GDC-2992
Based on 1 Customer Validation
GDC-2992 (Compound 28A) is an orally bioavailable androgen receptor (AR) PROTAC degrader. GDC-2992 degrads AR with a DC50 value of 2.7 nM and inhibits proliferation with an IC50 valude of 9.7 nM in VCaPcells. GDC-2992 can be used for prostatic cancer study.
(Pink: Androgen Receptor ligand (HY-130845); Blue: Cereblon ligand (HY-W1003189A); Black: linker (HY-169975)).
For research use only. We do not sell to patients.
- Purity: 99.38%
- CAS No.: 2753651-10-2
- Formula: C45H51ClN8O5
- Molecular Weight:819.39
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Storage:Powder -20°C, 3 years , 4°C, 2 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
GDC-2992 (RO7656594) inhibits AR signaling by binding to both AR and the E3 ubiquitin ligase cereblon (CRBN), resulting in ubiquitination and subsequent degradation of AR[2].
GDC-2992 inhibits AR signaling in the context of wild-type AR and AR proteins with mutations associated with resistance to standard-of-care AR signaling inhibitors (ARSIs)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | T1/2 | Plasma Concentration | AUC | Bioavailability |
|---|---|---|---|---|---|---|
| Dog | 10 mg/kg | p.o. | 34.3 h | 868 ng/mL | 15420 ng·h/mL | 33.9 % |
| Rat | 10 mg/kg | p.o. | 8.28 h | 173 ng/mL | 3212 ng·h/mL | 5.13 % |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2753651-10-2
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Appearance Solid
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Molecular Weight 819.39
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Formula C45H51ClN8O5
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Color Light yellow to brown
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SMILES
N#CC1=CC=C(O[C@H]2C(C)(C)[C@H](NC(C3=CC=C(N4CCC(CN5CCN(C6=CC(C=NN([C@@H]7C(NC(CC7)=O)=O)C8=O)=C8C=C6)CC5)CC4)C=C3)=O)C2(C)C)C=C1Cl
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Synonyms
RO7656594
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 50 mg/mL (61.02 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 (269 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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 | 1.2204 mL | 6.1021 mL | 12.2042 mL | 30.5105 mL |
| 5 mM | 0.2441 mL | 1.2204 mL | 2.4408 mL | 6.1021 mL | |
| 10 mM | 0.1220 mL | 0.6102 mL | 1.2204 mL | 3.0511 mL | |
| 15 mM | 0.0814 mL | 0.4068 mL | 0.8136 mL | 2.0340 mL | |
| 20 mM | 0.0610 mL | 0.3051 mL | 0.6102 mL | 1.5255 mL | |
| 25 mM | 0.0488 mL | 0.2441 mL | 0.4882 mL | 1.2204 mL | |
| 30 mM | 0.0407 mL | 0.2034 mL | 0.4068 mL | 1.0170 mL | |
| 40 mM | 0.0305 mL | 0.1526 mL | 0.3051 mL | 0.7628 mL | |
| 50 mM | 0.0244 mL | 0.1220 mL | 0.2441 mL | 0.6102 mL | |
| 60 mM | 0.0203 mL | 0.1017 mL | 0.2034 mL | 0.5085 mL |
GDC-2992 Related Classifications
HY-156751A Related Classifications
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