Iberdomide

目录号: GC19195纯度: >98.50%同义词: CC-220
A cereblon modulator

Iberdomide
Cas No.: 1323403-33-3
规格价格库存数量操作
1mg¥277.00现货
1
2mg¥385.00现货
1
5mg¥770.00现货
1
10mg¥1,190.00现货
1
25mg¥2,450.00现货
1
50mg¥3,920.00现货
1
10mM (in 1mL DMSO)¥762.00现货
1

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产品描述 Description

Iberdomide (CC-220) is a cereblon modulator with an IC50 of 60 nM.

Lenalidomide and pomalidomide, targeting cereblon, are immunomodulatory drugs that are clinically effective in the treatment of cancer, including newly diagnosed and relapsed multiple myeloma. Iberdomide contains a glutarimide ring that binds in the try-tryptophan pocket of cereblon and an isoindolinone ring that can interact with both cereblon and substrates. Treatment with Iberdomide results in the loss of Ikaros and Aiolos protein levels with EC50s of 1 nM and 0.5 nM [1].

Iberdomide (CC-220) is currently in phase 2 clinical trials for the treatment of systematic lupus erythematosus (SLE) and phase 1b/2a clinical trials for relapsed and refractory multiple myeloma (MM)[1].

References:
[1]. Matyskiela ME, et al. A Cereblon Modulator (CC-220) with Improved Degradation of Ikaros and Aiolos. J Med Chem. 2017 Apr 20.

实验参考方法 Experimental Reference Method

Kinase experiment:

Iberdomide is dissolved in DMSO. In the assay, 60 nM 6Xhis-tagged CRBN-DDB1 is combined with 30 nM cy5-conjugated cereblon modulator and 3 nM LanthaScreen Eu-anti-His Tag antibody in 20 mM HEPES pH 7, 150 mM NaCl, 0.005% Tween-20 assay buffer. FRET is observed by exciting at 340 nm and monitoring emission at 615 nm and 665 nm, and FRET efficiency is determined by the ratio of FRET to non-FRET emission. Competing cereblon modulating compound (Iberdomide) or DMSO carrier is titrated and incubated for 10 min before scanning[1].

References:

[1]. Matyskiela ME, et al. A Cereblon Modulator (CC-220) with Improved Degradation of Ikaros and Aiolos. J Med Chem. 2017 Apr 20.

产品文档 Product Documents

Purity:>98.50%

化学性质Chemical Properties

CAS 号
1323403-33-3
同义词
CC-220
SMILES
O=C([C@@H](N(CC1=C2C=CC=C1OCC3=CC=C(CN4CCOCC4)C=C3)C2=O)CC5)NC5=O
分子式
C25H27N3O5
分子量
449.5 g/mol
溶解性
DMSO : ≥ 30 mg/mL (66.74 mM)
保存条件
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°C,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。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol