c-Met
シグナル伝達経路
研究分野
阻害剤の選択性比較
| カタログ番号 | 製品カタログ | 溶解度(25°C) | ||
|---|---|---|---|---|
| 水 | DMSO | アルコール | ||
| S1068 | Crizotinib (PF-02341066) | <1 mg/mL | 9 mg/mL | <1 mg/mL |
| S1119 | Cabozantinib (BMS-907351) | <1 mg/mL | 100 mg/mL | <1 mg/mL |
| S1111 | Foretinib (GSK1363089) | <1 mg/mL | 100 mg/mL | <1 mg/mL |
| S1070 | PHA-665752 | <1 mg/mL | 128 mg/mL | <1 mg/mL |
| S1080 | SU11274 | <1 mg/mL | 92 mg/mL | 2 mg/mL |
| S8854 | JNJ-38877618(OMO-1) | <1 mg/mL | 10 mg/mL | 2 mg/mL |
| S8676 | Glumetinib (SCC244) | <1 mg/mL | 11 mg/mL | <1 mg/mL |
| S6412 | Altiratinib | <1 mg/mL | 100 mg/mL | <1 mg/mL |
| S7564 | SAR125844 | ˂1 mg/mL | 11 mg/mL | ˂1 mg/mL |
| S1112 | SGX-523 | <1 mg/mL | 3 mg/mL | <1 mg/mL |
| S1561 | BMS-777607 | <1 mg/mL | 47 mg/mL | <1 mg/mL |
| S2753 | Tivantinib (ARQ 197) | <1 mg/mL | 73 mg/mL | <1 mg/mL |
| S1114 | JNJ-38877605 | <1 mg/mL | 37 mg/mL | <1 mg/mL |
| S1094 | PF-04217903 | <1 mg/mL | 5 mg/mL | <1 mg/mL |
| S1361 | MGCD-265 analog | <1 mg/mL | 104 mg/mL | <1 mg/mL |
| S2788 | Capmatinib (INCB28060) | <1 mg/mL | 2 mg/mL | <1 mg/mL |
| S1124 | BMS-754807 | <1 mg/mL | 92 mg/mL | 92 mg/mL |
| S2201 | BMS-794833 | <1 mg/mL | 94 mg/mL | <1 mg/mL |
| S1316 | AMG-208 | <1 mg/mL | 0.25 mg/mL | <1 mg/mL |
| S2774 | MK-2461 | <1 mg/mL | 99 mg/mL | <1 mg/mL |
| S2859 | Golvatinib (E7050) | <1 mg/mL | 20 mg/mL | <1 mg/mL |
| S2747 | AMG-458 | <1 mg/mL | 21 mg/mL | <1 mg/mL |
| S2761 | NVP-BVU972 | <1 mg/mL | 68 mg/mL | 68 mg/mL |
| S8167 | AMG 337 | <1 mg/mL | 95 mg/mL | 95 mg/mL |
| S7014 | Merestinib (LY2801653) | <1 mg/mL | 100 mg/mL | 100 mg/mL |
| S8404 | S49076 | <1 mg/mL | 87 mg/mL | <1 mg/mL |
| S9308 | Pulsatilla saponin D | -1 mg/mL | 100 mg/mL | -1 mg/mL |
| S3759 | Norcantharidin | -1 mg/mL | 33 mg/mL | -1 mg/mL |
| S7669 | NPS-1034 | <1 mg/mL | 100 mg/mL | 4 mg/mL |
| S7674 | Savolitinib(AZD6094) | <1 mg/mL | 16 mg/mL | <1 mg/mL |
c-Met製品
| 製品コード | 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 |
|---|---|---|---|
| S1068 |
Crizotinib (PF-02341066)Crizotinib (PF-02341066) 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. |
(c) Western blot analyses of p-Akt (Ser473) and p-S6RP (Ser235 and Ser236) in two RCT-E565 transplanted tumors treated with vehicle or PF02341066. Samples were isolated 4 h after the last dose from mice treated with PF02341066 for 3 d. (d) Responses of RCT-E565 transplanted tumors in athymic mice to PF02341066 or vehicle. Data are means ±s.e.m. (each group, n = 6). *P < 0.005, **P < 0.001 (Student,s t test). |
|
| S1119 |
Cabozantinib (BMS-907351)Cabozantinib (XL184, BMS-907351) is a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret, 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. |
Effects of AXL inhibitors on induction of pAKT and rescue of pERK following AXL overexpression. R428, 500 nmol/L; XL184, 3 umol/L; XL880, 100 nmol/L; in the presence or absence of 2 umol/L PLX4720. shAXL is a positive control.
|
|
| S1111 |
Foretinib (GSK1363089)Foretinib (GSK1363089) is an ATP-competitive inhibitor of HGFR and VEGFR, mostly for 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, PDGFRα/β and Tie-2, and little activity to FGFR1 and EGFR. Phase 2. |
c-MET/RON inhibitors restore sensitivity to lapatinib in SK-BR-3-LR cells. Cell growth was determined using the sulforhodamine B assay. The concentration used was 0.1 uM for crizotinib, MGCD-265, XL880, sunitinib, dasatinib, and TAE-684I. The phosphorylation of HER2, AKT and ERK1/2 was determined by Western blotting.
|
|
| S1070 |
PHA-665752PHA-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. |
A, representative Western blot analyses of samples obtained from NSCLC cells exposed to 1 umol/L erlotinib or PHA-665,752 for 6 hours. Levels of total and phosphorylated forms of EGFR, MET, and HER3. B, representative Western blot analyses of samples obtained as described in A showing the levels of EGFR downstream signaling mediators. Protein samples obtained from untreated and treated cells were separated by SDS-PAGE and immunoblotted with each antibody. Tubulin served to ensure equal loading.
|
|
| S1080 |
SU11274SU11274 is a selective Met inhibitor with IC50 of 10 nM in cell-free assays, no effects on PGDFRβ, EGFR or Tie2. |
Effect of crizotinib, tivantinib, and SU11274 on levels of c-MET phosphorylation and downstream signaling pathway in SW1736 and TL3 thyroid cancer cells. Cells were prestarved in culture medium containing 0.5% FBS (24 hour) ?either crizotinib or tivantinib (0.1, 1.0, and 10 umol/L) or SU11274 (10 umol/L), and stimulated with 20 ng/mL recombinant human HGF for 10 minutes before lysates were made for Western blotting. A series of c-MET downstream signaling pathway proteins and phosphor proteins were detected using Western blotting. β-Actin was used as a loading balance control.
|
|
| S6762新 |
Bozitinib (PLB-1001)Bozitinib is a highly selective ATP-competitive small-molecule c-Met inhibitor with blood-brain barrier permeability. |
||
| S6764新 |
TAS-115TAS-115 is a unique VEGFR/MET-targeted inhibitor with IC50 of 30nM and 32nM for rVEGFR2 and rMET, respectively. |
||
| S8854新 |
JNJ-38877618(OMO-1)JNJ-38877618 (OMO-1) is a potent, highly selective, orally bioavailable MET kinase inhibitor with binding affinity (Kd) of 1.4 nM and enzyme inhibitory activity against wt and M1268T mutant MET (2 and 3 nM IC50). |
||
| S8676新 |
Glumetinib (SCC244)Glumetinib (SCC244) 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. |
||
| S6412新 |
AltiratinibAltiratinib is a potent single-digit nanomolar inhibitor of TRK, 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 and MET mutant with IC50 values in the range of 0.3-6 nM. |
||
| S7564新 |
SAR125844SAR125844 is a potent intravenously active and highly selective 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). |
||
| S1112 |
SGX-523SGX-523 is a selective Met inhibitor with IC50 of 4 nM, no activity to BRAFV599E, c-Raf, Abl and p38α. Phase 1. |
Association of c-Met phosphorylation and s-Met generation in EBC-1 xenograft tumor. Mice were treated with SGX523 at 10 mg/kg, 3 mg/kg, 0.1 mg/kg, at 0 h and 8 h point, respectively. Plasma and tumor lysates were collected using the method described in "Materials and methods"section at 24 h time point. The bar and line in the figure represents the average phosphorylation rate of c-Met and s-Met in subgroups, respectively. Each subgroup consists of four mice with tumor volume around 600 mm3.
|
|
| S1561 |
BMS-777607BMS-777607 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. Phase 1/2. |
Numbers of clonogenic cells from L3.6pl cells and CSCs＋24/44/ESAin duplicate were counted. Clonogenic growth from the cell control was set as 100%. |
|
| S2753 |
Tivantinib (ARQ 197)Tivantinib (ARQ 197) 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. Phase 3. |
Effect of tivantinib on the mitotic index was compared with the antimitotic drugs paclitaxel and vinblastine after overnight treatment of the HLE cell line with two different concentrations of each drug |
|
| S1114 |
JNJ-38877605JNJ-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. |
Growth factors induced ERK phosphorylation in RPE50 and ARPE19. (B) RPE50 cells were untreated (-), treated with 50 nM of HGF or EGF or 50 ng/ml HB-EGF coupled with DMSO or various inhibitors as indicated for 0.5 h. |
|
| S1094 |
PF-04217903PF-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. |
Clonogenicity of LXFA 526L and LXFA 1647L with titration of the MET inhibitor PF-04217903 and combination of PF-04217903 at 0.1 uM with 0.66 uM cetuximab.
|
|
| S1361 |
MGCD-265 analogMGCD-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. |
c-MET/RON inhibitors restore sensitivity to lapatinib in SK-BR-3-LR cells. The concentration used was 0.1 uM for crizotinib, MGCD-265, XL880, sunitinib, dasatinib, TAE-684, and RON inhibitor I. Columns, means; bars, SEMs (n = 3). The phosphorylation of HER2, AKT and ERK1/2 was determined by Western blotting.
|
|
| S2788 |
Capmatinib (INCB28060)Capmatinib (INCB28060) 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. Phase 1. |
(a) MET inhibition by INCB28060 prevents HGF-induced MET phosphorylation in MDA-MB231 and HCC-1954 cells. After one hour preincubation with INC2B8060, BC cells were stimulated with HGF for one hour. Phosphorylation of MET and total MET were determined by western blot and quantified by densitometric analysis. Results are expressed as percentage of unstimulated and untreated cells (negative control). |
|
| S1124 |
BMS-754807BMS-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, Aurora A/B, TrkA/B and Ron, and shows little activity to Flt3, Lck, MK2, PKA, PKC etc. Phase 2. |
|
|
| S2201 |
BMS-794833BMS-794833 is a potent ATP competitive inhibitor of 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. |
||
| S1316 |
AMG-208AMG 208 is a highly selective c-Met inhibitor with IC50 of 9 nM. Phase 1. |
||
| S2774 |
MK-2461MK-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. . |
Both V-H cells and V-J cells are treated with MK-2461, XL-184 or ABT-869, respectively. (i-k) Western blot analysis of sFlt-1 expression after incubation with three VEGF-A receptor inhibitors or in the control.
|
|
| 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. |
PC-9/LMC-GR cells (2 × 105 cells/well) were incubated in 6-well plates with various concentrations of gefitinib with or without crizotinib (1 μmol/L) or golvatinib (1 μmol/L) for 1 hour. Cell lysate were obtained and subjected to immunoblotting with antibodies toward the indicated molecules.
|
|
| S2747 |
AMG-458AMG 458 is a potent c-Met inhibitor with Ki of 1.2 nM, ~350-fold selectivity for c-Met than VEGFR2 in cells. |
||
| S2761 |
NVP-BVU972NVP-BVU972 is a selective and potent Met inhibitor with IC50 of 14 nM. |
||
| S8167 |
AMG 337AMG 337 is an oral, small molecule, ATP-competitive, highly selective inhibitor of the MET receptor. |
||
| S7014 |
Merestinib (LY2801653)LY2801653 is a type-II ATP competitive, slow-off inhibitor of 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. |
||
| S8404 |
S49076S49076 is a novel, potent inhibitor of MET, AXL/MER, and FGFR1/2/3 with IC50 values below 20 nmol/L. |
||
| S9308 |
Pulsatilla saponin DPulsatilla saponin D, isolated from the root of Pulsatilla koreana, targets c-Met and exerts antiangiogenic and antitumor activities. |
||
| S3759 |
NorcantharidinNorcantharidin is a synthetic anticancer compound which is a dual inhibitor for c-Met and EGFR in human colon cancers. |
||
| S7669 |
NPS-1034NPS-1034 is a dual Met/Axl inhibitor with IC50 of 48 nM and 10.3 nM, respectively. |
||
| 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. |
| 製品コード | 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 |
|---|---|---|---|
| S1068 |
Crizotinib (PF-02341066)Crizotinib (PF-02341066) 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. |
(c) Western blot analyses of p-Akt (Ser473) and p-S6RP (Ser235 and Ser236) in two RCT-E565 transplanted tumors treated with vehicle or PF02341066. Samples were isolated 4 h after the last dose from mice treated with PF02341066 for 3 d. (d) Responses of RCT-E565 transplanted tumors in athymic mice to PF02341066 or vehicle. Data are means ±s.e.m. (each group, n = 6). *P < 0.005, **P < 0.001 (Student,s t test). |
|
| S1119 |
Cabozantinib (BMS-907351)Cabozantinib (XL184, BMS-907351) is a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret, 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. |
Effects of AXL inhibitors on induction of pAKT and rescue of pERK following AXL overexpression. R428, 500 nmol/L; XL184, 3 umol/L; XL880, 100 nmol/L; in the presence or absence of 2 umol/L PLX4720. shAXL is a positive control.
|
|
| S1111 |
Foretinib (GSK1363089)Foretinib (GSK1363089) is an ATP-competitive inhibitor of HGFR and VEGFR, mostly for 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, PDGFRα/β and Tie-2, and little activity to FGFR1 and EGFR. Phase 2. |
c-MET/RON inhibitors restore sensitivity to lapatinib in SK-BR-3-LR cells. Cell growth was determined using the sulforhodamine B assay. The concentration used was 0.1 uM for crizotinib, MGCD-265, XL880, sunitinib, dasatinib, and TAE-684I. The phosphorylation of HER2, AKT and ERK1/2 was determined by Western blotting.
|
|
| S1070 |
PHA-665752PHA-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. |
A, representative Western blot analyses of samples obtained from NSCLC cells exposed to 1 umol/L erlotinib or PHA-665,752 for 6 hours. Levels of total and phosphorylated forms of EGFR, MET, and HER3. B, representative Western blot analyses of samples obtained as described in A showing the levels of EGFR downstream signaling mediators. Protein samples obtained from untreated and treated cells were separated by SDS-PAGE and immunoblotted with each antibody. Tubulin served to ensure equal loading.
|
|
| S1080 |
SU11274SU11274 is a selective Met inhibitor with IC50 of 10 nM in cell-free assays, no effects on PGDFRβ, EGFR or Tie2. |
Effect of crizotinib, tivantinib, and SU11274 on levels of c-MET phosphorylation and downstream signaling pathway in SW1736 and TL3 thyroid cancer cells. Cells were prestarved in culture medium containing 0.5% FBS (24 hour) ?either crizotinib or tivantinib (0.1, 1.0, and 10 umol/L) or SU11274 (10 umol/L), and stimulated with 20 ng/mL recombinant human HGF for 10 minutes before lysates were made for Western blotting. A series of c-MET downstream signaling pathway proteins and phosphor proteins were detected using Western blotting. β-Actin was used as a loading balance control.
|
|
| S6762新 |
Bozitinib (PLB-1001)Bozitinib is a highly selective ATP-competitive small-molecule c-Met inhibitor with blood-brain barrier permeability. |
||
| S6764新 |
TAS-115TAS-115 is a unique VEGFR/MET-targeted inhibitor with IC50 of 30nM and 32nM for rVEGFR2 and rMET, respectively. |
||
| S8854新 |
JNJ-38877618(OMO-1)JNJ-38877618 (OMO-1) is a potent, highly selective, orally bioavailable MET kinase inhibitor with binding affinity (Kd) of 1.4 nM and enzyme inhibitory activity against wt and M1268T mutant MET (2 and 3 nM IC50). |
||
| S8676新 |
Glumetinib (SCC244)Glumetinib (SCC244) 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. |
||
| S6412新 |
AltiratinibAltiratinib is a potent single-digit nanomolar inhibitor of TRK, 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 and MET mutant with IC50 values in the range of 0.3-6 nM. |
||
| S7564新 |
SAR125844SAR125844 is a potent intravenously active and highly selective 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). |
||
| S1112 |
SGX-523SGX-523 is a selective Met inhibitor with IC50 of 4 nM, no activity to BRAFV599E, c-Raf, Abl and p38α. Phase 1. |
Association of c-Met phosphorylation and s-Met generation in EBC-1 xenograft tumor. Mice were treated with SGX523 at 10 mg/kg, 3 mg/kg, 0.1 mg/kg, at 0 h and 8 h point, respectively. Plasma and tumor lysates were collected using the method described in "Materials and methods"section at 24 h time point. The bar and line in the figure represents the average phosphorylation rate of c-Met and s-Met in subgroups, respectively. Each subgroup consists of four mice with tumor volume around 600 mm3.
|
|
| S1561 |
BMS-777607BMS-777607 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. Phase 1/2. |
Numbers of clonogenic cells from L3.6pl cells and CSCs＋24/44/ESAin duplicate were counted. Clonogenic growth from the cell control was set as 100%. |
|
| S2753 |
Tivantinib (ARQ 197)Tivantinib (ARQ 197) 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. Phase 3. |
Effect of tivantinib on the mitotic index was compared with the antimitotic drugs paclitaxel and vinblastine after overnight treatment of the HLE cell line with two different concentrations of each drug |
|
| S1114 |
JNJ-38877605JNJ-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. |
Growth factors induced ERK phosphorylation in RPE50 and ARPE19. (B) RPE50 cells were untreated (-), treated with 50 nM of HGF or EGF or 50 ng/ml HB-EGF coupled with DMSO or various inhibitors as indicated for 0.5 h. |
|
| S1094 |
PF-04217903PF-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. |
Clonogenicity of LXFA 526L and LXFA 1647L with titration of the MET inhibitor PF-04217903 and combination of PF-04217903 at 0.1 uM with 0.66 uM cetuximab.
|
|
| S1361 |
MGCD-265 analogMGCD-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. |
c-MET/RON inhibitors restore sensitivity to lapatinib in SK-BR-3-LR cells. The concentration used was 0.1 uM for crizotinib, MGCD-265, XL880, sunitinib, dasatinib, TAE-684, and RON inhibitor I. Columns, means; bars, SEMs (n = 3). The phosphorylation of HER2, AKT and ERK1/2 was determined by Western blotting.
|
|
| S2788 |
Capmatinib (INCB28060)Capmatinib (INCB28060) 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. Phase 1. |
(a) MET inhibition by INCB28060 prevents HGF-induced MET phosphorylation in MDA-MB231 and HCC-1954 cells. After one hour preincubation with INC2B8060, BC cells were stimulated with HGF for one hour. Phosphorylation of MET and total MET were determined by western blot and quantified by densitometric analysis. Results are expressed as percentage of unstimulated and untreated cells (negative control). |
|
| S1124 |
BMS-754807BMS-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, Aurora A/B, TrkA/B and Ron, and shows little activity to Flt3, Lck, MK2, PKA, PKC etc. Phase 2. |
|
|
| S2201 |
BMS-794833BMS-794833 is a potent ATP competitive inhibitor of 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. |
||
| S1316 |
AMG-208AMG 208 is a highly selective c-Met inhibitor with IC50 of 9 nM. Phase 1. |
||
| S2774 |
MK-2461MK-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. . |
Both V-H cells and V-J cells are treated with MK-2461, XL-184 or ABT-869, respectively. (i-k) Western blot analysis of sFlt-1 expression after incubation with three VEGF-A receptor inhibitors or in the control.
|
|
| 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. |
PC-9/LMC-GR cells (2 × 105 cells/well) were incubated in 6-well plates with various concentrations of gefitinib with or without crizotinib (1 μmol/L) or golvatinib (1 μmol/L) for 1 hour. Cell lysate were obtained and subjected to immunoblotting with antibodies toward the indicated molecules.
|
|
| S2747 |
AMG-458AMG 458 is a potent c-Met inhibitor with Ki of 1.2 nM, ~350-fold selectivity for c-Met than VEGFR2 in cells. |
||
| S2761 |
NVP-BVU972NVP-BVU972 is a selective and potent Met inhibitor with IC50 of 14 nM. |
||
| S8167 |
AMG 337AMG 337 is an oral, small molecule, ATP-competitive, highly selective inhibitor of the MET receptor. |
||
| S7014 |
Merestinib (LY2801653)LY2801653 is a type-II ATP competitive, slow-off inhibitor of 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. |
||
| S8404 |
S49076S49076 is a novel, potent inhibitor of MET, AXL/MER, and FGFR1/2/3 with IC50 values below 20 nmol/L. |
||
| S9308 |
Pulsatilla saponin DPulsatilla saponin D, isolated from the root of Pulsatilla koreana, targets c-Met and exerts antiangiogenic and antitumor activities. |
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| S3759 |
NorcantharidinNorcantharidin is a synthetic anticancer compound which is a dual inhibitor for c-Met and EGFR in human colon cancers. |
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| S7669 |
NPS-1034NPS-1034 is a dual Met/Axl inhibitor with IC50 of 48 nM and 10.3 nM, respectively. |
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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. |
