PROTAC CYP1B1 degrader-1
Based on 1 publication(s) in Google Scholar
PROTAC CYP1B1 degrader-1 is a CYP1B1 PROTAC degrader with a human IC50 of 95.1 nM. PROTAC CYP1B1 degrader-1 induces concentration-dependent CYP1B1 degradation. PROTAC CYP1B1 degrader-1 can be used for the research of CYP1B1-mediated Docetaxel (HY-B0011)-resistant prostate cancer.
(Pink: CYP1B1 Target protein ligand; Blue: Cereblon ligand (HY-103596); Black: linker).
For research use only. We do not sell to patients.
- Purity: 98.26%
- CAS No.: 2411389-67-6
- Formula: C43H39N5O10
- Molecular Weight:785.80
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications Citing Use of MedChemExpress (MCE) PROTAC CYP1B1 degrader-1
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Biological Activity
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Cereblon |
CYP1B1 |
PROTAC CYP1B1 degrader-1 (Compound 6C) inhibits recombinant human CYP1B1 with an IC50 of 95.1 nM and shows 103.5-fold selectivity over recombinant human CYP1A2[1].
PROTAC CYP1B1 degrader-1 (5 μM) induces robust, concentration- and time-dependent degradation of CYP1B1 protein in CYP1B1-overexpressing DU145/CY human prostate cancer cells, reducing CYP1B1 levels to ~0.3-fold of control levels[1].
PROTAC CYP1B1 degrader-1 (up to 10 μM; 48 h) is non-toxic to CYP1B1-overexpressing DU145/CY human prostate cancer cells, with an IC50 >50 μM[1].
PROTAC CYP1B1 degrader-1 (5 μM; 48 h) reverses docetaxel resistance in CYP1B1-overexpressing DU145/CY human prostate cancer cells, reducing the docetaxel IC50 to 7.01 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:CYP1B1-overexpressing DU145/CY human prostate cancer cells
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Concentration:up to 10 μM
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Incubation Time:48 h
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Result:Showed no cytotoxicity against DU145/CY cells, with an IC50 value greater than 50 μM.
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Cell Line:CYP1B1-overexpressing DU145/CY human prostate cancer cells
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Concentration:5 μM
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Incubation Time:48 h
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Result:Reduced the IC50 of docetaxel in DU145/CY cells from 43.25 nM to 7.01 nM, a level comparable to the docetaxel IC50 in parental DU145 cells (4.95 nM).
Chemical Information
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CAS No. 2411389-67-6
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Appearance Solid
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Molecular Weight 785.80
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Formula C43H39N5O10
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Color Light yellow to yellow
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SMILES
COC1=CC=C(C2=C3OC(C4=CC=C(C=C4)C5=CN(N=N5)CCCCCCOC6=CC=CC7=C6C(N(C7=O)C8CCC(NC8=O)=O)=O)=CC(C3=CC(OC)=C12)=O)OC
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (1)
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Journal Impact Factor
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Most Recent
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Neoplasia
CYP1B1 promotes angiogenesis and sunitinib resistance in clear cell renal cell carcinoma via USP5-mediated HIF2α deubiquitination. [Abstract]2025 Aug:66:101186. PMID: 40435846
Solvent & Solubility
DMF : 10 mg/mL (12.73 mM; Need ultrasonic)
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 (protect from light). 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 (protect from light). 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 (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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 (protect from light). 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 |
|---|---|---|---|---|---|
| DMF | 1 mM | 1.2726 mL | 6.3629 mL | 12.7259 mL | 31.8147 mL |
| 5 mM | 0.2545 mL | 1.2726 mL | 2.5452 mL | 6.3629 mL | |
| 10 mM | 0.1273 mL | 0.6363 mL | 1.2726 mL | 3.1815 mL |