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Chemical Structure : CB5339
Catalog No.: PC-72409Not For Human Use, Lab Use Only.
CB5339 (CB-5339) is a second-generation, potent, selective, ATP-competitive, and oral inhibitor of valosin-containing protein (VCP/p97) with IC50 of 9 nM.
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CB5339 (CB-5339) is a second-generation, potent, selective, ATP-competitive, and oral inhibitor of valosin-containing protein (VCP/p97) with IC50 of 9 nM.
CB-5339 was 15-fold less active on the human cone PDE6 (PDE6C, IC50=3900 nM) in in vitro biochemical assays, and displayed a 31-times lower Cmax in vivo in rat retina compared to CB-5083.
CB5339 demonstrated growth inhibition against a panel of 16 AML cell lines and a panel of 16 primary AML patient samples harboring diverse genetic backgrounds (mean IC50 =375 nM).
CB5339 was validated in multiple AML models, including syngeneic and patient-derived xenograft murine models.
CB-5339 treatment synergizes to impair leukemic growth in an MLL-AF9-driven AML murine model when combined with DNA-damaging agents anthracyclines.
| M.Wt | 412.497 | |
| Formula | C24H24N6O | |
| Appearance | Solid | |
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1. Blandine Roux, et al. Sci Transl Med. 2021 Mar 31;13(587):eabg1168.
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