| Identification | Back Directory | [Name]
8-(6-cyclopropylpyridin-3-yl)-N-((5-fluoro-2,3-dihydrobenzofuran-4-yl)methyl)-1-(methylsulfonyl)imidazo[1,5-c]pyrimidin-5-amine | [CAS]
2488952-40-3 | [Synonyms]
8-(6-cyclopropylpyridin-3-yl)-N-((5-fluoro-2,3-dihydrobenzofuran-4-yl)methyl)-1-(methylsulfonyl)imidazo[1,5-c]pyrimidin-5-amine | [Molecular Formula]
C24H22FN5O3S | [MDL Number]
MFCD33029305 | [MOL File]
2488952-40-3.mol | [Molecular Weight]
479.53 |
| Chemical Properties | Back Directory | [density ]
1.56±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 125 mg/mL (260.67 mM; Need ultrasonic) | [form ]
Solid | [pka]
2.80±0.24(Predicted) |
| Hazard Information | Back Directory | [Uses]
EEDi-5285 is an exceptionally potent and orally active embryonic ectoderm development (EED) inhibitor with an IC50 value of 0.2 nM for binds to the EED protein. EEDi-5285 has anti-cancer activity[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[1].
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[1].
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]. | Animal Model: | SCID mice injected with KARPAS422 cells[1] | | Dosage: | 50 mg/kg, 100 mg/kg | | Administration: | Oral gavage; daily; for 28 days | | Result: | Showed highly efficacious and capable of achieving complete and long-lasting tumor regression in the KARPAS422 xenograft model in mice with oral administration.
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| [References]
[1] Rohan Kalyan Rej, et al. EEDi-5285: An Exceptionally Potent, Efficacious, and Orally Active Small-Molecule Inhibitor of Embryonic Ectoderm Development. J Med Chem. 2020 Jul 9;63(13):7252-7267. DOI:10.1021/acs.jmedchem.0c00479 |
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