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Results for "

mutant KIT

" in MedChemExpress (MCE) Product Catalog:

34

Inhibitors & Agonists

2

Isotope-Labeled Compounds

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-101561
    Avapritinib
    10+ Cited Publications

    BLU-285

    		 c-Kit PDGFR Cancer
    Avapritinib (BLU-285) is a highly potent, selective, and orally active KIT and PDGFRA activation loop mutant kinases inhibitor with IC50s of 0.27 and 0.24 nM for KIT D816V and PDGFRA D842V, respectively. Avapritinib (BLU-285) binds the active conformation of the kinase and shows antitumor activity. Avapritinib (BLU-285) attenuates the transport function of both ABCB1 and ABCG2 .
    Avapritinib
  • 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-112306
    Ripretinib
    5+ Cited Publications

    DCC-2618

    		 c-Kit PDGFR FLT3 VEGFR Apoptosis Cancer
    Ripretinib (DCC-2618) is an orally bioavailable, selective KIT and PDGFRA switch-control inhibitor. Ripretinib (DCC-2618) targets and binds to both wild-type and mutant forms of KIT and PDGFRA specifically at their switch pocket binding sites, thereby preventing the switch from inactive to active conformations of these kinases and inactivating their wild-type and mutant forms. Ripretinib (DCC-2618) also inhibits multiple other kinase targets, such as FLT3 and KDR (or VEGFR-2) . DCC-2618 exerts antineoplastic effect and induces apoptosis .
    Ripretinib
  • HY-10206
    Amuvatinib
    5+ Cited Publications

    MP470; HPK 56

    		 c-Kit PDGFR RAD51 FLT3 c-Met/HGFR RET Apoptosis Cancer
    Amuvatinib (MP470) is an orally bioavailable multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Kit, PDGFRα, Flt3, c-Met and c-Ret. Amuvatinib (MP470) is also a DNA repair suppressor through suppression of DNA repair protein RAD51, thereby disrupting DNA damage repair . Antineoplastic activity .
    Amuvatinib
  • HY-112802
    AZD3229

    		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-14217
    Quizartinib dihydrochloride
    Maximum Cited Publications
    45 Publications Verification

    AC220 dihydrochloride

    		 FLT3 Apoptosis PDGFR c-Kit Cancer
    Quizartinib (AC220) dihydrochloride is an orally active, potent and selective FLT3 inhibitor. Quizartinib dihydrochloride inhibits kinase activity of mutant-FLT3, -PDGFRA and -KIT isoforms and inhibits autophosphorylation. Quizartinib dihydrochloride inhibits cellular proliferation, induces apoptosis in cancer cells. Quizartinib dihydrochloride can be used for the research of cancer .
    Quizartinib dihydrochloride
  • HY-15814
    HG-7-85-01

    		Bcr-Abl PDGFR c-Kit Src JAK Apoptosis Cancer
    HG-7-85-01 is a type II ATP competitive inhibitor of wild-type and gatekeeper mutations forms of Bcr-Abl, PDGFRα, Kit, and Src kinases. HG-7-85-01 inhibits T315I mutant Bcr-Abl kinase, KDR and RET with IC50s of 3 nM, 20 nM and 30 nM, and is only weak or no inhibition of other kinases (IC50>2 μM). HG-7-85-01 inhibits the cell proliferation, which is mediated by the induction of apoptosis, and inhibition of cell-cycle progression .
    HG-7-85-01
  • HY-10206A
    Amuvatinib hydrochloride

    MP470 hydrochloride; HPK 56 hydrochloride

    		 c-Kit PDGFR RAD51 FLT3 c-Met/HGFR RET Cancer
    Amuvatinib hydrochloride (MP470 hydrochloride) is an orally bioavailable multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Kit, PDGFRα, Flt3, c-Met and c-Ret. Amuvatinib hydrochloride (MP470 hydrochloride) is also a DNA repair suppressor through suppression of DNA repair protein RAD51, thereby disrupting DNA damage repair . Antineoplastic activity .
    Amuvatinib hydrochloride
  • HY-122849
    CHMFL-KIT-031

    		c-Kit Cancer
    CHMFL-KIT-031 is a highly selective KIT V559D inhibitor, with an IC50 of 28 nM. CHMFL-KIT-031 potently affects KIT V559D mutant’s phosphorylation at Y703/719/823 sites. CHMFL-KIT-031 inhibits the tumor growth in BaF3-TEL-KIT-V559D cell inoculated mouse model .
    CHMFL-KIT-031
  • HY-128589
    CHMFL-KIT-033

    		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-10638
    AP23464

    		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-170911
    KIT/PDGFRA-IN-1

    		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-112306R
    Ripretinib (Standard)

    DCC-2618 (Standard)

    		 c-Kit PDGFR FLT3 VEGFR Apoptosis Reference Standards Cancer
    Ripretinib (Standard) is the analytical standard of Ripretinib. This product is intended for research and analytical applications. Ripretinib (DCC-2618) is an orally bioavailable, selective KIT and PDGFRA switch-control inhibitor. Ripretinib (DCC-2618) targets and binds to both wild-type and mutant forms of KIT and PDGFRA specifically at their switch pocket binding sites, thereby preventing the switch from inactive to active conformations of these kinases and inactivating their wild-type and mutant forms. Ripretinib (DCC-2618) also inhibits multiple other kinase targets, such as FLT3 and KDR (or VEGFR-2) . DCC-2618 exerts antineoplastic effect and induces apoptosis .
    Ripretinib (Standard)
  • HY-101561R
    Avapritinib (Standard)

    BLU-285 (Standard)

    		 Reference Standards c-Kit PDGFR Cancer
    Avapritinib (Standard) is the analytical standard of Avapritinib. This product is intended for research and analytical applications. Avapritinib (BLU-285) is a highly potent, selective, and orally active KIT and PDGFRA activation loop mutant kinases inhibitor with IC50s of 0.27 and 0.24 nM for KIT D816V and PDGFRA D842V, respectively. Avapritinib (BLU-285) binds the active conformation of the kinase and shows antitumor activity. Avapritinib (BLU-285) attenuates the transport function of both ABCB1 and ABCG2 .
    Avapritinib (Standard)
  • HY-W754911
    Avapritinib-d3

    BLU-285-d3

    		 Isotope-Labeled Compounds PDGFR c-Kit Cancer
    Avapritinib-d3 (BLU-285-d3) is deuterium labeled Avapritinib. Avapritinib (BLU-285) is a highly potent, selective, and orally active KIT and PDGFRA activation loop mutant kinases inhibitor with IC50s of 0.27 and 0.24 nM for KIT D816V and PDGFRA D842V, respectively. Avapritinib (BLU-285) binds the active conformation of the kinase and shows antitumor activity. Avapritinib (BLU-285) attenuates the transport function of both ABCB1 and ABCG2 .
    Avapritinib-d3
  • HY-13001R
    Quizartinib (Standard)

    AC220 (Standard)

    		 Reference Standards FLT3 Apoptosis PDGFR c-Kit Cancer
    Quizartinib (AC220) (Standard) is the analytical standard of Quizartinib (HY-13001). This product is intended for research and analytical applications. Quizartinib 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 (Standard)
  • HY-10206R
    Amuvatinib (Standard)

    MP470 (Standard); HPK 56 (Standard)

    		 Reference Standards c-Kit PDGFR RAD51 FLT3 c-Met/HGFR RET Apoptosis Cancer
    Amuvatinib (Standard) is the analytical standard of Amuvatinib. This product is intended for research and analytical applications. Amuvatinib (MP470) is an orally bioavailable multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Kit, PDGFRα, Flt3, c-Met and c-Ret. Amuvatinib (MP470) is also a DNA repair suppressor through suppression of DNA repair protein RAD51, thereby disrupting DNA damage repair . Antineoplastic activity .
    Amuvatinib (Standard)
  • HY-121708
    KI-328

    		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-112802A
    Ubavitinib tosylate

    AZD3229 tosylate

    		 c-Kit Cancer
    AZD3229 Tosylate is a potent pan-KIT mutant inhibitor for the treatment of gastrointestinal stromal tumors.
    Ubavitinib tosylate
  • HY-168580
    c-Kit-IN-7

    		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-168579
    c-Kit-IN-6

    		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-IN-8

    		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-E70742
    KIT V654A Recombinant Human Active Protein Kinase

    		c-Kit Cancer
    KIT (CD117) is an important cell surface marker used to identify certain types of hematopoietic(blood) progenitors in the bone marrow. KIT is a cytokine receptor expressed on the surface of hematopoietic stem cells as well as other cell types. Altered forms of this receptor may be associated with some types of cancer. KIT V654A is a mutant of KIT. KIT V654A Recombinant Human Active Protein Kinase is a recombinant KIT V654A protein that can be used to study KIT V654A-related functions .
    KIT V654A Recombinant Human Active Protein Kinase
  • HY-E70737
    KIT T670I Recombinant Human Active Protein Kinase

    		c-Kit Cancer
    KIT (CD117) is an important cell surface marker used to identify certain types of hematopoietic(blood) progenitors in the bone marrow. KIT is a cytokine receptor expressed on the surface of hematopoietic stem cells as well as other cell types. Altered forms of this receptor may be associated with some types of cancer. KIT T670I is a mutant of KIT. KIT T670I Recombinant Human Active Protein Kinase is a recombinant KIT T670I protein that can be used to study KIT T670I-related functions .
    KIT T670I Recombinant Human Active Protein Kinase
  • HY-E70738
    KIT V559D Recombinant Human Active Protein Kinase

    		c-Kit Cancer
    KIT (CD117) is an important cell surface marker used to identify certain types of hematopoietic(blood) progenitors in the bone marrow. KIT is a cytokine receptor expressed on the surface of hematopoietic stem cells as well as other cell types. Altered forms of this receptor may be associated with some types of cancer. KIT V559D is a mutant of KIT. KIT V559D Recombinant Human Active Protein Kinase is a recombinant KIT V559D protein that can be used to study KIT V559D-related functions .
    KIT V559D Recombinant Human Active Protein Kinase
  • HY-E70741
    KIT V560G Recombinant Human Active Protein Kinase

    		c-Kit Cancer
    KIT (CD117) is an important cell surface marker used to identify certain types of hematopoietic(blood) progenitors in the bone marrow. KIT is a cytokine receptor expressed on the surface of hematopoietic stem cells as well as other cell types. Altered forms of this receptor may be associated with some types of cancer. KIT V560G is a mutant of KIT. KIT V560G Recombinant Human Active Protein Kinase is a recombinant KIT V560G protein that can be used to study KIT V560G-related functions .
    KIT V560G Recombinant Human Active Protein Kinase
  • HY-E70736
    KIT D816V Recombinant Human Active Protein Kinase

    		c-Kit Cancer
    KIT (CD117) is an important cell surface marker used to identify certain types of hematopoietic(blood) progenitors in the bone marrow. KIT is a cytokine receptor expressed on the surface of hematopoietic stem cells as well as other cell types. Altered forms of this receptor may be associated with some types of cancer. KIT D816V is a mutant of KIT. KIT D816V Recombinant Human Active Protein Kinase is a recombinant KIT D816V protein that can be used to study KIT D816V-related functions .
    KIT D816V Recombinant Human Active Protein Kinase
  • HY-E70735
    KIT D816H Recombinant Human Active Protein Kinase

    		c-Kit Cancer
    KIT (CD117) is an important cell surface marker used to identify certain types of hematopoietic(blood) progenitors in the bone marrow. KIT is a cytokine receptor expressed on the surface of hematopoietic stem cells as well as other cell types. Altered forms of this receptor may be associated with some types of cancer. KIT D816H is a mutant of KIT. KIT D816H Recombinant Human Active Protein Kinase is a recombinant KIT D816H protein that can be used to study KIT D816H-related functions .
    KIT D816H Recombinant Human Active Protein Kinase
  • HY-E70734
    KIT A829P Recombinant Human Active Protein Kinase

    		c-Kit Cancer
    KIT (CD117) is an important cell surface marker used to identify certain types of hematopoietic(blood) progenitors in the bone marrow. KIT is a cytokine receptor expressed on the surface of hematopoietic stem cells as well as other cell types. Altered forms of this receptor may be associated with some types of cancer. KIT A829P is a mutant of KIT. KIT A829P Recombinant Human Active Protein Kinase is a recombinant KIT A829P protein that can be used to study KIT A829P-related functions .
    KIT A829P Recombinant Human Active Protein Kinase
  • HY-E70740
    KIT V559D/V654A Recombinant Human Active Protein Kinase

    		c-Kit Cancer
    KIT (CD117) is an important cell surface marker used to identify certain types of hematopoietic(blood) progenitors in the bone marrow. KIT is a cytokine receptor expressed on the surface of hematopoietic stem cells as well as other cell types. Altered forms of this receptor may be associated with some types of cancer. KIT V559D/V654A is a mutant of KIT. KIT V559D/V654A Recombinant Human Active Protein Kinase is a recombinant KIT V559D/V654A protein that can be used to study KIT V559D/V654A-related functions .
    KIT V559D/V654A Recombinant Human Active Protein Kinase
  • HY-E70739
    KIT V559D/T670I Recombinant Human Active Protein Kinase

    		c-Kit Cancer
    KIT (CD117) is an important cell surface marker used to identify certain types of hematopoietic(blood) progenitors in the bone marrow. KIT is a cytokine receptor expressed on the surface of hematopoietic stem cells as well as other cell types. Altered forms of this receptor may be associated with some types of cancer. KIT V559D/T670I is a mutant of KIT. KIT V559D/T670I Recombinant Human Active Protein Kinase is a recombinant KIT V559D/T670I protein that can be used to study KIT V559D/T670I-related functions .
    KIT V559D/T670I Recombinant Human Active Protein Kinase
  • HY-13001S
    Quizartinib-d8

    AC220-d8

    		 Isotope-Labeled Compounds Apoptosis FLT3 PDGFR c-Kit Cancer
    Quizartinib (AC220)-d8 is deuterium labeled Quizartinib (HY-13001). Quizartinib 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-d8
  • HY-179563
    c-Kit-IN-12

    		c-Kit Cancer
    C-Kit-IN-12 (Compound 2a) is a potent c-Kit inhibitor, with its IC50 value for c-Kit being less than 10 nM in four KIT mutant cell models (BAF3 KIT EX11 DEL, EX11 DEL/D816H, EX11 DEL/T670I, EX11 DEL/V654A). C-Kit-IN-12 can be used for studying diseases or disorders related to c-Kit, such as cancer .
    c-Kit-IN-12
  • HY-179563A
    (S)-c-Kit-IN-12

    		c-Kit Cancer
    (S)-c-Kit-IN-12 (Compound 2b) is a potent c-Kit inhibitor, with its IC50 value for c-Kit being less than 10 nM in four KIT mutant cell models (BAF3 KIT EX11 DEL, EX11 DEL/D816H, EX11 DEL/T670I, EX11 DEL/V654A). (S)-c-Kit-IN-12 can be used for studying diseases or disorders related to c-Kit, such as cancer .
    (S)-c-Kit-IN-12

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