MKI-3
MKI-3 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 disrupts the MASTL-ENSA-Aurora A signaling axis. MKI-3 induces chromosomal instability, mitotic catastrophe and apoptosis (apoptosis) in cancer cells. MKI-3 is applicable to research related to triple-negative breast cancer.
For research use only. We do not sell to patients.
- CAS No.: 3084702-28-0
- Formula: C21H19N7O
- Molecular Weight:385.42
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
In Vitro
MKI-3 inhibits cellular MASTL activity with an IC50 of 114.9 nM[1].
MKI-3 (72 h) 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) suppresses the MASTL-ENSA-Aurora A signaling axis, inducing apoptotic markers, in BT549 and 4T1 breast cancer cells[1].
MKI-3 (250 nM; 24 h) activates PP2A in BT549 breast cancer cells[1].
MKI-3 (250 nM; 24 h) induces mitotic defects including aberrant nuclear morphology, multipolar spindles, and centrosome abnormalities in BT549 breast cancer cells[1].
MKI-3 (250 nM; 48 h) 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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CAS No. 3084702-28-0
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Molecular Weight 385.42
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Formula C21H19N7O
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SMILES
O=C(C1=CC=C(NC2=NC3=CC=CC=C3C(NC4=NNC(C5CC5)=C4)=N2)C=C1)N
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent & Solubility
In Vitro:
DMSO : 1.25 mg/mL (3.24 mM; ultrasonic and adjust pH to 3 with Formic acid; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
DMSO : 0.33 mg/mL (0.86 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
Purity & Documentation
References
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5946 mL | 12.9729 mL | 25.9457 mL | 64.8643 mL |