MGCD-265
Modify Date: 2024-01-30 18:04:58
MGCD-265 structure
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Common Name | MGCD-265 | ||
|---|---|---|---|---|
| CAS Number | 875337-44-3 | Molecular Weight | 517.598 | |
| Density | 1.4±0.1 g/cm3 | Boiling Point | 195.7ºC at 760 mmHg | |
| Molecular Formula | C26H20FN5O2S2 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | 72.1ºC | |
Use of MGCD-265MGCD-265-analog (structurally related to MGCD-265) is an orally bioavailable multitargeted tyrosine kinase inhibitor with potential antineoplastic activity with IC50 of 29 nM and 10 nM for c-Met and VEGFR2, respectively.IC50 value:10 nM (VEGFR2), 29 nM(c-Met) [1]Target:VEGFR, c-Metin vivo: MGCD-265-analog has a reasonable half-life, 1.2 h in rats and 5.8 h in dogs, and has an acceptable clearance, 0.33 L/(kg h) in rats and 1.1 L/(kg h) in dogs. The steady state volume of distribution was low in rats (0.25 L/kg) and reasonable in dogs (1.5 L/kg), while the oral bio-availability was determined to be 12% and 42% in rats and dogs, respectively. GCD-265-analog performed well in vivo against a panel of different human tumor types, particularly those that are driven by or overexpress c-Met (MNNGHOS and MKN45). Tumor growth inhibition at a dose of 20 mg/kg po once daily ranged from 41% to 94%. MGCD-265-analog was found to show spill-over inhibition of a number of kinases in addition to the intended c-Met/VEGFR2 activity. MGCD-265-analog has significant antitumor activity in vivo.[1] |
| Name | N-[[3-fluoro-4-[2-(1-methylimidazol-4-yl)thieno[3,2-b]pyridin-7-yl]oxyphenyl]carbamothioyl]-2-phenylacetamide |
|---|---|
| Synonym | More Synonyms |
| Description | MGCD-265-analog (structurally related to MGCD-265) is an orally bioavailable multitargeted tyrosine kinase inhibitor with potential antineoplastic activity with IC50 of 29 nM and 10 nM for c-Met and VEGFR2, respectively.IC50 value:10 nM (VEGFR2), 29 nM(c-Met) [1]Target:VEGFR, c-Metin vivo: MGCD-265-analog has a reasonable half-life, 1.2 h in rats and 5.8 h in dogs, and has an acceptable clearance, 0.33 L/(kg h) in rats and 1.1 L/(kg h) in dogs. The steady state volume of distribution was low in rats (0.25 L/kg) and reasonable in dogs (1.5 L/kg), while the oral bio-availability was determined to be 12% and 42% in rats and dogs, respectively. GCD-265-analog performed well in vivo against a panel of different human tumor types, particularly those that are driven by or overexpress c-Met (MNNGHOS and MKN45). Tumor growth inhibition at a dose of 20 mg/kg po once daily ranged from 41% to 94%. MGCD-265-analog was found to show spill-over inhibition of a number of kinases in addition to the intended c-Met/VEGFR2 activity. MGCD-265-analog has significant antitumor activity in vivo.[1] |
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| Related Catalog | |
| Target |
VEGFR2:10 nM (IC50) c-Met:29 nM (IC50) |
| References |
| Density | 1.4±0.1 g/cm3 |
|---|---|
| Boiling Point | 195.7ºC at 760 mmHg |
| Molecular Formula | C26H20FN5O2S2 |
| Molecular Weight | 517.598 |
| Flash Point | 72.1ºC |
| Exact Mass | 517.104248 |
| PSA | 151.93000 |
| LogP | 6.91 |
| Index of Refraction | 1.707 |
| Storage condition | -20℃ |
| N-[(3-Fluoro-4-{[2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yl]oxy}phenyl)carbamothioyl]-2-phenylacetamide |
| Benzeneacetamide, N-[[[3-fluoro-4-[[2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yl]oxy]phenyl]amino]thioxomethyl]- |
| cc-38 |
| MGCD-265 |
| N-(3-fluoro-4-(2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yloxy)phenylcarbamothioyl)-2-phenylacetamide |
| S1361_Selleck |
| MGCD265,MGCD-265 |
| MGCD-265 analog |