PROTAC NAMPT Degrader-30
Based on 1 Customer Validation
PROTAC NAMPT Degrader-30 is a fluorescent PROTAC, which efficiently degrades NAMPT with an IC50 of 41.9 nM. PROTAC NAMPT Degrader-30 binds to NAMPT and VHL to form a ternary complex and subsequently induced NAMPT degradation via ubiquitin-proteasome system (UPS). PROTAC NAMPT Degrader-30 leads to significant reduction of NAD+ and exerts potent antitumor activities.
For research use only. We do not sell to patients.
- Purity: 99.41%
- CAS No.: 3035008-40-0
- Formula: C59H73N9O7S
- Molecular Weight:1052.33
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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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Metabolism/Protease Compound Library
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Biological Activity
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VHL |
NAMPT 41.9 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A2780 | IC50 |
100 nM
Compound: B4
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Cytotoxicity against human A2780 cells assessed as cell growth inhibition incubated for 72 hrs in presence of (2S,4R)-1-(2-amino-3,3-dimethyl-butanoyl)-4-hydroxy-N-[(1S)-1-[4-(4-methylthiazol-5-yl)phenyl]ethyl]pyrrolidine-2-carboxamide by CCK-8 assay
Cytotoxicity against human A2780 cells assessed as cell growth inhibition incubated for 72 hrs in presence of (2S,4R)-1-(2-amino-3,3-dimethyl-butanoyl)-4-hydroxy-N-[(1S)-1-[4-(4-methylthiazol-5-yl)phenyl]ethyl]pyrrolidine-2-carboxamide by CCK-8 assay
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[PMID: 36442664] |
| A2780 | IC50 |
12.1 nM
Compound: B4
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Cytotoxicity against human A2780 cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay
Cytotoxicity against human A2780 cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay
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[PMID: 36442664] |
PROTAC NAMPT Degrader-30 (Compound B4; 30 nM; 24 h) is able to degrade NAMPT with a DC50 value of 8.4 nM. PROTAC NAMPT Degrader-30 enables the visualization of degradation in A2780 cells[1].
PROTAC NAMPT Degrader-30 (Compound B4) shows the best antitumor activity in suppression of the proliferation in A2780 cells (IC50 = 12.1 nM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A2780 cells
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Concentration:30 nM
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Incubation Time:24 h
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Result:Were able to degrade NAMPT in A2780 cells at the concentration of 30 nM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/C nude female mice (4-5 weeks of age, 14-18 g) injected with A2780 cells[1]
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Dosage:10 mg/kg, 30 mg/kg
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Administration:i.p; once a day; for 14 consecutive days
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Result:Achieved excellent antitumor effects in a dose-dependent manner.
Chemical Information
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CAS No. 3035008-40-0
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Appearance Solid
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Molecular Weight 1052.33
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Formula C59H73N9O7S
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Color Light yellow to yellow
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SMILES
O=C(C(C1=CC=C(C=C1)C(NCC2=CN=CC=C2)=O)=NC3=C4C=C(C=C3)NC(CCCCCCCCCCC(N[C@@H](C(C)(C)C)C(N5C[C@H](O)C[C@H]5C(N[C@@H](C)C6=CC=C(C7=C(C)N=CS7)C=C6)=O)=O)=O)=O)N4CCC
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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 : 100 mg/mL (95.03 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 (271 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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 | 0.9503 mL | 4.7514 mL | 9.5027 mL | 23.7568 mL |
| 5 mM | 0.1901 mL | 0.9503 mL | 1.9005 mL | 4.7514 mL | |
| 10 mM | 0.0950 mL | 0.4751 mL | 0.9503 mL | 2.3757 mL | |
| 15 mM | 0.0634 mL | 0.3168 mL | 0.6335 mL | 1.5838 mL | |
| 20 mM | 0.0475 mL | 0.2376 mL | 0.4751 mL | 1.1878 mL | |
| 25 mM | 0.0380 mL | 0.1901 mL | 0.3801 mL | 0.9503 mL | |
| 30 mM | 0.0317 mL | 0.1584 mL | 0.3168 mL | 0.7919 mL | |
| 40 mM | 0.0238 mL | 0.1188 mL | 0.2376 mL | 0.5939 mL | |
| 50 mM | 0.0190 mL | 0.0950 mL | 0.1901 mL | 0.4751 mL | |
| 60 mM | 0.0158 mL | 0.0792 mL | 0.1584 mL | 0.3959 mL | |
| 80 mM | 0.0119 mL | 0.0594 mL | 0.1188 mL | 0.2970 mL |
PROTAC NAMPT Degrader-30 Related Classifications
HY-152154 Related Classifications
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