Golcadomide
Based on 1 Customer Validation
Golcadomide (CC-99282) is a blood-brain barrier-permeable, orally active Cereblon (CRBN) E3 ligase modulator. Golcadomide induces Cereblon to form a closed active conformation, thereby recruiting and triggering the ubiquitin-mediated proteasomal degradation of transcription factors IKZF1, IKZF3, Ikaros and Aiolos. Golcadomide is applicable to research related to relapsed or refractory non-Hodgkin lymphoma, chronic lymphocytic leukemia/small lymphocytic lymphoma, and diffuse large B-cell lymphoma.
For research use only. We do not sell to patients.
- Purity : 98.04%
- CAS No.: 2379572-34-4
- Formula: C28H30FN5O5
- Molecular Weight:535.57
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
[1]|
Cereblon |
IKZF1 |
IKZF3 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| THLE-2 | IC50 |
>25 μM
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Cytotoxicity against non-malignant THLE-2 epithelial cells assessed via dose-response assays.
Cytotoxicity against non-malignant THLE-2 epithelial cells assessed via dose-response assays.
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41182271 |
| PBMC | IC50 |
>10 μM
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Cytotoxicity against healthy human PBMCs assessed via dose-response assays.
Cytotoxicity against healthy human PBMCs assessed via dose-response assays.
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41182271 |
In Vitro
Golcadomide (24 h) induces significant degradation of IKZF1 and IKZF3 in a panel of expanded T-cell lymphoma cell lines. Specifically, after 24 h of treatment, IKZF1 is almost completely degraded in ATL-3I and MT-2 cells, with the degradation rate of IKZF3 reaching approximately 80%[1].
Golcadomide enhances Rituximab-mediated NK cell ADCC and macrophage ADCP by up to 20% in FL and DLBCL cell lines[3].
Golcadomide induces rapid and complete degradation of ePL-tagged IKZF1 and IKZF3 in DF-15 cells[4].
Golcadomide (100 nM; 48 hours) induces more than 79% degradation of IKZF1/3 in all tested DLBCL cell lines, and differences in the level of apoptosis are observed between sensitive and drug-resistant cell lines[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
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Cell Line:DLBCL cell lines
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Concentration:100 nM
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Incubation Time:48 hours
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Result:Induced deep IKZF1/3 degradation (>79% at 100 nM for 48 hours) in all cell lines examined.
Cleaved Caspase-3 positivity ranged from 51.62% to 0.56% following treatment, with variability between sensitive and resistant lines.
In Vivo
Golcadomide (0.3-1 mg/kg) enables up to 100% of follicular lymphoma xenograft mice to achieve a tumor-free state by day 40, and in the 1 mg/kg treatment group, combined treatment with Rituximab (HY-P9913) maintains the 100% tumor-free state until day 106[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Immunocompromised mice[4]
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Dosage:30 mg/kg; 10 mg/kg; 3 mg/kg
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Administration:p.o.
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Result:Was detected in brain tissue.
Induced rapid depletion of IKZF1 and IKZF3 proteins in brain tumor tissues.
Reduced tumor burden by 99.5%, 99.1%, and 97.2% at doses of 30, 10, and 3 mg/kg respectively by day 26.
Significantly improved survival compared to vehicle and pomalidomide.
Did not produce meaningful changes in body weight.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2379572-34-4
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Appearance Solid
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Molecular Weight 535.57
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Formula C28H30FN5O5
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Color Light yellow to yellow
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SMILES
FC(C=C(C=C1)CN2CC(N3CCOCC3)C2)=C1CNC4=C5C(C(N([C@]6([H])C(NC(CC6)=O)=O)C5=O)=O)=CC=C4
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Synonyms
CC-99282
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 125 mg/mL (233.40 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (290 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8672 mL | 9.3358 mL | 18.6717 mL | 46.6792 mL |
| 5 mM | 0.3734 mL | 1.8672 mL | 3.7343 mL | 9.3358 mL | |
| 10 mM | 0.1867 mL | 0.9336 mL | 1.8672 mL | 4.6679 mL | |
| 15 mM | 0.1245 mL | 0.6224 mL | 1.2448 mL | 3.1119 mL | |
| 20 mM | 0.0934 mL | 0.4668 mL | 0.9336 mL | 2.3340 mL | |
| 25 mM | 0.0747 mL | 0.3734 mL | 0.7469 mL | 1.8672 mL | |
| 30 mM | 0.0622 mL | 0.3112 mL | 0.6224 mL | 1.5560 mL | |
| 40 mM | 0.0467 mL | 0.2334 mL | 0.4668 mL | 1.1670 mL | |
| 50 mM | 0.0373 mL | 0.1867 mL | 0.3734 mL | 0.9336 mL | |
| 60 mM | 0.0311 mL | 0.1556 mL | 0.3112 mL | 0.7780 mL | |
| 80 mM | 0.0233 mL | 0.1167 mL | 0.2334 mL | 0.5835 mL | |
| 100 mM | 0.0187 mL | 0.0934 mL | 0.1867 mL | 0.4668 mL |
Golcadomide Related Classifications
HY-146237 Related Classifications
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