Pifusertib
Based on 1 Customer Validation
Pifusertib (TAS-117) is a potent, selective, orally active allosteric Akt inhibitor (with IC50s of 4.8, 1.6, and 44 nM for Akt1, 2, and 3, respectively). Pifusertib triggers anti-myeloma activities and enhances fatal endoplasmic reticulum (ER) stress induced by proteasome inhibition. Pifusertib induces apoptosis and autophagy.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.81%
- No. CAS: 1402602-94-1
- Fòrmula: C26H24N4O2
- Peso molecular:424.49
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
Akt1 4.8 nM (IC50) |
Akt2 1.6 nM (IC50) |
Akt3 44 nM (IC50) |
In Vitro
Pifusertib (1 μM; 6 hours) blocks basal phosphorylation of Akt and downstream p-FKHR/FKHRL1 in MM cells with high baseline p-Akt[1].
Pifusertib (0-10 μM; 72 hours) selectively inhibits Akt and induces cytotoxicity in MM cells with high baseline phosphorylation of Akt[1].
Pifusertib abrogates the cytoprotective effect of the bone marrow microenvironment associated with Akt inhibition in both MM cells and BMSCs. Pifusertib enhances Carfilzomib-induced cytotoxicity and fatal ER stress in MM cells. Pifusertib (0.5, 1 μM) triggers G0/G1 arrest followed by apoptosis, associated with induction of autophagy and endoplasmic reticulum stress response[1].
Pifusertib enhances bortezomib-induced cytotoxicity, associated with increased CHOP (a fatal ER-stress marker) and PARP cleavage and blockade of bortezomib-induced p-Akt, suggesting that Pifusertib augments Bortezomib-induced ER stress and apoptotic signaling[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MM cell lines
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Concentration:0-10 μM
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Incubation Time:72 hours
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Result:Induced significant growth inhibition in MM cell lines with high baseline p-Akt, but not in cell lines with low baseline p-Akt.
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Cell Line:MM cell lines
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Concentration:0-10 μM
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Incubation Time:72 hours
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Result:Blocked basal phosphorylation of Akt and downstream p-FKHR/FKHRL1 in MM cells with high baseline p-Akt, but did not inhibit autophosphorylation of PDK1 which phosphorylates Akt at Thr308.
In Vivo
Pifusertib enhances bortezomib-induced MM cytotoxicity in vivo[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SCID mice (xenograft models bearing MM.1S cells)[1]
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Dosage:12, 16 mg/kg
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Administration:P.o.; daily for 5 days a week, 21 days
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Result:Significantly reduced MM.1S tumor growth versus vehicle control.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1402602-94-1
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Appearance Solid
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Peso molecular 424.49
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Fòrmula C26H24N4O2
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Color Off-white to light yellow
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SMILES
C[C@@](C1)(O)C[C@]1(N)C2=CC=C(C3=C(N(COC4=CC=NC=C45)C5=N3)C6=CC=CC=C6)C=C2
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Synonyms
TAS-117
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 50 mg/mL (117.79 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)
Pureza y Documentación
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Ficha de datos (275 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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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. 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 | 2.3558 mL | 11.7788 mL | 23.5577 mL | 58.8942 mL |
| 5 mM | 0.4712 mL | 2.3558 mL | 4.7115 mL | 11.7788 mL | |
| 10 mM | 0.2356 mL | 1.1779 mL | 2.3558 mL | 5.8894 mL | |
| 15 mM | 0.1571 mL | 0.7853 mL | 1.5705 mL | 3.9263 mL | |
| 20 mM | 0.1178 mL | 0.5889 mL | 1.1779 mL | 2.9447 mL | |
| 25 mM | 0.0942 mL | 0.4712 mL | 0.9423 mL | 2.3558 mL | |
| 30 mM | 0.0785 mL | 0.3926 mL | 0.7853 mL | 1.9631 mL | |
| 40 mM | 0.0589 mL | 0.2945 mL | 0.5889 mL | 1.4724 mL | |
| 50 mM | 0.0471 mL | 0.2356 mL | 0.4712 mL | 1.1779 mL | |
| 60 mM | 0.0393 mL | 0.1963 mL | 0.3926 mL | 0.9816 mL | |
| 80 mM | 0.0294 mL | 0.1472 mL | 0.2945 mL | 0.7362 mL | |
| 100 mM | 0.0236 mL | 0.1178 mL | 0.2356 mL | 0.5889 mL |
Pifusertib Related Classifications
HY-19934 Related Classifications
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