Size | Price | |
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100mg | ||
250mg | ||
500mg | ||
Other Sizes |
Targets |
IC50: 29 nM (Mps1)[1]
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ln Vitro |
Compound 12 (Mps1-IN-5) (0-10 µM, 24, 48, 72 h) blocks MCF-7 and 4T1 cell proliferation in a time-dependent way[1].
Mps1-IN-5 (0, 0.5, 1.0, 5.0 µM; 24, 48 h) induces apoptosis and cell cycle arrest in the G2/M phase in MCF-7 and 4T1 cells in a dose-dependent way[1]. Mps1-IN-5 (0, 0.03, 0.1, 1, 3 µM; 2 h) causes DNA damage and inhibits Mps1 phosphorylation[1]. |
ln Vivo |
In breast cancer models, Mps1-IN-5 (30, 60 mg/kg; po; daily for 15 days) reduces tumor growth without clearly visible damage [1].
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Cell Assay |
Cell Proliferation Assay[1]
Cell Types: MDA-MB-231, MCF-7, 4T1, HEY, OVCAR- 3, ES-2, HCT-116, A549, AGS cells Tested Concentrations: 0-3 µM Incubation Duration: 72 h Experimental Results: Inhibited the cell growth with IC50s of 2.68, 0.37, 0.40, >3, >3, >3, 1.06, 2.03, >3 µM for MDA-MB-231, MCF-7, 4T1, HEY, OVCAR-3, ES-2, HCT-116, A549, AGS cells, respectively. Cell Cycle Analysis[1] Cell Types: MCF -7, 4T1 cells Tested Concentrations: 0, 0.5, 1.0, 5.0 µM Incubation Duration: 24 h Experimental Results: Induced cell cycle arrest of MCF-7 and 4T1 cells at the G2/M phase in a dose-dependent manner, diminished the protein expression levels of Cyclin B1 and CDK1. Apoptosis Analysis[1] Cell Types: MCF-7, 4T1 cells Tested Concentrations: 0, 0.5, 1.0, 5.0 µM Incubation Duration: 48 h Experimental Results: Induced apoptosis and Dramatically increased the expression level of an apoptosis- related protein, cleaved poly ADP-ribose polymerase (PARP). Western Blot Analysis[1] Cell Types: MCF-7, 4T1 cells Tested Concentrations: 0, 0.03, 0.1, 1, 3 µM Incubation Duration: 2 h Experimental Results: Increased the expression of level of γ-H2AX protein and diminished the protein expression of p-Mps1 in a dose-dependent manner. |
Animal Protocol |
Animal/Disease Models: 6-8 weeks, female balb/c (Bagg ALBino) mouse: (4T1-luc mouse xenograft model)[1]
Doses: 30, 60 mg/kg Route of Administration: Po; daily for 15 days Experimental Results: Dramatically suppressed tumor growth and caused negligible damage to organs such as heart, liver, spleen, lung and kidneys. |
References |
[1]. Li X, et al. Design, synthesis and biological evaluation of a new class of 7H-pyrrolo[2,3-d]pyrimidine derivatives as Mps1 inhibitors for the treatment of breast cancer. Eur J Med Chem. 2023 Jan 5;245(Pt 1):114887.
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Molecular Formula |
C24H25N9
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Molecular Weight |
439.52
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CAS # |
2890819-31-3
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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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 |
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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.2752 mL | 11.3760 mL | 22.7521 mL | |
5 mM | 0.4550 mL | 2.2752 mL | 4.5504 mL | |
10 mM | 0.2275 mL | 1.1376 mL | 2.2752 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.