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MASTL inhibitor 15

Chemical Structure : MASTL inhibitor 15

CAS No.: 3024916-67-1

MASTL inhibitor 15

Catalog No.: PC-23350Not For Human Use, Lab Use Only.

MASTL inhibitor 15 is a potent, highly selective inhibitor of microtubule-associated serine/threonine kinase-like (MASTL, Greatwall) with Ki of <0.03 nM, cellular pENSA IC50 of 1.1 nM in MDA-MB-231 cells.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

MASTL inhibitor 15 is a potent, highly selective inhibitor of microtubule-associated serine/threonine kinase-like (MASTL, Greatwall) with Ki of <0.03 nM, cellular pENSA IC50 of 1.1 nM in MDA-MB-231 cells.
MASTL inhibitor 15 exhibits cellular pENSA IC50 of 4.6 nM in the MiaPaca2 cell line.
MASTL inhibitor 15 displays 420-fold selectivity over MAP4K4, and a sentinel kinase for flagging selectivity over other homologous kinases.
MASTL inhibitor 15 (15 and 30 mg/kg QD and 10 and 15 mg/kg BID, oral) exhibits dose-dependent inhibition of MiaPaca2 xenograft growth.

Physicochemical Properties

M.Wt 403.49
Formula C21H25N9
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N6-(4-(3-aminopentan-3-yl)pyridin-2-yl)-3-(1-methyl-1H-1,2,3-triazol-5-yl)-2,7-naphthyridine-1,6-diamine

References

1. Gallego RA, et al. J Med Chem. 2024 Nov 5. doi: 10.1021/acs.jmedchem.4c01659.

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