Introduction：Basic information about CAS 875337-44-3|MGCD-265, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | MGCD-265 |
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| CAS Number | 875337-44-3 | Molecular Weight | 517.598 |
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| Density | 1.4±0.1 g/cm3 | Boiling Point | 195.7ºC at 760 mmHg |
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| Molecular Formula | C26H20FN5O2S2 | Melting Point | / |
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| MSDS | / | Flash Point | 72.1ºC |
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Names
| Name | N-[[3-fluoro-4-[2-(1-methylimidazol-4-yl)thieno[3,2-b]pyridin-7-yl]oxyphenyl]carbamothioyl]-2-phenylacetamide |
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| Synonym | More Synonyms |
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MGCD-265 BiologicalActivity
| 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 | Signaling Pathways >>Protein Tyrosine Kinase/RTK >>c-Met/HGFRResearch Areas >>Cancer |
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| Target | VEGFR2:10 nM (IC50) c-Met:29 nM (IC50) |
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| References | [1]. Claridge S, et al. Discovery of a novel and potent series of thieno[3,2-b]pyridine-based inhibitors of c-Met and VEGFR2 tyrosine kinases. Bioorg Med Chem Lett. 2008 May 1;18(9):2793-8. |
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Chemical & Physical Properties
| Density | 1.4±0.1 g/cm3 |
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| Boiling Point | 195.7ºC at 760 mmHg |
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| Molecular Formula | C26H20FN5O2S2 |
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| Molecular Weight | 517.598 |
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| Flash Point | 72.1ºC |
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| Exact Mass | 517.104248 |
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| PSA | 151.93000 |
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| LogP | 6.91 |
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| Index of Refraction | 1.707 |
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| InChIKey | UFICVEHDQUKCEA-UHFFFAOYSA-N |
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| SMILES | Cn1cnc(-c2cc3nccc(Oc4ccc(NC(=S)NC(=O)Cc5ccccc5)cc4F)c3s2)c1 |
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| Storage condition | -20℃ |
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Synonyms
| 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 |
