Cereblon modulator 1 (Synonyms: CC-90009) |
| カタログ番号GC60688 |
セレブロン モジュレーター 1 (CC-90009) は、クラス初の GSPT1 選択的セレブロン (CRBN) E3 リガーゼ モジュレーターであり、分子接着剤として機能します。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1860875-51-9
Sample solution is provided at 25 µL, 10mM.
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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
| Cas No. | 1860875-51-9 | SDF | |
| 同義語 | CC-90009 | ||
| Canonical SMILES | O=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 | ||
| Formula | C22H18ClF2N3O4 | M.Wt | 461.85 |
| 溶解度 | DMSO: 250 mg/mL (541.30 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1652 mL | 10.826 mL | 21.6521 mL |
| 5 mM | 0.433 mL | 2.1652 mL | 4.3304 mL |
| 10 mM | 0.2165 mL | 1.0826 mL | 2.1652 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 22 reference(s) in Google Scholar.)
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