Mps1-IN-6
Mps1-IN-6 is a potent Mps1 inhibitor with an IC50 value of 2.596 nM. Mps1-IN-6 shows antiproliferative activity. Mps1-IN-6 shows antitumor activity.
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- CAS No.: 3043761-59-4
- Formule: C35H39N9O3
- Masse moléculaire:633.74
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
IC50: 2.596 nM (Mps1)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HT-29 | IC50 |
>10 μM
Compound: 31
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Antiproliferative activity against human HT-29 cells assessed inhibition of cell growth incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human HT-29 cells assessed inhibition of cell growth incubated for 72 hrs by CCK-8 assay
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[PMID: 37037136] |
| MCF7 | IC50 |
>10 μM
Compound: 31
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Antiproliferative activity against human MCF7 cells assessed inhibition of cell growth incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human MCF7 cells assessed inhibition of cell growth incubated for 72 hrs by CCK-8 assay
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[PMID: 37037136] |
| MDA-MB-468 | IC50 |
0.221 μM
Compound: 31
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Antiproliferative activity against human MDA-MB-468 cells assessed inhibition of cell growth incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human MDA-MB-468 cells assessed inhibition of cell growth incubated for 72 hrs by CCK-8 assay
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[PMID: 37037136] |
| MV4-11 | IC50 |
0.823 μM
Compound: 31
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Antiproliferative activity against human MV4-11 cells assessed inhibition of cell growth incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human MV4-11 cells assessed inhibition of cell growth incubated for 72 hrs by CCK-8 assay
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[PMID: 37037136] |
Mps1-IN-6 (compound 31) (0-10 µM; 72 h) shows antiproliferative activity with IC50s of 0.221, >10, >10, 0.823, >10 µM for MDA-MB-468, MCF-7, REB, MV4-11, HT-29 cells, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-468, MCF-7, REB, MV4-11, HT-29 cells
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Concentration:0-10 µM
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Incubation Time:72 h
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Result:Showed antiproliferative activity with IC50s of 0.221, >10, >10, 0.823, >10 µM for MDA-MB-468, MCF-7, REB, MV4-11, HT-29 cells, respectively.
Pharmacokinetic Parameters of Mps1-IN-6 in Male Sprague-Dawley rats[1].
| parameters (unit) | iv (2 mg/kg) | po (10 mg/kg) |
| C0 (ng/mL) | 5237 | - |
| Cmax (ng/mL) | 2920 | 160 |
| T1/2 (h) | 0.825 | 1.05 |
| Tmax (h) | 0.083 | 0.333 |
| AUC(0-t) (h*ng/mL) | 1050 | 204 |
| AUC(0-∞) (h*ng/mL) | 1052 | 208 |
| MRT(0-t) (h) | 0.34 | 1.11 |
| MRT(0-∞) (h) | 0.354 | 1.23 |
| CL (mL/kg/min) | 32 | - |
| Vss (L/kg) | 0.672 | - |
| F % | - | 3.95 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Six to eight week-old female BALB/c nude mice (MDA-MB-468 mouse xenograft model)[1]
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Dosage:30, 60 mg/kg
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Administration:I.v.; once daily for 21 days
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Result:Inhibited the tumor growth with TGI values of 21%, 34% for 30, 60 mg/kg, respectively.
Chemical Information
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CAS No. 3043761-59-4
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Masse moléculaire 633.74
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Formule C35H39N9O3
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SMILES
CCC1=CC=CC(CC)=C1N2CCN3C=C(C=C3C2=O)C4=C5C=NNC5=NC(NC6=C(C=C(C=C6)N7CCN(CC7)C(C)=O)OC)=N4
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Mps1-IN-6 Related Classifications
HY-149959 Related Classifications
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