CC-885 |
| Katalog-Nr.GC18862 |
CC-885 ist ein Cereblon (CRBN)-Modulator mit starker Anti-Tumor-AktivitÄt.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1010100-07-8
Sample solution is provided at 25 µL, 10mM.
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CC-885 is a cereblon (CRBN) modulator with potent anti-tumour activity.
Acute myeloblatlic leukemia (AML) cell lines, human liver epithelial cell line (THLE-2) and human peripheral blood mononuclear cells (PBMC) are treated with varying concentrations of CC-885, with IC50s of 10×-6-1 μM. The effect of CC-885 on cell proliferation in AML cell lines, THLE-2 and human PBMC is more powerful than Lenalidomide and Pomalidomide with IC50s>10 μM. To address whether the cereblon-dependent degradation of GSPT1 is responsible for the cytotoxic effects of CC-885, a GSPT1 mutant that retains its normal function, but loses CC-885-dependent cereblon binding, is used to distinguish the role of GSPT1 from that of other substrates. CC-885 is tested in 293T HEK cells stably expressing the CC-885-sensitive or -resistant GSPT1 variants. Overexpression of a resistant variant GSPT1Δ(1–138)/(G575N) completely abrogate the CC-885-induced anti-proliferation, whereas overexpression of a CC-885-sensitive variant GSPT1Δ(1-138) only confer partial protection. Similar results are obtained in AML cell lines[1].
References:
[1]. Mary E. Matyskiela, et al. A novel cereblon modulator recruits GSPT1 to the CRL4CRBN ubiquitin ligase. Nature. 2016 Jul 14;535(7611):252-7.
Cell experiment: | Human cancer cell lines cultured in the growth medium are seeded into black 384-well plates containing DMSO or test compounds such as CC-885 (10×-6-1 μM). The seeding density for each cell line is optimized to allow the cell growth in the linear range during a 3-day culture period. To test the compound effect on cell proliferation in acute myeloid leukaemia (AML) cell lines, 5,000 to 10,000 cells per well in 200 μl complete culture media are seeded into black 96-well plates containing DMSO or test compounds such as CC-885. After 48 or 72 h, cell proliferation is assessed using the CellTiter-Glo (CTG) Luminescent Cell Viability Assay[1]. |
References: [1]. Mary E. Matyskiela, et al. A novel cereblon modulator recruits GSPT1 to the CRL4CRBN ubiquitin ligase. Nature. 2016 Jul 14;535(7611):252-7. | |
| Cas No. | 1010100-07-8 | SDF | |
| Chemical Name | N-(3-chloro-4-methylphenyl)-N'-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1-oxo-1H-isoindol-5-yl]methyl]-urea | ||
| Canonical SMILES | O=C1NC(CCC1N2C(C(C=CC(CNC(NC3=CC(Cl)=C(C)C=C3)=O)=C4)=C4C2)=O)=O | ||
| Formula | C22H21ClN4O4 | M.Wt | 440.9 |
| Löslichkeit | DMF: 12.5 mg/ml,DMSO: 12.5 mg/ml,DMSO:PBS(pH 7.2) (1:4): 0.2 mg/ml | 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 | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.2681 mL | 11.3404 mL | 22.6809 mL |
| 5 mM | 0.4536 mL | 2.2681 mL | 4.5362 mL |
| 10 mM | 0.2268 mL | 1.134 mL | 2.2681 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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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
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 21 reference(s) in Google Scholar.)
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