GNE-502
目录号 : GC65590
GNE-502 是一种口服有效的雌激素受体 (ER) 降解剂。GNE-502 可用于乳腺癌研究。
Cas No.:1953134-16-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
GNE-502 is an orally active and potent degrader for estrogen receptor (ER). GNE-502 can be used for the research of breast cancer[1].
GNE-502 (10 and 100 mg/kg; p.o.) possesses sufficient oral exposure to be tested in a WT MCF7 tumor xenograft model[1].GNE-502 shows dose dependent tumor growth inhibition at 10 mg/kg and 30 mg/kg, with tumor stasis at 100 mg/kg[1].
[1]. Zbieg JR, et al. Discovery of GNE-502 as an Orally Bioavailable and Potent Degrader for Estrogen Receptor Positive Breast Cancer [published online ahead of print, 2021 Aug 20]. Bioorg Med Chem Lett. 2021;128335.
| Cas No. | 1953134-16-1 | SDF | Download SDF |
| 分子式 | C25H30FN3O3S | 分子量 | 471.59 |
| 溶解度 | DMSO : 100 mg/mL (212.05 mM; Need ultrasonic) | 储存条件 | 4°C, protect from light |
| 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 | 2.1205 mL | 10.6024 mL | 21.2049 mL |
| 5 mM | 0.4241 mL | 2.1205 mL | 4.241 mL |
| 10 mM | 0.212 mL | 1.0602 mL | 2.1205 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。
Discovery of GNE-502 as an orally bioavailable and potent degrader for estrogen receptor positive breast cancer
Bioorg Med Chem Lett 2021 Oct 15;50:128335.PMID:34425201DOI:10.1016/j.bmcl.2021.128335
Fulvestrant is an FDA-approved drug with a dual mechanism of action (MOA), acting as a full antagonist and degrader of the estrogen receptor protein. A significant limitation of fulvestrant is the dosing regimen required for efficacy. Due to its high lipophilicity and poor pharmacokinetic profile, fulvestrant needs to be administered through intramuscular injections which leads to injection site soreness. This route of administration also limits the dose and target occupancy in patients. We envisioned a best-in-class molecule that would function with the same dual MOA as fulvestrant, but with improved physicochemical properties and would be orally bioavailable. Herein we report our progress toward that goal, resulting in a new lead GNE-502 which addressed some of the liabilities of our previously reported lead molecule GNE-149.