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Cereblon modulator 1
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Cereblon modulator 1图片
CAS NO:1860875-51-9
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
Cereblon modulator 1 (CC-90009) 是一流的 GSPT1 选择性 cereblon (CRBN) E3 连接酶调节剂,用作分子胶。
Cas No.1860875-51-9
别名CC-90009
Canonical SMILESO=C(NCC1=CC2=C(C(N(C(CC3)C(NC3=O)=O)C2)=O)C=C1)C(F)(F)C4=CC=C(Cl)C=C4
分子式C22H18ClF2N3O4
分子量461.85
溶解度DMSO: 250 mg/mL (541.30 mM)
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Cereblon modulator 1 (compound F) is a cereblon (CRBN) E3 ligase modulator. Cereblon modulator 1 specifically binds to CRBN, thereby affecting the activity of the ubiquitin E3 ligase complex. This leads to the ubiquitination of certain substrate proteins and induces the proteasome-mediated degradation of certain transcription factors, including Ikaros (IKZF1) and Aiolos (IKZF3)[1][2].

A different CRBN-binding compound, Cereblon modulator 1 (compound F), that demonstrates anti-proliferative activity in non-AML hematological cancer cell lines (such as multiple myeloma) does not inhibit cell growth in any of the 11 AML cell lines tested, including the ten cell lines that are sensitive to the growth inhibitory activity of Compound D. However, when excess Cereblon modulator 1 is added to KG-1 AML cell cultures in the presence of Compound D, the anti-proliferative activity of Compound D is reduced, presumably due to competition for binding of Compound D to CRBN. The relative impact of Cereblon modulator 1 on the anti-proliferative effect of Compound D progressively increased with increasing concentrations of Cereblon modulator 1. In the presence of 100 µμ Cereblon modulator 1, the potency of Compound D in inhibiting cell growth reduced by approximately 60-fold, and the potency of Compound D in inducing apoptosis reduced by approximately 40-fold[1].

[1]. Ellen Filvaroff, et al. Methods for treating cancer and the use of biomarkers as a predictor of clinical sensitivity to therapies. WO2017120446A1. [2]. CC-90009