EEDi-5285|cas:2488952-40-3|西域试剂

EEDi-5285,98.66%

产品编号：Bellancom-136977| CAS NO：2488952-40-3| 分子式：C₂₄H₂₂FN₅O₃S| 分子量：479.53

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-136977		￥5800.00	杭州北京（现货）
Bellancom-136977		￥9800.00	杭州北京（现货）

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EEDi-5285

产品介绍

EEDi-5285 是一种非常有效且具有口服活性的胚胎外胚层发育 (EED) 抑制剂，结合 EED 蛋白的 IC₅₀ 值为 0.2 nM，并具有抗癌活性。

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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 C_max 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 T_1/2 of approximately 2 h.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 125 mg/mL (260.67 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0854 mL	10.4269 mL	20.8538 mL
5 mM	0.4171 mL	2.0854 mL	4.1708 mL
10 mM	0.2085 mL	1.0427 mL	2.0854 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式