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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C26H20FN5O2S2 |
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分子量 | 517.60 | CAS No. | 875337-44-3 | |
Solubility (25°C)* | 体外 | DMSO | 104 mg/mL (200.92 mM) | |
Water | Insoluble | |||
Ethanol | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | 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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in vitro | MGCD-265 is a multi-target inhibitor of receptor tyrosine kinases. MGCD-265 potently inhibits Met, MetY1235D, MetM1250T, VEGFR1, VEGF2, VEGF3, Ron, and Tie2, with IC50 values ranging from 1 nM to 7 nM. [1] MGCD-265 inhibits cell proliferation both in c-Met-driven tumor cells (MKN45, MNNG-HOS, and SNU-5) and in non-c-Met-driven tumor cells (HCT116 and MDA-MB-231), with IC50 values of 6 nM–30 nM and 1 μM–3 μM, respectively. In serum starved MKN45 cells, MGCD-265 (40 nM–5 μM) effectively inhibits c-Met phosphorylation and its downstream signaling pathways, including Erk, Akt, Stat3, and Fak. MGCD-265 (6 nM–1 μM) also induces apoptosis in MKN45 cells. [2] |
in vivo | In c-Met-driven or non-c-Met-driven mice xenograft models of MKN45, U87MG, MDA-MB-231, COLO205, and A549 tumor cells, MGCD-265 (20 mg/kg–60 mg/kg) inhibits tumor growth and c-Met signaling. MGCD-265 (40 mg/kg) also downregulates genes involved in angiogenesis, including VEGF and IL-8, both in tumor and plasma of mice with U87MG xenograft. MGCD-265 also inhibits the plasma level of shed-Met. [2] |
細胞アッセイ | 細胞株 | HCT116, MDA-MB-231, SNU-5, and MKN45 cells |
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濃度 | 0–5 μM | |
反応時間 | 72 hours | |
実験の流れ | Cells are treated with MGCD-265 for 72 hours and cell number is determined as a function of mitochondrial activity, following incubation with MTT for 4 hours. |
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動物実験 | 動物モデル | Mice (CD-1 nude) xenograft models of MKN45, U87MG, MDA-MB-231, COLO205, and A549 cells |
投薬量 | 20 mg/kg–60 mg/kg | |
投与方法 | Orally |
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Data from [Data independently produced by Cancer Lett, 2013, 340(1), 43-50]
, , Dr. Zhang of Tianjin Medical University
Data from [Data independently produced by , , Mol Cancer Ther, 2018, 17(7):1526-1539]
Integrative analysis of drug response and clinical outcome in acute myeloid leukemia [ Cancer Cell, 2022, S1535-6108(22)00312-9] | PubMed: 35868306 |
A community challenge for a pancancer drug mechanism of action inference from perturbational profile data [ Cell Rep Med, 2022, 3(1):100492] | PubMed: 35106508 |
Chemical genomics reveals inhibition of breast cancer lung metastasis by Ponatinib via c-Jun. [ Protein Cell, 2019, 10(3):161-177] | PubMed: 29667003 |
A distinct cardiopharyngeal mesoderm genetic hierarchy establishes antero-posterior patterning of esophagus striated muscle [ Elife, 2019, 8e47460] | PubMed: 31535973 |
RAS-MAPK reactivation facilitates acquired resistance in FGFR1-amplified lung cancer and underlies a rationale for upfront FGFR-MEK blockade [Bockorny B Mol Cancer Ther, 2018, 17(7):1526-1539] | PubMed: 29654068 |
Acquired resistance to AZD9291 as an upfront treatment is dependent on ERK signaling in a preclinical model [Ku BM PLoS One, 2018, 13(4):e0194730] | PubMed: 29641535 |
The innate immune response in fetal lung mesenchymal cells targets VEGFR2 expression and activity. [ Am J Physiol Lung Cell Mol Physiol, 2017, 312(6):L861-L872] | PubMed: 28336813 |
Acquired METD1228V Mutation and Resistance to MET Inhibition in Lung Cancer. [ Cancer Discov, 2016, 6(12):1334-1341] | PubMed: 27694386 |
Dual inhibition of EGFR and MET induces synthetic lethality in triple-negative breast cancer cells through downregulation of ribosomal protein S6 [ Int J Oncol, 2015, 47(1):122-32] | PubMed: 25955731 |
Bioluminescent cell-based NAD(P)/NAD(P)H assays for rapid dinucleotide measurement and inhibitor screening [ Assay Drug Dev Technol, 2014, 12(9-10):514-26] | PubMed: 25506801 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。