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c-Met
c-Met製品
- All (56)
- c-Met阻害剤 (45)
- c-Met抗体(7)
- 新製品
| 製品コード | 製品名称 | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
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| S1068 | Crizotinib | Crizotinib is a potent inhibitor of c-Met and ALK with IC50 of 11 nM and 24 nM in cell-based assays, respectively. It is also a potent ROS1 inhibitor with Ki value less than 0.025 nM. Crizotinib induces autophagy through inhibition of the STAT3 pathway in multiple lung cancer cell lines. |
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| S1119 | Cabozantinib (XL184) | カボザンチニブ (Cabozantinib (XL184, BMS-907351)) は強力な VEGFR2 阻害剤であり、IC50 は 0.035 nM です。また c-Met, Ret, Kit, Flt-1/3/4, Tie2 および AXL に対しても阻害活性があり、cell-free assay における IC50 はそれぞれ 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM, 7 nM です。カボザンチニブは大腸がん細胞において AKT/GSK-3β/NF-κB 経路を介して PUMA 依存性アポトーシス (PUMA-dependent apoptosis) を誘発します。 |
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| S1112 | SGX-523 | SGX-523 is a selective Met (c-Met) inhibitor with IC50 of 4 nM, no activity to BRAFV599E, c-Raf, Abl and p38α. Phase 1. |
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| S4001 | Cabozantinib malate | Cabozantinib malate (XL184) is the malate of Cabozantinib, a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret (c-Ret), Kit (c-Kit), Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM in cell-free assays, respectively. Cabozantinib malate (XL184) induces apoptosis. |
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| S1111 | Foretinib | Foretinib is an ATP-competitive inhibitor of HGFR and VEGFR, mostly for Met (c-Met) and KDR with IC50 of 0.4 nM and 0.9 nM in cell-free assays. Less potent against Ron, Flt-1/3/4, Kit (c-Kit), PDGFRα/β and Tie-2, and little activity to FGFR1 and EGFR. Phase 2. |
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| S1070 | PHA-665752 | PHA-665752 is a potent, selective and ATP-competitive c-Met inhibitor with IC50 of 9 nM in cell-free assays, >50-fold selectivity for c-Met than RTKs or STKs. |
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| S2788 | Capmatinib | Capmatinib is a novel, ATP-competitive inhibitor of c-MET with IC50 of 0.13 nM in a cell-free assay, inactive against RONβ, as well as EGFR and HER-3. Capmatinib (INCB28060) inhibits Wnt/β-catenin and EMT signaling pathways and induces apoptosis in diffuse gastric cancer positive for c-MET amplification. Phase 1. |
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| S5190 | Crizotinib hydrochloride | Crizotinib (PF-02341066) hydrochloride (Xalkori) inhibits tyrosine phosphorylation of c-Met and nucleophosmin (NPM)-anaplastic lymphoma kinase (ALK) with IC50 of of 11 nM and 24 nM in cell-based assays, respectively. Crizotinib hydrochloride is also a potent ROS1 inhibitor with Ki less than 0.025 nM. Crizotinib induces autophagy through inhibition of the STAT3 pathway in multiple lung cancer cell lines. | ||
| S1080 | SU11274 | SU11274 (PKI-SU11274) is a selective Met (c-Met) inhibitor with IC50 of 10 nM in cell-free assays, no effects on PGDFRβ, EGFR or Tie2. SU11274 induces autophagy, apoptosis and cell cycle arrest. |
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| S1561 | BMS-777607 | BMS-777607 (BMS 817378) is a Met-related inhibitor for c-Met, Axl, Ron and Tyro3 with IC50 of 3.9 nM, 1.1 nM, 1.8 nM and 4.3 nM in cell-free assays, 40-fold more selective for Met-related targets versus Lck, VEGFR-2, and TrkA/B, and more than 500-fold greater selectivity versus all other receptor and non receptor kinases. |
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| S1114 | JNJ-38877605 | JNJ-38877605 is an ATP-competitive inhibitor of c-Met with IC50 of 4 nM, 600-fold selective for c-Met than 200 other tyrosine and serine-threonine kinases. Phase 1. |
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| S1124 | BMS-754807 | BMS-754807 is a potent and reversible inhibitor of IGF-1R/InsR with IC50 of 1.8 nM/1.7 nM in cell-free assays, less potent to Met (c-Met), Aurora A/B, TrkA/B and Ron, and shows little activity to Flt3, Lck, MK2, PKA, PKC etc. Phase 2. |
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| S2753 | Tivantinib | Tivantinib is the first non-ATP-competitive c-Met inhibitor with Ki of 0.355 μM in a cell-free assay, little activity to Ron, and no inhibition to EGFR, InsR, PDGFRα or FGFR1/4. Tivantinib (ARQ 197) induces a G2/M arrest and apoptosis. |
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| S1094 | PF-04217903 | PF-04217903 is a selective ATP-competitive c-Met inhibitor with IC50 of 4.8 nM in A549 cell line, susceptible to oncogenic mutations (no activity to Y1230C mutant). Phase 1. |
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| S1244 | Amuvatinib (MP-470) | Amuvatinib (MP-470, HPK 56) is a potent and multi-targeted inhibitor of c-Kit, PDGFRα and Flt3 with IC50 of 10 nM, 40 nM and 81 nM, respectively. Amuvatinib suppresses c-MET and c-RET. Amuvatinib is also active as a DNA repair protein Rad51 inhibitor with antineoplastic activity. Phase 2. |
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| S7674 | Savolitinib (AZD6094) | Savolitinib (Volitinib, AZD6094, HMPL-504) is a novel, potent, and selective MET inhibitor currently in clinical development in various indications, including PRCC. The IC50 values of this compound for c-Met and p-Met are 5 nM and 3 nM, respectively. It shows exquisite selectivity for c-Met over 274 kinase. | ||
| S1361 | MGCD-265 analog | MGCD-265 is a potent, multi-target and ATP-competitive inhibitor of c-Met and VEGFR1/2/3 with IC50 of 1 nM, 3 nM/3 nM/4 nM, respectively; also inhibits Ron and Tie2. Phase 1/2. |
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| S2859 | Golvatinib (E7050) | Golvatinib (E7050) is a dual c-Met and VEGFR-2 inhibitor with IC50 of 14 nM and 16 nM, does not inhibit bFGF-stimulated HUVEC growth (up to 1000 nM). Phase 1/2. |
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| S7014 | Merestinib (LY2801653) | Merestinib (LY2801653) is a type-II ATP competitive, slow-off inhibitor of Met (c-Met) tyrosine kinase with a dissociation constant (Ki) of 2 nM, a pharmacodynamic residence time (Koff) of 0.00132 min(-1) and t1/2 of 525 min. Merestinib (LY2801653) also inhibits MST1R, AXL, ROS1, MKNK1/2, FLT3, MERTK, DDR1 and DDR2 with IC50 of 11 nM, 2 nM, 23 nM, 7 nM, 7 nM, 10 nM, 0.1 nM and 7 nM, respectively. | ||
| S9662 | UNC2025 | UNC2025 is a potent and orally active dual inhibitor of FLT3 and MER with IC50 of 0.35 nM and 0.46 nM, respectively. UNC2025 also inhibits AXL, TRKA, TRKC, QIK, TYRO3, SLK, NuaK1, Kit (c-Kit) and Met (c-Met) with IC50 of 1.65 nM, 1.67 nM, 4.38 nM, 5.75 nM, 5.83 nM, 6.14 nM, 7.97 nM, 8.18 nM and 364 nM, respectively. | ||
| S8570 | CEP-40783 (RXDX-106) | CEP-40783 (RXDX-106) is an orally-available, potent and selective TAM(TYRO3, AXL, MER)/Met (c-Met) inhibitor displaying low nanomolar biochemical activity and slow (T1/2 >120 min) inhibitor off-rate in peptide phosphorylation assays and in vitro kinase binding assays, respectively. | ||
| S2774 | MK-2461 | MK-2461 is a potent, multi-targeted inhibitor for c-Met(WT/mutants) with IC50 of 0.4-2.5 nM, less potent to Ron, Flt1; 8- to 30-fold greater selectivity of c-Met targets versus FGFR1, FGFR2, FGFR3, PDGFRβ, KDR, Flt3, Flt4, TrkA, and TrkB. Phase 1/2. . |
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| S7669 | NPS-1034 | NPS-1034 is a dual Met (c-Met)/Axl inhibitor with IC50 of 48 nM and 10.3 nM, respectively. | ||
| S8167 | AMG 337 | AMG 337 is an oral, small molecule, ATP-competitive, highly selective inhibitor of the Met (c-Met) receptor with an IC50 of 1 nM. | ||
| S3759 | Norcantharidin | Norcantharidin (Endothall anhydride) is a synthetic anticancer compound which is a dual inhibitor for c-Met and EGFR in human colon cancers. | ||
| S6412 | Altiratinib | Altiratinib (DCC-2701) is a potent single-digit nanomolar inhibitor of TRK, Met (c-Met), TIE2, and VEGFR2 kinases with IC50 vaules of 0.9 nM, 4.6 nM, and 0.8 nM for TRKA, B, and C, respectively. It inhibits Met (c-Met) and Met (c-Met) mutant with IC50 values in the range of 0.3-6 nM. | ||
| S5115 | Sodium L-ascorbyl-2-phosphate | Sodium L-ascorbyl-2-phosphate (Sodium ascorbyl monophosphate, Sodium ascorbyl phosphate, SAP) is specifically produced for use as a stabilized source of vitamin C in cosmetic products. It is used in skin care recipes for UV protection, collagen production, as an antioxidant and for its skin lightening and brightening effects. | ||
| S2201 | BMS-794833 | BMS-794833 is a potent ATP competitive inhibitor of Met (c-Met)/VEGFR2 with IC50 of 1.7 nM/15 nM, also inhibits Ron, Axl and Flt3 with IC50 of <3 nM; a prodrug of BMS-817378. Phase 1. | ||
| S2761 | NVP-BVU972 | NVP-BVU972 is a selective and potent Met (c-Met) inhibitor with IC50 of 14 nM. | ||
| S8404 | S49076 | S49076 is a novel, potent inhibitor of Met (c-Met), AXL/MER, and FGFR1/2/3 with IC50 values below 20 nmol/L. | ||
| S1316 | AMG-208 | AMG 208 is a highly selective dual c-Met and RON inhibitor with IC50 of 9 nM for c-Met. | ||
| S2747 | AMG-458 | AMG 458 is a potent c-Met inhibitor with Ki of 1.2 nM, ~350-fold selectivity for c-Met than VEGFR2 in cells. | ||
| S6899 | Licochalcone D | Licochalcone D (Lico D, LCD, LD), a flavonoid isolated from a Chinese medicinal plant Glycyrrhiza inflata, has antioxidant, anti-inflammatory and anti-cancer properties. Licochalcone D inhibit phosphorylation of NF-κB p65 in LPS signaling pathway. Licochalcone D inhibits JAK2, EGFR and Met (c-Met) activities and induces ROS-dependent apoptosis. Licochalcone D also induces caspases activation and poly (ADP-ribose) polymerase (PARP) cleavage. | ||
| E4606New | Dihexa | Dihexa(PNB-0408), an oligopeptide drug, is an orally active and blood-brain barrier-permeable analog of angiotensin IV. It binds to hepatocyte growth factor (HGF) with high affinity and potentiates its activity at its receptor, c-Met. Dihexa can also be used as a therapeutic potential in the treatment of Alzheimer’s disease. | ||
| S0540 | BAY-474 | BAY-474 is an inhibitor of tyrosine-protein kinase c-Met and can act as an epigenetics probe. | ||
| S8854 | JNJ-38877618(OMO-1) | JNJ-38877618 (OMO-1) is a potent, highly selective, orally bioavailable Met (c-Met) kinase inhibitor with binding affinity (Kd) of 1.4 nM and enzyme inhibitory activity against wt and M1268T mutant Met (c-Met) (2 and 3 nM IC50). | ||
| S9620 | Elzovantinib (TPX-0022) | Elzovantinib (TPX-0022, CSF1R-IN-2) is a potent inhibitor of MET/CSF1R/SRC with enzymatic kinase inhibition IC50s of 0.14 nM, 0.71 nM and 0.12 nM, respectively. TPX-0022 modulates the tumor immune microenvironment in preclinical models. | ||
| A2467 | Telisotuzumab (Anti-HGFR / c-Met) | Telisotuzumab (Anti-HGFR / c-Met) is a monoclonal antibody that targets c-Met. MW: 145.64 KD. | ||
| A2468 | Onartuzumab (Anti-HGFR / c-Met) | Onartuzumab (Anti-HGFR / c-Met) is a unique, humanized and affinity-matured monovalent (one-armed) monoclonal antibody against the MET receptor. Onartuzumab potently inhibits HGF binding and receptor phosphorylation and signaling. Onartuzumab has antibody-like pharmacokinetics and antitumor activity. MW: 144.64 KD. | ||
| A2469 | Rilotumumab (Anti-HGF / SF) | Rilotumumab (Anti-HGF / SF) is a monoclonal antibody that inhibits HGF/MET-driven signaling. Rilotumumab shows anti-tumor activity, and can be used in castration-resistant prostate cancer (CRPC) and solid tumor research. MW: 145.5 KD. | ||
| A2661 | Ficlatuzumab (Anti-HGF / SF) | Ficlatuzumab (Anti-HGF / SF) is a monoclonal antibody (McAb) targeting human hepatocyte growth factor (HGF). It inhibits c-Met receptor-mediated cancer cell proliferation, migration, and invasion and can be used to treat head and neck squamous cell carcinoma (HNSCC). MW :150 KD. | ||
| A2662 | Emibetuzumab (Anti-HGFR / c-Met) | Emibetuzumab (Anti-HGFR / c-Met) is a humanized bivalent MET antibody targeting both HGF-dependent and HGF-independent MET pathway activation and tumor growth. It can be used in study of cancer. MW :144.56 KD. | ||
| S9308 | Pulsatilla saponin D | Pulsatilla saponin D (SB365), isolated from the root of Pulsatilla koreana, targets c-Met and exerts antiangiogenic and antitumor activities. | ||
| S6870 | Ningetinib | Ningetinib (CT-053, DE-120, CT053PTSA) is a potent, orally bioavailable inhibitor of tyrosine kinase with IC50 of 6.7 nM, 1.9 nM and <1.0 nM for c-Met, VEGFR2 and Axl, respectively. Ningetinib exhibits antitumor activity. | ||
| S0361 | AMG-1 | AMG-1 (c-Met/RON Dual Kinase Inhibitor, RON-IN-1) is a potent inhibitor of human c-Met and RON with IC50 of 4 nM and 9 nM, respectively. | ||
| A2930 | Anti-HGF / SF (TAK-701) | Anti-HGF / SF (TAK-701) is a humanized monoclonal antibody directed against human hepatocyte growth factor (HGF) with potential antineoplastic activity. It reverses gefitinib resistance in non-small-cell lung cancer. MW: 145.04 KD. | ||
| A2932 | Anti-HGFR / c-Met (SAIT301) | Anti-HGFR / c-Met (SAIT301) is a humanized monoclonal antibody targeting the alpha chain of the extracellular domain of the human hepatocyte growth factor receptor (HGFR or c-Met) with potential antineoplastic activity. MW: 146.0 KD. | ||
| S6762 | Bozitinib | Bozitinib is a highly selective ATP-competitive c-Met inhibitor with blood-brain barrier permeability. Bozitinib (PLB-1001) selectively inhibits MET-altered tumor cells in preclinical models. | ||
| S6764 | Pamufetinib (TAS-115) | Pamufetinib (TAS-115) is a highly potent c-Met and VEGFR dual inhibitor with IC50s of 30 nM and 32 nM for recombinant VEGFR2 and recombinant MET, respectively. | ||
| E2655 | Terevalefim | Terevalefim (ANG-3777), a small molecule hepatocyte growth factor (HGF) mimetic, induces c-MET dimerization and phosphorylation, reducing apoptosis and increasing cellular proliferation. | ||
| S7564 | SAR125844 | SAR125844 is a potent intravenously active and highly selective Met (c-Met) kinase inhibitor, displaying nanomolar activity against the wild-type kinase (IC50 value of 4.2 nmol/L) and H1094Y, Y1235D, M1250T, L1195V, and D1228H kinase domain mutants (IC50 values of 0.22, 1.7, 6.5, 65, and 81 nmol/L, respectively). | ||
| E4914New | Cabozantinib hydrochloride | Cabozantinib hydrochloride(XL184, BMS-907351 hydrochloride) is a potent small-molecule kinase inhibitor of c-MET and VEGFR2 with an IC50 of 1.3 nM, 0.035 nM respectively. It also inhibits RET, KIT, AXL, Tie2 and FLT3 with an IC50's of 5.2 nM, 4.6 nM, 7 nM, 14.3 nM, 11.3nM respectively. It can be promising agent for inhibiting tumor angiogenesis and metastasis in cancers with dysregulated MET and VEGFR signaling. | ||
| E1340New | Glesatinib | Glesatinib(MGCD265) is an orally bioavailable potent dual inhibitor of c-MET and SMO. Glesatinib counteracts P-glycoprotein (P-gp) mediated multidrug resistance (MDR) in non-small cell lung cancer (NSCLC). | ||
| S8676 | Glumetinib | Glumetinib is a potent and highly selective c-Met inhibitor with an IC50 of 0.42 ± 0.02 nmol/L. Glumetinib has greater than 2,400-fold selectivity for c-Met over those 312 kinases evaluated, including the c-Met family member RON and highly homologous kinases Axl, Mer, and TyrO3. | ||
| D4046 | Telisotuzumab vedotin | Telisotuzumab vedotin (Teliso-V, ABBV-399) is an antibody-drug conjugate (ADC) composed of the anti–c-Met humanized monoclonal antibody coupled to the cytotoxic monomethyl auristatin E (MMAE) through a mc-val-cit-PABC type linker. Telisotuzumab vedotin can be used for research on advanced solid tumours. | ||
| E0142 | XL092 | XL092 (JUN04542) is an ATP-competitive inhibitor of multiple RTKs including MET, VEGFR2, AXL and MER, with IC50 values of 15 nM, 1.6 nM, 3.4 nM, and 7.2 nM in cell-based assays, respectively. | ||
| S1068 | Crizotinib | Crizotinib is a potent inhibitor of c-Met and ALK with IC50 of 11 nM and 24 nM in cell-based assays, respectively. It is also a potent ROS1 inhibitor with Ki value less than 0.025 nM. Crizotinib induces autophagy through inhibition of the STAT3 pathway in multiple lung cancer cell lines. |
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| S1119 | Cabozantinib (XL184) | カボザンチニブ (Cabozantinib (XL184, BMS-907351)) は強力な VEGFR2 阻害剤であり、IC50 は 0.035 nM です。また c-Met, Ret, Kit, Flt-1/3/4, Tie2 および AXL に対しても阻害活性があり、cell-free assay における IC50 はそれぞれ 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM, 7 nM です。カボザンチニブは大腸がん細胞において AKT/GSK-3β/NF-κB 経路を介して PUMA 依存性アポトーシス (PUMA-dependent apoptosis) を誘発します。 |
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| S1112 | SGX-523 | SGX-523 is a selective Met (c-Met) inhibitor with IC50 of 4 nM, no activity to BRAFV599E, c-Raf, Abl and p38α. Phase 1. |
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| S4001 | Cabozantinib malate | Cabozantinib malate (XL184) is the malate of Cabozantinib, a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret (c-Ret), Kit (c-Kit), Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM in cell-free assays, respectively. Cabozantinib malate (XL184) induces apoptosis. |
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| S1111 | Foretinib | Foretinib is an ATP-competitive inhibitor of HGFR and VEGFR, mostly for Met (c-Met) and KDR with IC50 of 0.4 nM and 0.9 nM in cell-free assays. Less potent against Ron, Flt-1/3/4, Kit (c-Kit), PDGFRα/β and Tie-2, and little activity to FGFR1 and EGFR. Phase 2. |
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| S1070 | PHA-665752 | PHA-665752 is a potent, selective and ATP-competitive c-Met inhibitor with IC50 of 9 nM in cell-free assays, >50-fold selectivity for c-Met than RTKs or STKs. |
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| S2788 | Capmatinib | Capmatinib is a novel, ATP-competitive inhibitor of c-MET with IC50 of 0.13 nM in a cell-free assay, inactive against RONβ, as well as EGFR and HER-3. Capmatinib (INCB28060) inhibits Wnt/β-catenin and EMT signaling pathways and induces apoptosis in diffuse gastric cancer positive for c-MET amplification. Phase 1. |
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| S5190 | Crizotinib hydrochloride | Crizotinib (PF-02341066) hydrochloride (Xalkori) inhibits tyrosine phosphorylation of c-Met and nucleophosmin (NPM)-anaplastic lymphoma kinase (ALK) with IC50 of of 11 nM and 24 nM in cell-based assays, respectively. Crizotinib hydrochloride is also a potent ROS1 inhibitor with Ki less than 0.025 nM. Crizotinib induces autophagy through inhibition of the STAT3 pathway in multiple lung cancer cell lines. | ||
| S1080 | SU11274 | SU11274 (PKI-SU11274) is a selective Met (c-Met) inhibitor with IC50 of 10 nM in cell-free assays, no effects on PGDFRβ, EGFR or Tie2. SU11274 induces autophagy, apoptosis and cell cycle arrest. |
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| S1561 | BMS-777607 | BMS-777607 (BMS 817378) is a Met-related inhibitor for c-Met, Axl, Ron and Tyro3 with IC50 of 3.9 nM, 1.1 nM, 1.8 nM and 4.3 nM in cell-free assays, 40-fold more selective for Met-related targets versus Lck, VEGFR-2, and TrkA/B, and more than 500-fold greater selectivity versus all other receptor and non receptor kinases. |
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| S1114 | JNJ-38877605 | JNJ-38877605 is an ATP-competitive inhibitor of c-Met with IC50 of 4 nM, 600-fold selective for c-Met than 200 other tyrosine and serine-threonine kinases. Phase 1. |
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| S1124 | BMS-754807 | BMS-754807 is a potent and reversible inhibitor of IGF-1R/InsR with IC50 of 1.8 nM/1.7 nM in cell-free assays, less potent to Met (c-Met), Aurora A/B, TrkA/B and Ron, and shows little activity to Flt3, Lck, MK2, PKA, PKC etc. Phase 2. |
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| S2753 | Tivantinib | Tivantinib is the first non-ATP-competitive c-Met inhibitor with Ki of 0.355 μM in a cell-free assay, little activity to Ron, and no inhibition to EGFR, InsR, PDGFRα or FGFR1/4. Tivantinib (ARQ 197) induces a G2/M arrest and apoptosis. |
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| S1094 | PF-04217903 | PF-04217903 is a selective ATP-competitive c-Met inhibitor with IC50 of 4.8 nM in A549 cell line, susceptible to oncogenic mutations (no activity to Y1230C mutant). Phase 1. |
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| S1244 | Amuvatinib (MP-470) | Amuvatinib (MP-470, HPK 56) is a potent and multi-targeted inhibitor of c-Kit, PDGFRα and Flt3 with IC50 of 10 nM, 40 nM and 81 nM, respectively. Amuvatinib suppresses c-MET and c-RET. Amuvatinib is also active as a DNA repair protein Rad51 inhibitor with antineoplastic activity. Phase 2. |
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| S7674 | Savolitinib (AZD6094) | Savolitinib (Volitinib, AZD6094, HMPL-504) is a novel, potent, and selective MET inhibitor currently in clinical development in various indications, including PRCC. The IC50 values of this compound for c-Met and p-Met are 5 nM and 3 nM, respectively. It shows exquisite selectivity for c-Met over 274 kinase. | ||
| S1361 | MGCD-265 analog | MGCD-265 is a potent, multi-target and ATP-competitive inhibitor of c-Met and VEGFR1/2/3 with IC50 of 1 nM, 3 nM/3 nM/4 nM, respectively; also inhibits Ron and Tie2. Phase 1/2. |
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| S2859 | Golvatinib (E7050) | Golvatinib (E7050) is a dual c-Met and VEGFR-2 inhibitor with IC50 of 14 nM and 16 nM, does not inhibit bFGF-stimulated HUVEC growth (up to 1000 nM). Phase 1/2. |
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| S7014 | Merestinib (LY2801653) | Merestinib (LY2801653) is a type-II ATP competitive, slow-off inhibitor of Met (c-Met) tyrosine kinase with a dissociation constant (Ki) of 2 nM, a pharmacodynamic residence time (Koff) of 0.00132 min(-1) and t1/2 of 525 min. Merestinib (LY2801653) also inhibits MST1R, AXL, ROS1, MKNK1/2, FLT3, MERTK, DDR1 and DDR2 with IC50 of 11 nM, 2 nM, 23 nM, 7 nM, 7 nM, 10 nM, 0.1 nM and 7 nM, respectively. | ||
| S9662 | UNC2025 | UNC2025 is a potent and orally active dual inhibitor of FLT3 and MER with IC50 of 0.35 nM and 0.46 nM, respectively. UNC2025 also inhibits AXL, TRKA, TRKC, QIK, TYRO3, SLK, NuaK1, Kit (c-Kit) and Met (c-Met) with IC50 of 1.65 nM, 1.67 nM, 4.38 nM, 5.75 nM, 5.83 nM, 6.14 nM, 7.97 nM, 8.18 nM and 364 nM, respectively. | ||
| S8570 | CEP-40783 (RXDX-106) | CEP-40783 (RXDX-106) is an orally-available, potent and selective TAM(TYRO3, AXL, MER)/Met (c-Met) inhibitor displaying low nanomolar biochemical activity and slow (T1/2 >120 min) inhibitor off-rate in peptide phosphorylation assays and in vitro kinase binding assays, respectively. | ||
| S2774 | MK-2461 | MK-2461 is a potent, multi-targeted inhibitor for c-Met(WT/mutants) with IC50 of 0.4-2.5 nM, less potent to Ron, Flt1; 8- to 30-fold greater selectivity of c-Met targets versus FGFR1, FGFR2, FGFR3, PDGFRβ, KDR, Flt3, Flt4, TrkA, and TrkB. Phase 1/2. . |
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| S7669 | NPS-1034 | NPS-1034 is a dual Met (c-Met)/Axl inhibitor with IC50 of 48 nM and 10.3 nM, respectively. | ||
| S8167 | AMG 337 | AMG 337 is an oral, small molecule, ATP-competitive, highly selective inhibitor of the Met (c-Met) receptor with an IC50 of 1 nM. | ||
| S3759 | Norcantharidin | Norcantharidin (Endothall anhydride) is a synthetic anticancer compound which is a dual inhibitor for c-Met and EGFR in human colon cancers. | ||
| S6412 | Altiratinib | Altiratinib (DCC-2701) is a potent single-digit nanomolar inhibitor of TRK, Met (c-Met), TIE2, and VEGFR2 kinases with IC50 vaules of 0.9 nM, 4.6 nM, and 0.8 nM for TRKA, B, and C, respectively. It inhibits Met (c-Met) and Met (c-Met) mutant with IC50 values in the range of 0.3-6 nM. | ||
| S2201 | BMS-794833 | BMS-794833 is a potent ATP competitive inhibitor of Met (c-Met)/VEGFR2 with IC50 of 1.7 nM/15 nM, also inhibits Ron, Axl and Flt3 with IC50 of <3 nM; a prodrug of BMS-817378. Phase 1. | ||
| S2761 | NVP-BVU972 | NVP-BVU972 is a selective and potent Met (c-Met) inhibitor with IC50 of 14 nM. | ||
| S8404 | S49076 | S49076 is a novel, potent inhibitor of Met (c-Met), AXL/MER, and FGFR1/2/3 with IC50 values below 20 nmol/L. | ||
| S1316 | AMG-208 | AMG 208 is a highly selective dual c-Met and RON inhibitor with IC50 of 9 nM for c-Met. | ||
| S2747 | AMG-458 | AMG 458 is a potent c-Met inhibitor with Ki of 1.2 nM, ~350-fold selectivity for c-Met than VEGFR2 in cells. | ||
| S6899 | Licochalcone D | Licochalcone D (Lico D, LCD, LD), a flavonoid isolated from a Chinese medicinal plant Glycyrrhiza inflata, has antioxidant, anti-inflammatory and anti-cancer properties. Licochalcone D inhibit phosphorylation of NF-κB p65 in LPS signaling pathway. Licochalcone D inhibits JAK2, EGFR and Met (c-Met) activities and induces ROS-dependent apoptosis. Licochalcone D also induces caspases activation and poly (ADP-ribose) polymerase (PARP) cleavage. | ||
| S0540 | BAY-474 | BAY-474 is an inhibitor of tyrosine-protein kinase c-Met and can act as an epigenetics probe. | ||
| S8854 | JNJ-38877618(OMO-1) | JNJ-38877618 (OMO-1) is a potent, highly selective, orally bioavailable Met (c-Met) kinase inhibitor with binding affinity (Kd) of 1.4 nM and enzyme inhibitory activity against wt and M1268T mutant Met (c-Met) (2 and 3 nM IC50). | ||
| S9620 | Elzovantinib (TPX-0022) | Elzovantinib (TPX-0022, CSF1R-IN-2) is a potent inhibitor of MET/CSF1R/SRC with enzymatic kinase inhibition IC50s of 0.14 nM, 0.71 nM and 0.12 nM, respectively. TPX-0022 modulates the tumor immune microenvironment in preclinical models. | ||
| S9308 | Pulsatilla saponin D | Pulsatilla saponin D (SB365), isolated from the root of Pulsatilla koreana, targets c-Met and exerts antiangiogenic and antitumor activities. | ||
| S6870 | Ningetinib | Ningetinib (CT-053, DE-120, CT053PTSA) is a potent, orally bioavailable inhibitor of tyrosine kinase with IC50 of 6.7 nM, 1.9 nM and <1.0 nM for c-Met, VEGFR2 and Axl, respectively. Ningetinib exhibits antitumor activity. | ||
| S0361 | AMG-1 | AMG-1 (c-Met/RON Dual Kinase Inhibitor, RON-IN-1) is a potent inhibitor of human c-Met and RON with IC50 of 4 nM and 9 nM, respectively. | ||
| S6762 | Bozitinib | Bozitinib is a highly selective ATP-competitive c-Met inhibitor with blood-brain barrier permeability. Bozitinib (PLB-1001) selectively inhibits MET-altered tumor cells in preclinical models. | ||
| S6764 | Pamufetinib (TAS-115) | Pamufetinib (TAS-115) is a highly potent c-Met and VEGFR dual inhibitor with IC50s of 30 nM and 32 nM for recombinant VEGFR2 and recombinant MET, respectively. | ||
| S7564 | SAR125844 | SAR125844 is a potent intravenously active and highly selective Met (c-Met) kinase inhibitor, displaying nanomolar activity against the wild-type kinase (IC50 value of 4.2 nmol/L) and H1094Y, Y1235D, M1250T, L1195V, and D1228H kinase domain mutants (IC50 values of 0.22, 1.7, 6.5, 65, and 81 nmol/L, respectively). | ||
| E4914New | Cabozantinib hydrochloride | Cabozantinib hydrochloride(XL184, BMS-907351 hydrochloride) is a potent small-molecule kinase inhibitor of c-MET and VEGFR2 with an IC50 of 1.3 nM, 0.035 nM respectively. It also inhibits RET, KIT, AXL, Tie2 and FLT3 with an IC50's of 5.2 nM, 4.6 nM, 7 nM, 14.3 nM, 11.3nM respectively. It can be promising agent for inhibiting tumor angiogenesis and metastasis in cancers with dysregulated MET and VEGFR signaling. | ||
| E1340New | Glesatinib | Glesatinib(MGCD265) is an orally bioavailable potent dual inhibitor of c-MET and SMO. Glesatinib counteracts P-glycoprotein (P-gp) mediated multidrug resistance (MDR) in non-small cell lung cancer (NSCLC). | ||
| S8676 | Glumetinib | Glumetinib is a potent and highly selective c-Met inhibitor with an IC50 of 0.42 ± 0.02 nmol/L. Glumetinib has greater than 2,400-fold selectivity for c-Met over those 312 kinases evaluated, including the c-Met family member RON and highly homologous kinases Axl, Mer, and TyrO3. | ||
| E0142 | XL092 | XL092 (JUN04542) is an ATP-competitive inhibitor of multiple RTKs including MET, VEGFR2, AXL and MER, with IC50 values of 15 nM, 1.6 nM, 3.4 nM, and 7.2 nM in cell-based assays, respectively. | ||
| A2467 | Telisotuzumab (Anti-HGFR / c-Met) | Telisotuzumab (Anti-HGFR / c-Met) is a monoclonal antibody that targets c-Met. MW: 145.64 KD. | ||
| A2468 | Onartuzumab (Anti-HGFR / c-Met) | Onartuzumab (Anti-HGFR / c-Met) is a unique, humanized and affinity-matured monovalent (one-armed) monoclonal antibody against the MET receptor. Onartuzumab potently inhibits HGF binding and receptor phosphorylation and signaling. Onartuzumab has antibody-like pharmacokinetics and antitumor activity. MW: 144.64 KD. | ||
| A2469 | Rilotumumab (Anti-HGF / SF) | Rilotumumab (Anti-HGF / SF) is a monoclonal antibody that inhibits HGF/MET-driven signaling. Rilotumumab shows anti-tumor activity, and can be used in castration-resistant prostate cancer (CRPC) and solid tumor research. MW: 145.5 KD. | ||
| A2661 | Ficlatuzumab (Anti-HGF / SF) | Ficlatuzumab (Anti-HGF / SF) is a monoclonal antibody (McAb) targeting human hepatocyte growth factor (HGF). It inhibits c-Met receptor-mediated cancer cell proliferation, migration, and invasion and can be used to treat head and neck squamous cell carcinoma (HNSCC). MW :150 KD. | ||
| A2662 | Emibetuzumab (Anti-HGFR / c-Met) | Emibetuzumab (Anti-HGFR / c-Met) is a humanized bivalent MET antibody targeting both HGF-dependent and HGF-independent MET pathway activation and tumor growth. It can be used in study of cancer. MW :144.56 KD. | ||
| A2930 | Anti-HGF / SF (TAK-701) | Anti-HGF / SF (TAK-701) is a humanized monoclonal antibody directed against human hepatocyte growth factor (HGF) with potential antineoplastic activity. It reverses gefitinib resistance in non-small-cell lung cancer. MW: 145.04 KD. | ||
| A2932 | Anti-HGFR / c-Met (SAIT301) | Anti-HGFR / c-Met (SAIT301) is a humanized monoclonal antibody targeting the alpha chain of the extracellular domain of the human hepatocyte growth factor receptor (HGFR or c-Met) with potential antineoplastic activity. MW: 146.0 KD. | ||
| E4606New | Dihexa | Dihexa(PNB-0408), an oligopeptide drug, is an orally active and blood-brain barrier-permeable analog of angiotensin IV. It binds to hepatocyte growth factor (HGF) with high affinity and potentiates its activity at its receptor, c-Met. Dihexa can also be used as a therapeutic potential in the treatment of Alzheimer’s disease. | ||
| E4914New | Cabozantinib hydrochloride | Cabozantinib hydrochloride(XL184, BMS-907351 hydrochloride) is a potent small-molecule kinase inhibitor of c-MET and VEGFR2 with an IC50 of 1.3 nM, 0.035 nM respectively. It also inhibits RET, KIT, AXL, Tie2 and FLT3 with an IC50's of 5.2 nM, 4.6 nM, 7 nM, 14.3 nM, 11.3nM respectively. It can be promising agent for inhibiting tumor angiogenesis and metastasis in cancers with dysregulated MET and VEGFR signaling. | ||
| E1340New | Glesatinib | Glesatinib(MGCD265) is an orally bioavailable potent dual inhibitor of c-MET and SMO. Glesatinib counteracts P-glycoprotein (P-gp) mediated multidrug resistance (MDR) in non-small cell lung cancer (NSCLC). |
c-Met阻害剤の選択性比較
c-Metシグナル伝達経路
Tags: c-Met inhibition | c-Met cancer | c-Met pathway | c-Met activation | c-Met phosphorylation | c-Met inhibitor clinical trial | c-Met assay | c-Met inhibitor therapy | c-Met inhibitor review
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