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Chemical Structure : DSP-5336
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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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.
| M.Wt | 419.41 | |
| Formula | C20H20F3N5O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Ken Eguchi, et al. Blood, Volume 138, Supplement 1, 23 November 2021, Page 3339
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