产品
编 号：F741629
分子式：C24H22FN5O3S
分子量：479.53
分子式：C24H22FN5O3S
分子量：479.53
产品类型
规格
价格
是否有货
5mg
询价
询价
10mg
询价
询价
结构图
CAS No: 2488952-40-3
产品详情
生物活性：
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.
体内研究：
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.Animal Model:SCID mice injected with KARPAS422 cells
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.
体外研究：
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 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.
体内研究：
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.Animal Model:SCID mice injected with KARPAS422 cells
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.
体外研究：
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.
产品资料
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