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EEDi-5285

Chemical Structure : EEDi-5285

CAS No.: 2488952-40-3

EEDi-5285 (EEDi5285)

Catalog No.: PC-72488Not For Human Use, Lab Use Only.

EEDi-5285 (EEDi5285) is a highly potent, efficacious, and orally active EED inhibitor with IC50 of 0.2 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

EEDi-5285 (EEDi5285) is a highly potent, efficacious, and orally active PRC2 EED inhibitor with IC50 of 0.2 nM.
EEDi-5285 inhibits cell growth with IC50 values of 20 pM and 0.5 nM in the Pfeiffer and KARPAS422 lymphoma cell lines, respectively, carrying an EZH2 mutation.
EEDi-5285 is approximately 100 times more potent than EED226 in binding to EED and >300 times more potent than EED226 in inhibition of cell growth in the KARPAS422 cell line.
EEDi-5285 has excellent pharmacokinetics and achieves complete and durable tumor regression in the KARPAS422 xenograft model in mice with oral administration, achieved complete tumor regression at 50 mg/kg.

Physicochemical Properties

M.Wt 479.53
Formula C24H22FN5O3S
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

8-(6-Cyclopropylpyridin-3-yl)-N-((5-fluoro-2,3-dihydrobenzofuran-4-yl)methyl)-1-(methylsulfonyl)imidazo[1,5-c]pyrimidin-5-amine

References

1. Rohan Kalyan Rej, et al. J Med Chem. 2020 Jul 9;63(13):7252-7267.

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