EEDi-5285
目录号 : GC67934EEDi-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。
Cas No.:2488952-40-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
IC50: 0.2 nM (Embryonic ectoderm development (EED))[1]
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].
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[1].
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. |
[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.
| Cas No. | 2488952-40-3 | SDF | Download SDF |
| 分子式 | C24H22FN5O3S | 分子量 | 479.53 |
| 溶解度 | DMSO : 125 mg/mL (260.67 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
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.PMID:32580550DOI:PMC8859984
Inhibition of embryonic ectoderm development (EED) is a new cancer therapeutic strategy. Herein, we report our discovery of EEDi-5285 as an exceptionally potent, efficacious, and orally active EED inhibitor. EEDi-5285 binds to the EED protein with an IC50 value of 0.2 nM and 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 approximately 100 times more potent than EED226 in binding to EED and >300 times more potent than EED226 in inhibition of cell growth in the KARPAS422 cell line. EEDi-5285 has excellent pharmacokinetics and achieves complete and durable tumor regression in the KARPAS422 xenograft model in mice with oral administration. The cocrystal structure of EEDi-5285 in a complex with EED defines the precise structural basis for their high binding affinity. EEDi-5285 is the most potent and efficacious EED inhibitor reported to date.