PHTPP-1304
Based on 1 Customer Validation
PHTPP-1304 is a PHTPP-based autophagy targeting chimera (AUTOTAC). PHTPP-1304 induces the degradation of estrogen receptor ERβ through the autophagy pathway, rather than ubiquitination (DC50 ≈ 2 nM, in HEK293T cells; < 100 nM in ACHN renal carcinoma and MCF-7 breast cancer cells). PHTPP-1304 can induce the self-oligomerization of p62. PHTPP-1304 can be used to study various cancers mediated by ERβ.
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- Pureza: 99.96%
- No. CAS: 2410081-60-4
- Fòrmula: C51H50F6N4O7
- Peso molecular:944.96
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Almacenamiento:
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Actividad biológica
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ERβ 2 nM (DC50) |
PHTPP-1304 (0.5-10 μM, 24 h) induces the formation of p62+ERβ+ puncta that are affected by autophagic flux in a dose-dependent manner in ACHN cells[1].
PHTPP-1304 (0.01-100 μM) has cytotoxicity against ACHN cells (IC50 = 3.3 μM), and can effectively inhibit the migration of cancer cells[1].
PHTPP-1304 (0.5 μM, 24 h) exhibits a 10-fold stronger inhibitory effect on ERβ downstream signaling (EGFR, p-ERK/ERK, p-Akt/Akt) in estrogen (E2)-stimulated LNCaP cells compared to PHTPP alone[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LNCaP cells with or without E2 (10 nM)
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Concentration:0.5 μM
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Incubation Time:24 h
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Result:Inhibited ERβ signaling 10-folds more efficiently than its TBL as determined by the levels of EGFR, p-ERK/ERK and p-Akt/Akt in E2-stimulated LNCaP cells.
Chemical Information
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No. CAS 2410081-60-4
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Appearance Solid
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Peso molecular 944.96
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Fòrmula C51H50F6N4O7
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Color Light yellow to yellow
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SMILES
O[C@H](CNCCOCCOCCOC1=CC=C(C2=C3N(C(C(F)(F)F)=CC(C(F)(F)F)=N3)N=C2C4=CC=CC=C4)C=C1)COC5=CC(OCCCC6=CC=CC=C6)=C(OCC7=CC=CC=C7)C=C5
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Solvente y solubilidad
DMSO : 110 mg/mL (116.41 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 (protect from light, stored under nitrogen). 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, stored under nitrogen). 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)
Pureza y Documentación
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Ficha de datos (271 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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Instrucciones de manejo (2659 KB)
Referencias
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, stored under nitrogen). 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 | 1.0582 mL | 5.2912 mL | 10.5825 mL | 26.4561 mL |
| 5 mM | 0.2116 mL | 1.0582 mL | 2.1165 mL | 5.2912 mL | |
| 10 mM | 0.1058 mL | 0.5291 mL | 1.0582 mL | 2.6456 mL | |
| 15 mM | 0.0705 mL | 0.3527 mL | 0.7055 mL | 1.7637 mL | |
| 20 mM | 0.0529 mL | 0.2646 mL | 0.5291 mL | 1.3228 mL | |
| 25 mM | 0.0423 mL | 0.2116 mL | 0.4233 mL | 1.0582 mL | |
| 30 mM | 0.0353 mL | 0.1764 mL | 0.3527 mL | 0.8819 mL | |
| 40 mM | 0.0265 mL | 0.1323 mL | 0.2646 mL | 0.6614 mL | |
| 50 mM | 0.0212 mL | 0.1058 mL | 0.2116 mL | 0.5291 mL | |
| 60 mM | 0.0176 mL | 0.0882 mL | 0.1764 mL | 0.4409 mL | |
| 80 mM | 0.0132 mL | 0.0661 mL | 0.1323 mL | 0.3307 mL | |
| 100 mM | 0.0106 mL | 0.0529 mL | 0.1058 mL | 0.2646 mL |