c-Kit
C-kit is a type of receptor tyrosine kinase and a type of tumor marker, also called CD117 and stem cell factor receptor.
Products for c-Kit
- Cat.No. Product Name Information
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GC18167
AC710
A potent and selective PDGFR family inhibitor
- GC16391 Amuvatinib (MP-470, HPK 56) A multi-targeted RTK inhibitor
- GC33362 Amuvatinib hydrochloride (MP470 hydrochloride) Amuvatinib hydrochloride (MP470 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) (MP470 hydrochloride) is also a DNA repair suppressor through suppression of DNA repair protein RAD51, thereby disrupting DNA damage repair. Antineoplastic activity.
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GC14292
Apatinib Mesylate
Apatinib blocks the downstream signal transduction of VEGF pathway to inhibit neovascularization.
- GC10914 AST 487 A multi-kinase inhibitor
- GC19074 Avapritinib Avapritinib is a potent and selective exon 17 mutant KIT kinase inhibitor with IC50 of 0.27 nM for KIT D816V.
- GC17959 AZD2932 inhibitor of VEGFR-2, PDGFRβ, Flt-3, and c-Kit
- GC33027 AZD3229 An inhibitor of c-Kit-driven cell proliferation
- GC33246 AZD3229 Tosylate AZD3229 Tosylate is a potent pan-KIT mutant inhibitor for the treatment of gastrointestinal stromal tumors.
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GC68727
Barzolvolimab
Barzolvolimab (CDX 0159) is a humanized monoclonal antibody against KIT IgG1. Barzolvolimab specifically and effectively inhibits the activation of KIT. Barzolvolimab can reduce skin mast cells and disease activity in chronic inducible urticaria.
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GC64810
Bezuclastinib
Bezuclastinib (CGT9486; PLX 9486) is a potent inhibitor of c-kit and c-kit D816V (0.0001
- GC19106 c-Kit-IN-1 c-Kit-IN-1 is a potent inhibitor of c-Kit and c-Met with IC50s of <200 nM.
- GC35705 c-Kit-IN-2 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.
- GC38595 c-Kit-IN-3
- GC38756 c-Kit-IN-3 D-tartrate
- GC38757 c-Kit-IN-3 hydrochloride
- GC65948 c-Kit-IN-5-1 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.
- GC15779 Cabozantinib (XL184, BMS-907351) Cabozantinib (XL184, BMS-907351) is a potent and orally active inhibitor of VEGFR2 and MET, with IC50 values of 0.035, and 1.3 nM, respectively. Cabozantinib (XL184, BMS-907351) displays strong inhibition of KIT, RET, AXL, TIE2, and FLT3 (IC50=4.6, 5.2, 7, 14.3, and 11.3 nM, respectively). Cabozantinib (XL184, BMS-907351) shows antiangiogenic activity. Cabozantinib (XL184, BMS-907351) disrupts tumor vasculature and promotes tumor and endothelial cell apoptosis.
- GC62145 Chiauranib Chiauranib (CS2164) is an orally active multi-target inhibitor against tumor angiogenesis. Chiauranib potently inhibits the angiogenesis-related kinases (VEGFR1, VEGFR2, VEGFR3, PDGFRα and c-Kit), mitosis-related kinase Aurora B, and chronic inflammation-related kinase CSF-1R, with IC50 values ranging from 1-9 nM. Chiauranib has strongly anticancer effects.
- GC35682 CHMFL-ABL/KIT-155 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.
- GC35685 CHMFL-KIT-033 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.
- GC25313 CS-2660 (JNJ-38158471) CS-2660 (JNJ-38158471) is a well tolerated, orally available, highly selective VEGFR-2 inhibitor with IC50 of 40 nM. CS-2660 (JNJ-38158471) also inhibits closely related tyrosine kinases such as RET (c-RET) and Kit (c-Kit) with IC50 of 180 nM and 500 nM,while it has no significant activity (>1 microM) against VEGFR-1 and VEGFR-3.
- GC11171 DCC-2618 A dual inhibitor of c-Kit and c-MET
- GC32867 Flumatinib (HHGV678) Flumatinib (HHGV678) (HHGV678) is an orally available, selective inhibitor of Bcr-Abl. Flumatinib (HHGV678) inhibits c-Abl, PDGFRβ and c-Kit with IC50s of 1.2 nM, 307.6 nM and 665.5 nM, respectively.
- GC13914 Flumatinib mesylate PDGRFβ inhibitor
- GC10314 Imatinib (STI571) Imatinib (STI571) (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively. Imatinib (STI571) also is an inhibitor of SARS-CoV and MERS-CoV.
- GC60930 Imatinib D4 Imatinib D4 (STI571 D4) is a deuterium labeled Imatinib (STI571). Imatinib is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity.
- GC39612 Imatinib D8 Imatinib D8 (STI571 D8) is a deuterium labeled Imatinib (STI571). Imatinib is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity.
- GC11759 Imatinib Mesylate (STI571) Imatinib Mesylate (STI571) (STI571 Mesylate) is a tyrosine kinases inhibitor that inhibits c-Kit, Bcr-Abl, and PDGFR (IC50=100 nM) tyrosine kinases.
- GC13961 ISCK03 inhibitor of SCF-mediated c-kit activation
- GC13264 Ki20227 A c-Fms kinase inhibitor
- GC15454 Lenvatinib (E7080) Lenvatinib (E7080) (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities.
- GC36438 Lenvatinib mesylate An inhibitor of VEGFR2 and VEGFR3
- GC17958 Linifanib (ABT-869) Linifanib (ABT-869) (ABT-869) is a potent and orally active multi-target inhibitor of VEGFR and PDGFR family with IC50s of 4, 3, 66, and 4 nM for KDR, FLT1, PDGFRβ, and FLT3, respectively. Linifanib (ABT-869) shows prominent antitumor activity. Linifanib (ABT-869) has much less activity against unrelated RTKs, soluble tyrosine kinases, or serine/threonine kinases. Linifanib (ABT-869) is a specific miR-10b inhibitor that blocks miR-10b biogenesis.
- GC62314 M4205 M4205 is a c-KIT inhibitor, with an IC50 of 10 nM for c-KIT V654A. M4205 has high activity on c-KIT mutations in exon 11, 13, 17.
- GC36546 Masitinib mesylate Masitinib mesylate (AB-1010 mesylate) is a potent, orally bioavailable, and selective inhibitor of c-Kit (IC50=200 nM for human recombinant c-Kit). It also inhibits PDGFRα/β (IC50s=540/800 nM), Lyn (IC50= 510 nM for LynB), Lck, and, to a lesser extent, FGFR3 and FAK. Masitinib mesylate (AB-1010 mesylate) has anti-proliferative, pro-apoptotic activity and low toxicity.
- GC13012 Motesanib
- GC11336 Motesanib Diphosphate (AMG-706) Motesanib Diphosphate (AMG-706) (AMG 706 Diphosphate) is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC50s of 2 nM/3 nM/6 nM, respectively, and has similar activity against Kit, and is approximately 10-fold more selective for VEGFR than PDGFR and Ret.
- GC14957 OSI-930 Inhibitor of Kit, KDR, Flt, CSF-1R, c-Raf and Lck
- GC16327 Pazopanib (GW-786034) A multi-kinase inhibitor
- GC12730 Pazopanib Hydrochloride VEGFR/PDGFR/FGFR/c-Kit/ c-Fms inhibitor
- GC12222 Pexidartinib (PLX3397) Pexidartinib (PLX3397) (PLX-3397) is a potent, orally active, selective, and ATP-competitive colony stimulating factor 1 receptor (CSF1R or M-CSFR) and c-Kit inhibitor, with IC50s of 20 and 10 nM, respectively. Pexidartinib (PLX3397) (PLX-3397) exhibits 10- to 100-fold selectivity for c-Kit and CSF1R over other related kinases. Pexidartinib (PLX3397) (PLX-3397) induces cell apoptosis and has anti-tumor activity.
- GC34708 Pexidartinib hydrochloride Pexidartinib hydrochloride (PLX-3397 hydrochloride) is a potent, orally active, selective, and ATP-competitive colony stimulating factor 1 receptor (CSF1R or M-CSFR) and c-Kit inhibitor, with IC50s of 20 and 10 nM, respectively. Pexidartinib hydrochloride exhibits 10- to 100-fold selectivity for c-Kit and CSF1R over other related kinases. Pexidartinib hydrochloride induces cell apoptosis and has anti-cancer activity.
- GC15075 PLX647 dual inhibitor of FMS and KIT kinases
- GC37538 Ripretinib 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.
- GC19332 Sitravatinib Sitravatinib is a novel small molecule inhibitor targeting multiple RTKs involved in driving sarcoma cell growth with IC50 of 3980 nmol/L.
- GC14733 SU14813 A dual VEGFR and PDGFR family kinase inhibitor
- GC14315 SU14813 maleate A dual VEGFR and PDGFR family kinase inhibitor
- GC15254 Tandutinib (MLN518) Tandutinib (MLN518) (MLN518) is a potent and selective inhibitor of the FLT3 with an IC50 of 0.22 μM, and also inhibits c-Kit and PDGFR with IC50s of 0.17 μM and 0.20 μM, respectively. Tandutinib (MLN518) can be used for acute myelogenous leukemia (AML). Tandutinib (MLN518) has the ability to cross the blood-brain barrier.
- GC38853 Tandutinib hydrochloride Tandutinib hydrochloride (MLN518 hydrochloride) is a potent and selective inhibitor of the FLT3 with an IC50 of 0.22 μM, and also inhibits c-Kit and PDGFR with IC50s of 0.17 μM and 0.20 μM, respectively. Tandutinib hydrochloride can be used for acute myelogenous leukemia (AML). Tandutinib hydrochloride has the ability to cross the blood-brain barrier.
- GC11763 Telatinib (BAY 57-9352) Telatinib (BAY 57-9352) (Bay 57-9352) is an orally active, small molecule inhibitor of VEGFR2, VEGFR3, PDGFα, and c-Kit with IC50s of 6, 4, 15 and 1 nM, respectively.
- GC10719 Toceranib A multi-targeted receptor tyrosine kinase inhibitor
- GC37808 Toceranib phosphate Toceranib phosphate (SU11654 phosphate) is an orally active receptor tyrosine kinase (RTK) inhibitor, and it potently inhibits PDGFR, VEGFR, and Kit with Kis of 5 and 6 nM for PDGFRβ and Flk-1/KDR, respectively. Toceranib phosphate (SU11654 phosphate) has antitumor and antiangiogenic activity, and used in the treatment of canine mast cell tumors .