Antibodies
MGCD-265
- 貨號 Cat. No.
- S1361
- 規格 Size
- 5~200mg
- 品牌 Brand
- Selleckchem
Description
MGCD-265
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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Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
| Description | 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. | |||||
|---|---|---|---|---|---|---|
| Targets | Met | VEGFR1 | VEGFR2 | VEGFR3 | Ron | Tie2 |
| IC50 | 1 nM | 3 nM | 3 nM | 4 nM | 2 nM | 7 nM [1] |
| 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] | |||||
| Features | ||||||
Protocol(Only for Reference)
Cell Assay: [2]
| Cell lines | HCT116, MDA-MB-231, SNU-5, and MKN45 cells |
|---|---|
| Concentrations | 0–5 μM |
| Incubation Time | 72 hours |
| Method | 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. |
Animal Study: [2]
| Animal Models | Mice (CD-1 nude) xenograft models of MKN45, U87MG, MDA-MB-231, COLO205, and A549 cells |
|---|---|
| Dosages | 20 mg/kg–60 mg/kg |
| Administration | Orally |
References
Clinical Trial Information( data from http://clinicaltrials.gov)
| NCT Number | Recruitment | Conditions | Sponsor /Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT00679133 | Completed | Advanced Malignancies | MethylGene Inc. | 2008-04 | Phase 1 |
| NCT00697632 | Recruiting | Advanced Malignancies | MethylGene Inc. | 2008-06 | Phase 1 |
| NCT00975767 | Recruiting | Advanced Malignancies, Non-small Cell Lung Cancer | MethylGene Inc. | 2009-08 | Phase 1|Phase 2 |
Chemical Information
| Molecular Weight (MW) | 517.60 |
|---|---|
| Formula | C26H20FN5O2S2 |
| CAS No. | 875337-44-3 |
| Storage | 3 years -20℃Powder |
|---|---|
| 6 months-80℃in DMSO | |
| Syonnyms | N/A |
| Solubility (25°C) * | In vitro | DMSO | 104 mg/mL (200 mM) |
|---|---|---|---|
| Water | <1 mg/mL (<1 mM) | ||
| Ethanol | <1 mg/mL (<1 mM) | ||
| * <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. | |||
| Chemical Name |
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Preparing Stock Solutions
| Stock Solution (1ml DMSO) | 1mM | 10mM | 20mM | 30mM |
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| Mass(mg) | 0.5176 | 5.176 | 10.352 | 15.528 |
Customer Reviews (1)
 Click to enlarge | Rating | |
| Source | Dr. Zhang of Tianjin Medical University. MGCD-265 purchased from Selleck | |
| Method | Western blot | |
| Cell Lines | MDA-MB-231 cells | |
| Concentrations | 0-5 μM | |
| Incubation Time | ||
| Results | MGCD-265 treatment resulted in a reduction of c-Met phosphorylation in MDA-MB-231 cells. |
Product Citations (1)
RON confers lapatinib resistance in HER2-positive breast cancer cells. [Wang Q, et al. Cancer Lett 2013;340(1):43-50]
PubMed: 23811285
