| Cat.No. | Product Name | Information | Product Use Citations | Product Validations |
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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. |
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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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| 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. This compound 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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| 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. |
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| 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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| 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. This compound 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. |
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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, respectively. This compound does not inhibit bFGF-stimulated HUVEC growth (up to 1000 nM) and is currently in Phase 1/2 trials. |
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| 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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| S5115 | Sodium L-Ascorbyl-2-Phosphate (SAP) | 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. Sodium L-ascorbyl-2-phosphate (2-Phospho-L-ascorbic acid trisodium salt, L-Ascorbic acid 2-phosphate trisodium salt, Sodium ascorbyl phosphate, SAP) is a selective antioxidant and a stimulator of hepatocyte growth factor (HGF) production. |
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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. |
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| 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. |
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| 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. |
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| S2761 | NVP-BVU972 | NVP-BVU972 is a selective and potent Met (c-Met) inhibitor with IC50 of 14 nM. |
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| 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. |
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| S9308 | Pulsatilla saponin D | Pulsatilla saponin D (SB365), isolated from the root of Pulsatilla koreana, targets c-Met and exerts antiangiogenic and antitumor activities. |
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| S6762 | Bozitinib | Bozitinib (PLB-1001) is a highly selective ATP-competitive c-Met inhibitor with blood-brain barrier permeability. This compound selectively inhibits MET-altered tumor cells in preclinical models. |
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| 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. |
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| E1340 | Glesatinib | Glesatinib(MGCD265) is an orally bioavailable potent dual inhibitor of c-MET and SMO. This compound counteracts P-glycoprotein (P-gp) mediated multidrug resistance (MDR) in non-small cell lung cancer (NSCLC). |
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| S8676 | Glumetinib | Glumetinib is a potent and highly selective c-Met inhibitor with an IC50 of 0.42 ± 0.02 nmol/L. This compound 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. |
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| 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. | ||
| 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) | A potent, highly selective, orally bioavailable Met (c-Met) kinase inhibitor, JNJ-38877618 (OMO-1) exhibits 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. | ||
| 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. This compound 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. | ||
| 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). | ||
| E4914 | 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. | ||
| 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. |
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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. This compound induces apoptosis. |
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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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| 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. It suppresses c-MET and c-RET, and is also active as a DNA repair protein Rad51 inhibitor with antineoplastic activity. Phase 2. |
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| 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. |
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| S3759 | Norcantharidin | Norcantharidin (Endothall anhydride) is a synthetic anticancer compound which is a dual inhibitor for c-Met and EGFR in human colon cancers. |
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| 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. This compound inhibits Met (c-Met) and Met (c-Met) mutant with IC50 values in the range of 0.3-6 nM. |
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| 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. This compound inhibits phosphorylation of NF-κB p65 in LPS signaling pathway. It inhibits JAK2, EGFR and Met (c-Met) activities and induces ROS-dependent apoptosis. This chemical also induces caspases activation and poly (ADP-ribose) polymerase (PARP) cleavage. | ||
| 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. |