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MKI-3

Chemical Structure : MKI-3

CAS No.: 3084702-28-0

MKI-3 (MASTL kinase inhibitor-3)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

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.

物理化学性质&存储条件

分子量 385.43
分子式 C21H19N7O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

4-((4-((5-Cyclopropyl-1H-pyrazol-3-yl)amino)quinazolin-2-yl)amino)benzamide

参考文献

1. Kim JI, et al. J Med Chem. 2026 Mar 19. doi: 10.1021/acs.jmedchem.5c03599.

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