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Results for "

KIT/PDGFRA-driven GIST

" in MedChemExpress (MCE) Product Catalog:

193

Inhibitors & Agonists

2

Biochemical Assay Reagents

112

MCE Kits

7

Inhibitory Antibodies

3

Natural
Products

21

Recombinant Proteins

27

Isotope-Labeled Compounds

3

Antibodies

3

Oligonucleotides

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-15240
    c-Kit-IN-1
    1 Publications Verification

    c-Kit c-Met/HGFR Cancer
    c-Kit-IN-1 is a potent inhibitor of c-Kit and c-Met with IC50s of <200 nM.
    c-Kit-IN-1
  • HY-18302

    c-Kit Inflammation/Immunology
    c-Kit-IN-5 is potent inhibitor of c-Kit, with IC50s of 22 nM and 16 nM in kinase assay and cell assay, respectively. c-Kit-IN-5 shows more than 200-fold selectivity for c-Kit over KDR, p38, Lck, and Src. c-Kit-IN-5 also exhibits desirable pharmacokinetic properties .
    c-Kit-IN-5-1
  • 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-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-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-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-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-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-101034

    CHMFL-ABL-KIT-155

    Bcr-Abl c-Kit Apoptosis PDGFR Discoidin Domain Receptor Cancer
    CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155; compound 34) is a highly potent and orally active type II ABL/c-KIT dual kinase inhibitor (IC50s of 46 nM and 75 nM, respectively), and it also presents significant inhibitory activities to BLK (IC50=81 nM), CSF1R (IC50=227 nM), DDR1 (IC50=116 nM), DDR2 (IC50=325 nM), LCK (IC50=12 nM) and PDGFRβ (IC50=80 nM) kinases. CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155) arrests cell cycle progression and induces apoptosis .
    CHMFL-ABL/KIT-155
  • HY-RS07319

    Small Interfering RNA (siRNA) Others

    KIT Human Pre-designed siRNA Set A contains three designed siRNAs for KIT gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

    KIT Human Pre-designed siRNA Set A
    KIT Human Pre-designed siRNA Set A
  • HY-RS07320

    Small Interfering RNA (siRNA) Others

    Kit Mouse Pre-designed siRNA Set A contains three designed siRNAs for Kit gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

    Kit Mouse Pre-designed siRNA Set A
    Kit Mouse Pre-designed siRNA Set A
  • HY-RS07321

    Small Interfering RNA (siRNA) Others

    Kit Rat Pre-designed siRNA Set A contains three designed siRNAs for Kit gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

    Kit Rat Pre-designed siRNA Set A
    Kit Rat Pre-designed siRNA Set A
  • HY-P990615

    LOP628 antibody

    c-Kit Inflammation/Immunology
    Anti-c-Kit Antibody (LMJ729) (LOP628 antibody) is a CHO-expressed human antibody that targets SCFR/c-Kit/CD117. The predicted molecular weight (MW) of Anti-c-Kit Antibody (LMJ729) is 150 kDa. The isotype control for Anti-c-Kit Antibody (LMJ729) can refer to Human IgG1 kappa, Isotype Control (HY-P99001).
    Anti-c-Kit Antibody (LMJ729)
  • HY-P990851

    c-Kit Others
    Anti-c-Kit/CD117 Antibody (SR-1) is a kind of mouse IgG2a, κ chimeric antibody, targeting to human c-Kit/CD117. The recommend isotype control of Anti-c-Kit/CD117 Antibody (SR-1): Mouse IgG2a kappa, Isotype Control (HY-P99978).
    Anti-c-Kit/CD117 Antibody (SR-1)
  • HY-KT001

    E3 Ligase Ligand-Linker Conjugates Cancer
    E3 Ligase Ligand-Linker Conjugate Kit is a series of synthesized compounds that incorporate an E3 ligase ligand and a linker used in PROTAC technology.
    E3 Ligase Ligand-Linker Conjugate Kit
  • HY-132451S

    Isotope-Labeled Compounds Cancer
    (R,S)-4-Hydroxy Cyclophosphamide-d4 Preparation Kit is the deuterium labeled (R,S)-4-Hydroxy Cyclophosphamide Preparation Kit. (R,S)-4-Hydroxy Cyclophosphamide is an isomer of 4-Hydroxycyclophosphamide, the active metabolite of the cytotoxic alkylating agent Cyclophosphamide (HY-17420) .
    (R,S)-4-Hydroxy Cyclophosphamide-d4 Preparation Kit
  • HY-P99462

    CDX-0159; CDX-0158

    c-Kit Inflammation/Immunology
    Barzolvolimab (CDX 0159) is a humanized anti-KIT IgG1 monoclonal antibody. Barzolvolimab specificity and potently inhibits KIT activation by SCF. Barzolvolimab can reduce skin mast cells and disease activity in chronic inducible urticaria .
    Barzolvolimab
  • HY-145557

    CGT9486; PLX 9486

    c-Kit Cancer
    Bezuclastinib (CGT9486) is an orally active, highly selective tyrosine kinase inhibitor with potent activity against KIT D816V. Bezuclastinib can be used for the research of nonadvanced systemic mastocytosis (NonAdvSM) .
    Bezuclastinib
  • 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-18317

    VEGFR RET c-Kit Cancer
    JNJ-38158471 is a well tolerated, orally available, highly selective VEGFR-2 inhibitor, with an IC50 of 40 nM. JNJ-38158471 also inhibits Ret and Kit with IC50s of 180 and 500 nM, respectively .
    JNJ-38158471
  • 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-P990002

    c-Kit Cancer
    Anti-Mouse CD117/c-Kit Antibody (2B8) is an IgG2b antibody inhibitor against mouse CD117. Derived from rat.
    Anti-Mouse CD117/c-Kit Antibody (2B8)
  • HY-W143698

    Bcr-Abl c-Kit PDGFR Cancer
    PDGFRα kinase inhibitor 2 (compound 1), an Imatinib (HY-15463) analogue, is a covalent and irreversible kinase inhibitor with IC50s of 6.95 μM, 2.45 μM, 1.39 μM for ABL1 wt, KIT wt, PDGFRR wt .
    PDGFRα kinase inhibitor 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-B0523A
    Anagrelide hydrochloride
    2 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-B0523AR

    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-15198

    Raf PDGFR FLT3 c-Kit Cancer
    KG5 is an orally active dual PDGFRβ and B-Raf allosteric inhibitor. KG5 also inhibits Flt3, KIT and c-Raf. KG5 has anticancer, antiangiogenic activities .
    KG5
  • HY-139996

    PROTACs Apoptosis FLT3 c-Kit FGFR VEGFR PDGFR c-Fms Cancer
    Pomalidomide-C5-Dovitinib (compound 2) is a PROTAC containing Pomalidomide, Dovitinib and connected with CRBN. Pomalidomide-C5-Dovitinib shows enhanced antiproliferative effects against FLT3-ITD+ AML cells. Pomalidomide-C5-Dovitinib induces the degradation of the FLT3-ITD and KIT proteins in a ubiquitin-proteasome-dependent manner and completely blocks their downstream signaling pathway. Pomalidomide-C5-Dovitinib has the potential for the research of FLT3-ITD + acute myeloid leukemia .
    Pomalidomide-C5-Dovitinib
  • HY-121708

    c-Kit Cancer
    KI-328 is a novel inhibitor targeting KIT kinase that has selective activity against some KIT mutant kinases commonly found in acute myeloid leukemia (AML). KI-328 showed specificity for KIT kinase in in vitro kinase assays and inhibited the growth of wild-type (Wt) and mutant KIT-expressing cells, but had lower activity against D816V-KIT. Comparative analysis of the inhibitory effects of several potent KIT inhibitors on the growth of multiple mutant KIT-expressing cells showed that the multi-kinase inhibitors had comparable activity against D816V-KIT as against other mutant KITs; however, heat shock protein 90 (HSP90) inhibitors showed significant activity against D816V-KIT, inhibiting the growth of D816V-KIT-expressing cells at concentrations that did not affect the growth of other mutant KIT-expressing cells. These results suggest that potent KIT inhibitors have different activities against different types of KIT mutant kinases. Therefore, in clinical development, KIT inhibitors need to validate their activity against multiple types of KIT mutant kinases.
    KI-328
  • HY-10638

    c-Kit Apoptosis Cancer
    AP23464 is an ATP-based inhibitor for Kit, that inhibits the phosphorylation of Kit wildtype and mutants, with IC50 of 5-85 nM. AP23464 inhibits the proliferation of Kit mutated cells (IC50 is 3-20 nM), arrests the cell cycle at G0/G1 phase, and induces apoptosis in Kit mutated cells .
    AP23464
  • HY-16961
    Sitravatinib
    5 Publications Verification

    MGCD516; MG-516

    VEGFR c-Kit FLT3 Discoidin Domain Receptor Trk Receptor Inflammation/Immunology Cancer
    Sitravatinib (MGCD516) is an orally bioavailable receptor tyrosine kinase (RTK) inhibitor with IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively . Sitravatinib shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment .
    Sitravatinib
  • HY-16961A

    MGCD516 malate; MG-516 malate

    VEGFR c-Kit FLT3 Discoidin Domain Receptor Trk Receptor Inflammation/Immunology Cancer
    Sitravatinib malate (MGCD516 malate) is an orally bioavailable receptor tyrosine kinase (RTK) inhibitor with IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively . Sitravatinib malate shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment .
    Sitravatinib malate
  • 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-101443
    ISCK03
    3 Publications Verification

    c-Kit Inflammation/Immunology
    ISCK03 is a SCF/c-Kit and CD117-specific inhibitor. ISCK03 significantly inhibits c-Kit phosphorylation at 10 μM .
    ISCK03
  • HY-10331S

    BAY 73-4506-d3

    VEGFR Autophagy PDGFR Raf RET Cancer
    Regorafenib-d3 is a deuterium labeled Regorafenib. Regorafenib is a multi-targeted receptor tyrosine kinase inhibitor[1].
    Regorafenib-d3
  • HY-156619

    c-Kit Cancer
    Labuxtinib is c-kit tyrosine kinase inhibitor .
    Labuxtinib
  • HY-10873
    N-Desethyl Sunitinib
    5+ Cited Publications

    SU-12662

    Drug Metabolite Cancer
    N-Desethyl Sunitinib (SU-12662) is a metabolite of sunitinib. Sunitinib is a potent, ATP-competitive VEGFR, PDGFRβ and KIT inhibitor with Ki values of 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT, respectively .
    N-Desethyl Sunitinib
  • HY-138813

    SU-12662 hydrochloride

    Drug Metabolite Cancer
    N-Desethyl Sunitinib (SU-12662) (hydrochloride) is a metabolite of sunitinib. Sunitinib is a potent, ATP-competitive VEGFR, PDGFRβ and KIT inhibitor with Ki values of 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT, respectively .
    N-Desethyl Sunitinib hydrochloride
  • HY-112452

    VEGFR FGFR PDGFR c-Kit Apoptosis Cancer
    SU11652 is a potent receptor tyrosine kinase (RTK) inhibitor. SU11652 also inhibits several members of the split kinase family of RTKs, including VEGFR, FGFR, PDGFR, and Kit. SU11652 can be uesd for spontaneous cancers expressing Kit mutations research .
    SU11652
  • HY-B0523
    Anagrelide
    2 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-112802A

    c-Kit Cancer
    AZD3229 Tosylate is a potent pan-KIT mutant inhibitor for the treatment of gastrointestinal stromal tumors.
    AZD3229 Tosylate
  • HY-P990020

    c-Kit Others
    Eglatoprutug is an humanized immunoglobulin G1-kappa, anti-c-Kit monoclonal antibody .
    Eglatoprutug
  • HY-13838

    c-Fms c-Kit Cancer
    PLX647 is an orally active, highly specific dual FMS and KIT kinase inhibitor, with IC50s of 28 and 16 nM, respectively. PLX647 shows selectivity for FMS and KIT over a panel of 400 kinases at a concentration of 1 μM except FLT3 and KDR (IC50s=91 and 130 nM, respectively) .
    PLX647
  • HY-10873S

    Isotope-Labeled Compounds Drug Metabolite Cancer
    N-Desethyl Sunitinib-d5 is the deuterium labeled N-Desethyl Sunitinib. N-Desethyl Sunitinib (SU-12662) is a metabolite of sunitinib. Sunitinib is a potent, ATP-competitive VEGFR, PDGFRβ and KIT inhibitor with Ki values of 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT, respectively[1].
    N-Desethyl Sunitinib-d5
  • HY-13838A

    c-Fms c-Kit Inflammation/Immunology Cancer
    PLX647 dihydrochloride is an orally active, highly specific dual FMS and KIT kinase inhibitor, with IC50s of 28 and 16 nM, reapectively. PLX647 dihydrochloride shows selectivity for FMS and KIT over a panel of 400 kinases at a concentration of 1 μM except FLT3 and KDR (IC50s=91 and 130 nM, respectively) .
    PLX647 dihydrochloride
  • HY-10873S2

    SU-12662-d5 hydrochloride

    Isotope-Labeled Compounds Drug Metabolite Cancer
    N-Desethyl Sunitinib-d5 (hydrochloride) is a deuterated labeled N-Desethyl Sunitinib . N-Desethyl Sunitinib (SU-12662) is a metabolite of sunitinib. Sunitinib is a potent, ATP-competitive VEGFR, PDGFRβ and KIT inhibitor with Ki values of 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT, respectively .
    N-Desethyl Sunitinib-d5 hydrochloride
  • HY-107458

    c-Kit Cancer
    AP23848 is an ATP-dependent kinase inhibitor that effectively and selectively targets the Kit activation loop mutation both in vitro and in vivo, showing anti-tumor activity. AP23848 can inhibit the phosphorylation of the activated Kit mutation and tumor growth in mice, making it suitable for targeting diseases with the D816V mutation, such as systemic mastocytosis (SM) and acute myeloid leukemia (AML) research .
    AP23848
  • HY-50946
    Imatinib Mesylate
    85+ Cited Publications

    STI571 Mesylate; CGP-57148B Mesylate

    c-Kit Bcr-Abl PDGFR Autophagy Cancer
    Imatinib Mesylate (STI571 Mesylate) is a tyrosine kinases inhibitor that inhibits c-Kit, Bcr-Abl, and PDGFR (IC50=100 nM) tyrosine kinases.
    Imatinib Mesylate
  • HY-B1514R

    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-G0017

    Norimatinib; Imatinib metabolite N-Desmethyl imatinib

    Drug Metabolite Others
    N-Desmethyl imatinib (Norimatinib) is a metabolite of Imatinib (HY-15463). Imatinib is a multi-target inhibitor of v-Abl, c-Kit and PDGFR .
    N-Desmethyl imatinib

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