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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $187 | Backorder | |
5 mg | $478 | Backorder | |
10 mg | $689 | Backorder | |
25 mg | $1,080 | Backorder | |
50 mg | $1,480 | Backorder | |
1 mL x 10 mM (in DMSO) | $558 | Backorder |
Description | EEDi-5285, an orally active and highly potent inhibitor targeting embryonic ectoderm development (EED) protein, exhibits anti-cancer activity. It demonstrates exceptional efficacy with an IC50 value of 0.2 nM, indicating robust binding affinity to the EED protein. |
In vitro | EEDi-5285 effectively suppresses cell proliferation in lymphoma cell lines Pfeiffer and KARPAS422, which possess an EZH2 mutation, demonstrating inhibition concentrations (IC50) of 20 pM and 0.5 nM, respectively[1]. |
In vivo | EEDi-5285 (compound 28; 50-100 mg/kg; oral gavage; daily; for 28 days; SCID mice) treatment achieves complete and durable tumor regression in the KARPAS422 xenograft model in mice with oral administration. A single 100 mg/kg oral administration of EEDi-5285 (compound 28) effectively reduces the level of H3K27me3 at 24 h in KARPAS422 tumor tissue in mice. EEDi-5285 (compound 28) achieves a Cmax of 1.8 μM and an AUC of 6.0 h▪μg/ml with 10 mg/kg oral administration and has an oral bioavailability (F) of 75%. EEDi-5285 has a moderate volume of distribution of 1.4 L/kg and a terminal T1/2 of approximately 2 h[1]. |
Alias | UM-EEDi-5285, EEDI5285 |
Molecular Weight | 479.53 |
Formula | C24H22FN5O3S |
Cas No. | 2488952-40-3 |
Storage | keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 112.5 mg/mL (234.6 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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