Chemical Structure : MKI-3
CAS No.:
3084702-28-0
MKI-3
(MASTL kinase inhibitor-3)
Catalog No.: PC-26420Not For Human Use, Lab Use Only.
MKI-3 (MASTL kinase inhibitor-3) is a potent and selective MASTL (Greatwall kinase) inhibitor with IC50 of 5.72 nM, binds to MASTL with BLI KD of 1.89 nM.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
MKI-3 (MASTL kinase inhibitor-3) is a potent and selective MASTL (Greatwall kinase) inhibitor with IC50 of 5.72 nM, binds to MASTL with BLI KD of 1.89 nM.
MKI-3 selectively inhibits MASTL over other AGC kinases, including large tumor suppressor kinase 1 (LATS1), LATS2, RSK, PDK1, PKA, PKC alpha, and Rho-associated coiled-coil containing protein kinase 1.
MKI-3 demonstrates strong suppression of pENSA with an IC50 of 341 nM.
MKI-3 inhibits viability of various breast cancer cell lines, including MCF7, MDA-MB231, BT549, and murine 4T1 cells.
MKI-3 (250 nM) exerts potent antitumor activity in breast cancer cells by inhibiting the MASTL-ENSA-Aurora A pathway, thereby inducing fatal CIN and mitotic catastrophe.
MKI-3 (8 mg/kg) effectively suppresses tumor growth in 4T1 triple-negative breast cancer (TNBC) model.
Physicochemical Properties
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M.Wt
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385.43
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Formula
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C21H19N7O
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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4-((4-((5-Cyclopropyl-1H-pyrazol-3-yl)amino)quinazolin-2-yl)amino)benzamide
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References
1. Kim JI, et al. J Med Chem. 2026 Mar 19. doi: 10.1021/acs.jmedchem.5c03599.
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