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Chemical Structure : EEDi-5285
CAS No.: 2488952-40-3
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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 2 mg | $288 | In stock | |
| 5 mg | $478 | In stock | |
| 10 mg | $758 | In stock | |
| 25 mg | Get quote | ||
| 50 mg | Get quote | ||
| 100 mg | Get quote |
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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.
| M.Wt | 479.53 | |
| Formula | C24H22FN5O3S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| 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 |
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1. Rohan Kalyan Rej, et al. J Med Chem. 2020 Jul 9;63(13):7252-7267.
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