastrointestinal stromal tumor, and chronic myeloid leukemia .
    N-Desmethyl imatinib-d8
  • HY-B1514R

    Reference Standards Endogenous Metabolite Others
    Anagrelide (hydrochloride) (Standard) is the analytical standard of Anagrelide (hydrochloride). This product is intended for research and analytical applications. Anagrelide hydrochloride (BL4162A) is a potent inhibitor of phosphodiesterase type III (PDE3) (IC50=36 nM). Anagrelide hydrochloride, an imidazoquinazoline derivative, acts as an inhibitor of platelet aggregation. Anagrelide hydrochloride inhibits bone marrow megakaryocytopoiesis. Anagrelide hydrochloride decreases gastrointestinal stromal tumor (GIST) cell proliferation and promotes their apoptosis in vitro. Anagrelide hydrochloride is a platelet-lowering agent and plays in the antithrombopoietic action .
    Allantoic acid (Standard)
  • HY-178219

    Drug-Linker Conjugates for ADC Microtubule/Tubulin Apoptosis Cancer
    Bis-sulfone-(PEG24)-Glu-Val-Cit-PAB-MMAE is a drug-linker conjugate for ADC. Bis-sulfone-(PEG24)-Glu-Val-Cit-PAB-MMAE contains a linker and bioactive small molecule toxins MMAE (HY-15162). Bis-sulfone-(PEG24)-Glu-Val-Cit-PAB-MMAE can conjugate with NN2101 (HY-P991293) (anti c-Kit) for synthesizing NN3201. NN3201 rapidly internalizes and inhibits SCF-driven signaling, thereby delivering its payload to induce cell cycle arrest and apoptosis. NN3201 exhibits significant c-Kit-dependent anti-tumor efficacies in various tumor models, such as small cell lung cancer (SCLC) and gastrointestinal stromal tumor (GIST) .
    Bis-sulfone-(PEG24)-Glu-Val-Cit-PAB-MMAE
  • HY-128589

    c-Kit Cancer
    CHMFL-KIT-033 is a potent and selective inhibitor of c-KIT T670I mutant for gastrointestinal stromal tumors (GISTs), with an IC50 of 0.045 μM .
    CHMFL-KIT-033
  • HY-177275

    c-Kit Cancer
    c-Kit Receptor modulator-1 (Compound #22) is a c-Kit Receptor modulator. c-Kit Receptor modulator-1 can be used for malignant cancers such as canine mastocytoma, human gastrointestinal stromal tumor and small cell lung cancer research .
    c-Kit Receptor modulator-1
  • HY-170911

    PDGFR Cancer
    KIT/PDGFRA-IN-1 (compound 19) is a stem cell growth factor receptor (KIT) and platelet-derived growth factor receptor alpha (PDGFRA) inhibitor. KIT/PDGFRA-IN-1 inhibits KIT-wt, KIT-D816H, KIT-T670I, PDGFRA-wt, PDGFRA-D842V, PDGFRA-T674I and PDGFRA-G680R with IC50s of 2.3, 12, 492, 0.8, 99.9, 42.3, and 4.3 μM, respectively. KIT/PDGFRA-IN-1 inhibits GIST-T1, T1-a-D842V and GIST-48B cells (PDGFR- and KIT-Mutant GIST cell Lines) with GR50s of 12, 8900, ≥10 000 nM, respectively .
    KIT/PDGFRA-IN-1
  • HY-173275

    PDGFR Cancer
    PDGFRα kinase inhibitor 3 (Compound L7) is a highly potent inhibitor targeting the PDGFRα D842V kinase with IC50s values of 23.8 nM and 2.1 nM in biochemical and cellular assays, respectively. PDGFRα kinase inhibitor 3 binds to the ATP-binding pocket of PDGFRα D842V to block its downstream signaling pathways and inhibit kinase activity. PDGFRα kinase inhibitor 3 can be used for gastrointestinal stromal tumors (GISTs) study .
    PDGFRα kinase inhibitor 3
  • HY-P990851

    c-Kit Inflammation/Immunology Cancer
    Anti-c-Kit/CD117 Antibody (SR-1) is a kind of mouse IgG2a κ chimeric antibody inhibitor, targeting to human c-Kit/CD117. Anti-c-Kit/CD117 Antibody (SR-1) binds to the extracellular domain of human c-Kit (also known as CD117) and blocks stem cell factor (SCF) binding to CD117. Anti-c-Kit/CD117 Antibody (SR-1) can be used for the researches of cancer and immunology, such as gastrointestinal stromal tumor (GIST) and xenograft .
    Anti-c-Kit/CD117 Antibody (SR-1)
  • HY-B0523B

    Phosphodiesterase (PDE) Apoptosis Cardiovascular Disease Cancer
    Anagrelide hydrochloride monohydrate is a potent inhibitor of phosphodiesterase type III (PDE3) (IC50=36 nM). Anagrelide hydrochloride monohydrate, an imidazoquinazoline derivative, acts as an inhibitor of platelet aggregation. Anagrelide hydrochloride monohydrate inhibits bone marrow megakaryocytopoiesis. Anagrelide hydrochloride monohydrate decreases gastrointestinal stromal tumor (GIST) cell proliferation and promotes their apoptosis in vitro. Anagrelide hydrochloride monohydrate is a platelet-lowering agent and plays in the antithrombopoietic action .
    Anagrelide hydrochloride monohydrate
  • HY-B0523AR

    BL4162A (Standard)

    Reference Standards Phosphodiesterase (PDE) Apoptosis Cardiovascular Disease Cancer
    Anagrelide (hydrochloride) (Standard) is the analytical standard of Anagrelide (hydrochloride). This product is intended for research and analytical applications. Anagrelide hydrochloride (BL4162A) is a potent inhibitor of phosphodiesterase type III (PDE3) (IC50=36 nM). Anagrelide hydrochloride, an imidazoquinazoline derivative, acts as an inhibitor of platelet aggregation. Anagrelide hydrochloride inhibits bone marrow megakaryocytopoiesis. Anagrelide hydrochloride decreases gastrointestinal stromal tumor (GIST) cell proliferation and promotes their apoptosis in vitro. Anagrelide hydrochloride is a platelet-lowering agent and plays in the antithrombopoietic action .
    Anagrelide hydrochloride (Standard)
  • HY-112802A

    AZD3229 tosylate

    c-Kit Cancer
    AZD3229 Tosylate is a potent pan-KIT mutant inhibitor for the treatment of gastrointestinal stromal tumors.
    Ubavitinib tosylate
  • HY-W591818

    Drug Derivative Cancer
    Sunitinib carboxylic acid is a carboxylic acid metabolite of Sunitinib (HY-10255A). Sunitinib is a multi-target tyrosine kinase inhibitor, mainly used to inhibit malignant tumors such as gastrointestinal stromal tumors, renal cell carcinoma, and pancreatic neuroendocrine tumors .
    Sunitinib carboxylic acid
  • HY-G0017A

    Norimatinib mesylate; Imatinib metabolite N-Desmethyl imatinib mesylate; CGP 74588 mesylate

    Drug Metabolite P-glycoprotein Apoptosis Neurological Disease Cancer
    N-Desmethyl imatinib mesylate (Norimatinib mesylate) is an active metabolite of Imatinib (HY-15463), a selective c‑Abl inhibitor, and a substrate of P‑glycoprotein. N-Desmethyl imatinib mesylate binds to the c-Abl catalytic domain to prevent substrate phosphorylation, inhibits c-Abl-mediated α-synuclein activation and downstream inflammatory signaling pathways. N-Desmethyl imatinib mesylate induces apoptosis in K562 human leukemia cells. N-Desmethyl imatinib mesylate exhibits significantly elevated plasma levels in gastrointestinal stromal tumor (GIST) settings following mild SARS CoV 2 infection. N-Desmethyl imatinib mesylate can be used for the research of Parkinson’s disease, gastrointestinal stromal tumor, and chronic myeloid leukemia .
    N-Desmethyl imatinib mesylate
  • HY-G0017S1

    Norimatinib-d4; Imatinib metabolite N-Desmethyl imatinib-d4; CGP 74588-d4

    Isotope-Labeled Compounds Drug Metabolite P-glycoprotein Apoptosis Neurological Disease Cancer
    N-Desmethyl imatinib-d4 is the deuterium-labeled N-Desmethyl imatinib (HY-G0017). N‑Desmethyl imatinib (Norimatinib) is an active metabolite of Imatinib (HY-15463), a selective c‑Abl inhibitor, and a substrate of P‑glycoprotein. N-Desmethyl imatinib binds to the c-Abl catalytic domain to prevent substrate phosphorylation, inhibits c-Abl-mediated α-synuclein activation and downstream inflammatory signaling pathways. N-Desmethyl imatinib induces apoptosis in K562 human leukemia cells. N-Desmethyl imatinib exhibits significantly elevated plasma levels in gastrointestinal stromal tumor (GIST) settings following mild SARS CoV 2 infection. N-Desmethyl imatinib can be used for the research of Parkinson’s disease, gastrointestinal stromal tumor, and chronic myeloid leukemia .
    N-Desmethyl imatinib-d4
  • HY-G0017R

    Norimatinib (Standard); Imatinib metabolite N-Desmethyl imatinib (Standard); CGP 74588 (Standard)

    Reference Standards Drug Metabolite P-glycoprotein Apoptosis Others
    N‑Desmethyl imatinib (Standard) is the analytical standard of N‑Desmethyl imatinib (Norimatinib) (HY-G0017R). This product is intended for research and analytical applications. N‑Desmethyl imatinib (Norimatinib) is an active metabolite of Imatinib (HY-15463), a selective c‑Abl inhibitor, and a substrate of P‑glycoprotein. N-Desmethyl imatinib binds to the c-Abl catalytic domain to prevent substrate phosphorylation, inhibits c-Abl-mediated α-synuclein activation and downstream inflammatory signaling pathways. N-Desmethyl imatinib induces apoptosis in K562 human leukemia cells. N-Desmethyl imatinib exhibits significantly elevated plasma levels in gastrointestinal stromal tumor (GIST) settings following mild SARS CoV 2 infection. N-Desmethyl imatinib can be used for the research of Parkinson’s disease, gastrointestinal stromal tumor, and chronic myeloid leukemia .
    N-Desmethyl imatinib (Standard)
  • HY-117253

    Drug Metabolite Cancer
    PHA-782584 is a metabolite of sunitinib. Sunitinib is an oral multitargeted tyrosine kinase inhibitor with antitumor activities .
    PHA-782584
  • HY-B0523S

    Apoptosis Phosphodiesterase (PDE) Isotope-Labeled Compounds Cardiovascular Disease Cancer
    Anagrelide- 13C2, 15N,d2 is 15N and deuterated labeled Anagrelide (HY-B0523). Anagrelide is a potent inhibitor of phosphodiesterase type III (PDE3) (IC50=36 nM). Anagrelide, an imidazoquinazoline derivative, acts as an inhibitor of platelet aggregation. Anagrelide inhibits bone marrow megakaryocytopoiesis. Anagrelide decreases gastrointestinal stromal tumor (GIST) cell proliferation and promotes their apoptosis in vitro. Anagrelide is a platelet-lowering agent and plays in the antithrombopoietic action .
    Anagrelide-13C2,15N,d2
  • HY-182043

    c-Kit PDGFR Cancer
    BLU-654 is an orally active antineoplastic agent and KIT inhibitor. BLU-654 is a highly selective inhibitor targeting wild-type KIT, PDGFRβ, and KIT V654A over most other kinases in the kinome. BLU-654 exerts sustained antineoplastic activity in KIT V654A cell-derived xenograft mouse models. BLU-654 can be used in research related to Imatinib (HY-15463)-resistant gastrointestinal stromal tumors .
    BLU-654
  • HY-162730R

    Reference Standards Molecular Glues Phosphodiesterase (PDE) Cancer
    OPB-171775 (Standard) is the analytical standard of OPB-171775 (HY-162730). This product is intended for research and analytical applications. OPB-171775 is an orally active molecular glue. OPB-171775 forms ternary complex with phosphodiesterase 3A (PDE3A) and schlafen family member 12 (SLFN12). OPB-171775 causes SLFN12 RNase-mediated cell death, activates SLFN12 RNase-associated GCN2 signaling pathway. OPB-171775 exhibits significant efficacy against gastrointestinal stromal tumor.
    OPB-171775 (Standard)
  • HY-17674

    Bombesin Receptor Neurological Disease Cancer
    Bombesin receptor antagonist-1 (Example 32) is a bombesin receptor antagonist with Ki values for neurotide B (NMB receptor) and gastrin-releasing peptide receptor (GRP receptor) of 0.17 and 20 nM respectively. Bombesin receptor antagonist-1 can be used to study various diseases, such as cancer, depression, and eating disorders .
    Bombesin receptor antagonist-1

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