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GIST

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18

Inhibitors & Agonists

1

Inhibitory Antibodies

1

Natural
Products

1

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • 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-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-128602

    c-Kit Cancer
    c-Kit-IN-2 is a c-KIT inhibitor with an IC50 of 82 nM, shows superior antiproliferative activities against all the three GIST cell lines, GIST882, GIST430, and GIST48, with GI50s of 3, 1, and 2 nM, respectively .
    c-Kit-IN-2
  • 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-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-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-178219

    Drug-Linker Conjugates for ADC Microtubule/Tubulin Apoptosis Cancer
    4-(3-Tosyl-2-(tosylmethyl)propanoyl)benzoic acid-glu(PEG24-Me)-val-cit-NH-benzyloxyformic acid-MMAE is a drug-linker conjugate for ADC. 4-(3-Tosyl-2-(tosylmethyl)propanoyl)benzoic acid-glu(PEG24-Me)-val-cit-NH-benzyloxyformic acid-MMAE contains a linker and bioactive small molecule toxins MMAE (HY-15162). 4-(3-Tosyl-2-(tosylmethyl)propanoyl)benzoic acid-glu(PEG24-Me)-val-cit-NH-benzyloxyformic acid-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) .
    4-(3-Tosyl-2-(tosylmethyl)propanoyl)benzoic acid-glu(PEG24-Me)-val-cit-NH-benzyloxyformic acid-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-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-168579

    c-Kit Cancer
    c-Kit-IN-6 (Compound 101) is an inhibitor of c-Kit with an IC50 value ranging between 100 nM and 1 μM. Additionally, c-Kit-IN-6 can inhibit the proliferation of GIST430 and BaF3 mutant cells .
    c-Kit-IN-6
  • HY-168581

    c-Kit Cancer
    c-Kit-IN-8 (Compound 53) is an inhibitor for c-Kit kinase, that inhibits uKIT kinase with an IC50 > 1 μM. c-Kit-IN-8 inhibits the proliferation of cancer cell GIST430 and BaF3 wildtype and mutants with IC50 > 0.1 μM .
    c-Kit-IN-8
  • HY-168580

    c-Kit Cancer
    c-Kit-IN-7 (Compound 104) is a potent inhibitor of c-Kit, with IC50 values of ≤10 nM. c-Kit-IN-7 inhibits the cell proliferation in GIST430 and BaF3 mutants, with IC50 values of ≤100 nM. c-Kit-IN-7 plays an important role in cancer driven by c-KIT kinase mutations research .
    c-Kit-IN-7
  • 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-112616

    NAMPT Drug-Linker Conjugates for ADC Cancer
    NAMPT inhibitor-linker 2 is a agent-linker conjugates for ADC, composed of an NAMPT inhibitor as a payload, and a linker. ADC-4 consists of an NAMPT inhibitor-linker 2 and an anti-c-Kit monoclonal antibody, exihibits potent activity against c-Kit expressing cell lines such as GIST-T1 and NCI-H526, with IC50s of <7 pM and 40 pM, respectively.
    NAMPT inhibitor-linker 2
  • HY-112615

    Drug-Linker Conjugates for ADC Cancer
    NAMPT inhibitor-linker 1 is a agent-linker conjugates for ADC, composed of an NAMPT inhibitor as a payload, and a linker. ADC-3 consists of an NAMPT inhibitor-linker 1 and an anti-c-Kit monoclonal antibody, exihibits potent activity against c-Kit expressing cell lines such as GIST-T1 and NCI-H526 cells, with IC50s of <3 pM and 9 pM, respectively.
    NAMPT inhibitor-linker 1
  • 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-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

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