| Size | Price | Stock | Qty |
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| 2mg |
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| 5mg |
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| 10mg |
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| 25mg |
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Purity: ≥98%
MGCD-265 analog (Glesatinib analog) is a potent, orally bioavailable, and ATP-competitive multi-kinase inhibitor with potential antitumor activity. In clinical trials, MGCD265 analog has been investigated as a monotherapy and in combination with either docetaxel or erlotinib for patients with advanced solid tumors, including NSCLC. In a phase I trial, patients with advanced solid cancer were given MGCD265 analog orally twice daily, continuously increasing the dose from 24 mg/m2 to 235 mg/m2 until the disease progressed.
| Targets |
Met (IC50 = 1 nM); RON (IC50 = 2 nM); VEGFR1 (IC50 = 3 nM); VEGFR2 (IC50 = 3 nM); VEGFR3 (IC50 = 4 nM)
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| ln Vivo |
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| Enzyme Assay |
The orally bioavailable multitargeted tyrosine kinase inhibitor MGCD-265-analog (structurally related to MGCD-265) has an IC50 of 29 nM for c-Met and 10 nM for VEGFR2, respectively, suggesting that it may have antineoplastic potential. IC50 values: 29 nM for c-Met and 10 nM for VEGFR2.
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| Cell Assay |
After MGCD-265 treatment for 72 hours, cells are incubated with MTT for 4 hours, and the number of cells is calculated based on mitochondrial activity.
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| Animal Protocol |
Mice (CD-1 nude) xenograft models of MKN45, U87MG, MDA-MB-231, COLO205, and A549 cells
20 mg/kg–60 mg/kg Orally |
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| References |
| Molecular Formula |
C26H20FN5O2S2
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| Molecular Weight |
517.60
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| Exact Mass |
517.10
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| Elemental Analysis |
C, 60.33; H, 3.89; F, 3.67; N,13.53; O, 6.18; S, 12.39
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| CAS # |
875337-44-3
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| Related CAS # |
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| Appearance |
Solid powder
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| SMILES |
CN1C=C(N=C1)C2=CC3=NC=CC(=C3S2)OC4=C(C=C(C=C4)NC(=S)NC(=O)CC5=CC=CC=C5)F
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| InChi Key |
UFICVEHDQUKCEA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C26H20FN5O2S2/c1-32-14-20(29-15-32)23-13-19-25(36-23)22(9-10-28-19)34-21-8-7-17(12-18(21)27)30-26(35)31-24(33)11-16-5-3-2-4-6-16/h2-10,12-15H,11H2,1H3,(H2,30,31,33,35)
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| Chemical 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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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.75 mg/mL (5.31 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 27.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.75 mg/mL (5.31 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 27.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.75 mg/mL (5.31 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9320 mL | 9.6600 mL | 19.3199 mL | |
| 5 mM | 0.3864 mL | 1.9320 mL | 3.8640 mL | |
| 10 mM | 0.1932 mL | 0.9660 mL | 1.9320 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
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