MKI-3 diformate
Based on 1 Customer Validation
MKI-3 diformate is a selective microtubule-associated serine/threonine kinase-like (MASTL) inhibitor with an IC50 of 5.72 nM and a Kd of 1.89 nM. MKI-3 diformate disrupts the MASTL-ENSA-Aurora A signaling axis. MKI-3 diformate induces chromosomal instability, mitotic catastrophe and apoptosis (apoptosis) in cancer cells. MKI-3 diformate is applicable to research related to triple-negative breast cancer.
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- Formel: C23H23N7O5
- Molecular Weight:477.47
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Speicherung:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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Biologische Aktivität
Beschreibung
In Vitro
MKI-3 diformate inhibits cellular MASTL activity with an IC50 of 114.9 nM[1].
MKI-3 (72 h) diformate inhibits proliferation of breast cancer cell lines 4T1, MCF7, MDA-MB-231, and BT549 with IC50 values of 42.01 nM, 93.61 nM, 91.44 nM, and 160.9 nM, respectively[1].
MKI-3 (250 nM; 12 h) diformate suppresses the MASTL-ENSA-Aurora A signaling axis, inducing apoptotic markers, in BT549 and 4T1 breast cancer cells[1].
MKI-3 diformate (250 nM; 24 h) activates PP2A in BT549 breast cancer cells[1].
MKI-3 (250 nM; 24 h) diformate induces mitotic defects including aberrant nuclear morphology, multipolar spindles, and centrosome abnormalities in BT549 breast cancer cells[1].
MKI-3 (250 nM; 48 h) diformate antiproliferative activity in BT549 breast cancer cells is mediated in part by PP2A activation, as co-treatment with 20 nM okadaic acid rescues cell viability[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Appearance Solid
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Molecular Weight 477.47
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Formel C23H23N7O5
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SMILES
NC(C1=CC=C(NC2=NC3=CC=CC=C3C(NC4=NNC(C5CC5)=C4)=N2)C=C1)=O.O=CO.O=CO
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Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : ≥ 100 mg/mL (209.44 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
Verweise
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0944 mL | 10.4719 mL | 20.9437 mL | 52.3593 mL |
| 5 mM | 0.4189 mL | 2.0944 mL | 4.1887 mL | 10.4719 mL | |
| 10 mM | 0.2094 mL | 1.0472 mL | 2.0944 mL | 5.2359 mL | |
| 15 mM | 0.1396 mL | 0.6981 mL | 1.3962 mL | 3.4906 mL | |
| 20 mM | 0.1047 mL | 0.5236 mL | 1.0472 mL | 2.6180 mL | |
| 25 mM | 0.0838 mL | 0.4189 mL | 0.8377 mL | 2.0944 mL | |
| 30 mM | 0.0698 mL | 0.3491 mL | 0.6981 mL | 1.7453 mL | |
| 40 mM | 0.0524 mL | 0.2618 mL | 0.5236 mL | 1.3090 mL | |
| 50 mM | 0.0419 mL | 0.2094 mL | 0.4189 mL | 1.0472 mL | |
| 60 mM | 0.0349 mL | 0.1745 mL | 0.3491 mL | 0.8727 mL | |
| 80 mM | 0.0262 mL | 0.1309 mL | 0.2618 mL | 0.6545 mL | |
| 100 mM | 0.0209 mL | 0.1047 mL | 0.2094 mL | 0.5236 mL |