Home>>SJF620

SJF620 Sale

目录号 : GC61280

SJF620是一种PROTACBTK降解剂,DC50为7.9nM。SJF620含有Lenalidomide类似物,可募集CRBN。

SJF620 Chemical Structure

Cas No.:2376187-16-3

规格 价格 库存 购买数量
5mg
¥5,220.00
现货
10mg
¥8,820.00
现货
25mg
¥17,100.00
现货

电话:400-920-5774 Email: sales@glpbio.cn

Customer Reviews

Based on customer reviews.

Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

View current batch:

产品描述

SJF620 is a potent PROTAC BTK degrader with a DC50 of 7.9 nM. SJF620 contains a Lenalidomide analog for recruiting CRBN[1].

SJF620 is a PROTAC that retains potent degradation of BTK in cellular assays with a DC50 of 7.9 nM in Burkitt lymphoma cell line NAMALWA[1].

SJF620 has a super pharmacokinetic profile in mice (1 mg/kg; i.v.) with half life (t1/2) of 1.64 h. SJF620 exhibits a significantly better pharmacokinetic profile than MT802[1].

[1]. Jaime-Figueroa S, et al. Design, synthesis and biological evaluation of Proteolysis Targeting Chimeras (PROTACs) as a BTK degraders with improved pharmacokinetic properties. 2020 Feb 1;30(3):126877.

Chemical Properties

Cas No. 2376187-16-3 SDF
Canonical SMILES O=C(C(N(CC1=C2C=CC(OCCOCCOCCN3CCC(N4N=C(C5=CC=C(OC6=CC=CC=C6)C=C5)C7=C(N)N=CN=C74)CC3)=C1)C2=O)CC8)NC8=O
分子式 C41H44N8O7 分子量 760.84
溶解度 DMSO: 100 mg/mL (131.43 mM) 储存条件 -20°C, stored under nitrogen
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。
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。

溶解性数据

制备储备液
1 mg 5 mg 10 mg
1 mM 1.3143 mL 6.5717 mL 13.1434 mL
5 mM 0.2629 mL 1.3143 mL 2.6287 mL
10 mM 0.1314 mL 0.6572 mL 1.3143 mL
  • 摩尔浓度计算器

  • 稀释计算器

  • 分子量计算器

质量
=
浓度
x
体积
x
分子量
 
 
 
*在配置溶液时,请务必参考产品标签上、MSDS / COA(可在Glpbio的产品页面获得)批次特异的分子量使用本工具。

计算

动物体内配方计算器 (澄清溶液)

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
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

Research Update

Design, synthesis and biological evaluation of Proteolysis Targeting Chimeras (PROTACs) as a BTK degraders with improved pharmacokinetic properties

Bioorg Med Chem Lett 2020 Feb 1;30(3):126877.PMID:31879210DOI:PMC7318425

A new series of Proteolysis Targeting Chimeras (PROTACs) targeting Bruton's Tyrosine Kinase (BTK) was synthesized, with the goal of improving the pharmacokinetic properties of our previously reported PROTAC, MT802. We recently described the ability of MT802 to induce degradation of both wild-type and C481S mutant BTK in immortalized cells and patient-derived B-lymphocytes. However, the pharmacokinetic properties of MT802 were not suitable for further in vivo development. Therefore, we undertook a systematic medicinal chemistry campaign to overcome this issue and made a series of PROTACs with structural modifications to the linker and E3-recruiting ligand; more specifically, the new PROTACs were synthesized with different von Hippel-Lindau (VHL) and cereblon (CRBN) ligands while keeping the BTK ligand and linker length constant. This approach resulted in an equally potent PROTAC, SJF620, with a significantly better pharmacokinetic profile than MT802. This compound may hold promise for further in vivo exploration of BTK degradation.