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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Purity: ≥98%
MPI-0479605 (MPI0479605; MPI 0479605) is an ATP-competitive and selective inhibitor of mitotic kinase Mps1 (Monopolar spindle1) with potential antineoplastic activity. It inhibits Mps1 with an IC50 of 1.8 nM, and shows >40-fold selectivity over other closely related kinases.
ln Vitro |
MPI-0479605, having an IC50 of 1.8 nM, is a strong and specific ATP-competitive inhibitor of Mps1. HCT-116 cell viability is dose-dependently lowered by MPI-0479605 (0.1–10 μM). While causing full cytokinesis, MPI-0479605 exhibits severe defects in chromosome alignment at the metaphase plate[1].
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ln Vivo |
In HCT-116 xenografts, MPI-0479605 (30 mg/kg daily or 150 mg/kg every fourth day (Q4D), ip) suppresses tumor development by 49% and 74%. On the Colo-205 xenografts, MPI-0479605 does not exhibit inhibitory action when dosed daily; in contrast, dosing every four days results in 63% tumor growth inhibition (TGI)[1].
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Animal Protocol |
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References |
[1]. Tardif KD, et al. Characterization of the cellular and antitumor effects of MPI-0479605, a small-molecule inhibitor of the mitotic kinase Mps1. Mol Cancer Ther. 2011 Dec;10(12):2267-2275
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Molecular Formula |
C22H29N7O
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Molecular Weight |
407.51
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CAS # |
1246529-32-7
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SMILES |
CC(C=C(N1CCOCC1)C=C2)=C2NC3=NC4=C(N=CN4)C(NC5CCCCC5)=N3
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InChi Key |
OVJBNYKNHXJGSA-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C22H29N7O/c1-15-13-17(29-9-11-30-12-10-29)7-8-18(15)26-22-27-20-19(23-14-24-20)21(28-22)25-16-5-3-2-4-6-16/h7-8,13-14,16H,2-6,9-12H2,1H3,(H3,23,24,25,26,27,28)
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Chemical Name |
N6-cyclohexyl-N2-(2-methyl-4-morpholinophenyl)-9H-purine-2,6-diamin
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Synonyms |
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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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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.4539 mL | 12.2696 mL | 24.5393 mL | |
5 mM | 0.4908 mL | 2.4539 mL | 4.9079 mL | |
10 mM | 0.2454 mL | 1.2270 mL | 2.4539 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.
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