keep away from direct sunlight
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 187.00 | |
5 mg | In stock | $ 478.00 | |
10 mg | In stock | $ 689.00 | |
25 mg | In stock | $ 1,080.00 | |
50 mg | In stock | $ 1,480.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 558.00 |
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. |
Targets&IC50 | EED:0.2 nM (IC50) |
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]. |
Synonyms | UM-EEDi-5285, EEDI5285 |
Molecular Weight | 479.53 |
Formula | C24H22FN5O3S |
CAS No. | 2488952-40-3 |
keep away from direct sunlight
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 112.5 mg/mL (234.6 mM), Sonication is recommended.
You can also refer to dose conversion for different animals. More
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
EEDi-5285 2488952-40-3 Chromatin/Epigenetic Histone Methyltransferase UM-EEDi-5285 EEDI5285 EEDI 5285 inhibitor inhibit