DSP-5336 | menin-MLL inhibitor | Probechem Biochemicals

Chemical Structure : DSP-5336

DSP-5336 (DSP5336)

Catalog No.: PC-22768Not For Human Use, Lab Use Only.

DSP-5336 is a potent, and orally bioavailable menin-MLL interaction inhibitor with IC50 of 1.4 nM, directly binds to the menin protein with Kd of 6 nM.

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Biological Activity

DSP-5336 is a potent, and orally bioavailable menin-MLL interaction inhibitor with IC50 of 1.4 nM, directly binds to the menin protein with Kd of 6 nM.
DSP-5336 selectively inhibited the cell growth of human leukemia cell lines including MV-4-11, MOLM-13, KOPN-8, and OCI-AML3 (IC 50 = 10, 15, 31 and 15 nM, respectively).
DSP-5336 did not affect the cell growth of human leukemia cell lines such as HL-60, MOLT-4, and Reh (IC50>10 uM), which do not have MLL-r or NPM1 mutations.
DSP-5336 exhibited a signicant antitumor activity at the doses of 25 mg/kg and 50 mg/kg, administered twice daily (BID) for 20 days, mouse xenograft model using MV-4-11 cells, which express MLL-AF4.

Physicochemical Properties

M.Wt	419.41
Formula	C20H20F3N5O2
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	(R)-2-(((3-cyclobutyl-5-(3,4,5-trifluorophenoxy)-3H-imidazo[4,5-b]pyridin-2-yl)methyl)amino)propanamide

References

1. Ken Eguchi, et al. Blood, Volume 138, Supplement 1, 23 November 2021, Page 3339

DSP-5336 (DSP5336)

Biological Activity

Physicochemical Properties

References

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