ETP-46321
Based on 1 Customer Validation
ETP-46321 is a potent and orally bioavailable PI3Kα and PI3Kδ inhibitor with Kiapps of 2.3 and 14.2 nM, respectively.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.34%
- No. CAS: 1252594-99-2
- Fòrmula: C20H27N9O3S
- Peso molecular:473.55
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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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
Actividad biológica
Descripciòn
IC50 & Target
[1]|
p110α 2.3 nM (Ki) |
PI3Kα-E545K 1.77 nM (Ki) |
PI3Kα-E542K 1.89 nM (Ki) |
PI3Kα-H1047R 2.33 nM (Ki) |
p110δ 14.2 nM (Ki) |
p110β 170 nM (Ki) |
p110γ 179 nM (Ki) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| U2OS | IC50 |
8.3 nM
Compound: 14, ETP-46321
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Inhibition of PI3Kalpha in human U2OS cells assessed as inhibition of AKT Ser 473 phosphorylation by Western blot
Inhibition of PI3Kalpha in human U2OS cells assessed as inhibition of AKT Ser 473 phosphorylation by Western blot
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[PMID: 22520259] |
In Vitro
ETP-46321 is selected to be screened against other PI3K isoforms. ETP-46321 is more potent against isoform α (Kiapp=2.3 nM). ETP-4632, has been profiled and shown to be a potent PI3K α and δ inhibitor, highly selective versus mTOR and 288 representative kinases. ETP-46321 is also tested against three of the p110α mutant enzymes detected in human cancers (E542K, E545K and H1047R), being equipotent against these mutants when compared to the wild type protein (Kiapp=2.33, 1.77 and 1.89 nM for PI3Kα-H1047R, PI3Kα-E545K and PI3Kα-E542K, respectively). ETP-46321 inhibits the phosphorilation of AKT in U2OS cell line with an IC50 of 8.3 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1252594-99-2
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Appearance Solid
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Peso molecular 473.55
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Fòrmula C20H27N9O3S
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Color White to off-white
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SMILES
NC(N=C1)=NC=C1C2=CN3C=C(CN4CCN(S(=O)(C)=O)CC4)N=C3C(N5CCOCC5)=N2
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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 2 years -20°C 1 year
Solvente y solubilidad
In Vitro:
DMSO : ≥ 33 mg/mL (69.69 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocolo
Animal Administration[1]
Mice[1]
BALB/C mice are treated daily with ETP-46321 (50 mg/kg, p.o.) for three weeks. Tumor volumes of four mice in each treatment group are measured and compared to the starting volume at the beginning of the treatment.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (274 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1117 mL | 10.5585 mL | 21.1171 mL | 52.7927 mL |
| 5 mM | 0.4223 mL | 2.1117 mL | 4.2234 mL | 10.5585 mL | |
| 10 mM | 0.2112 mL | 1.0559 mL | 2.1117 mL | 5.2793 mL | |
| 15 mM | 0.1408 mL | 0.7039 mL | 1.4078 mL | 3.5195 mL | |
| 20 mM | 0.1056 mL | 0.5279 mL | 1.0559 mL | 2.6396 mL | |
| 25 mM | 0.0845 mL | 0.4223 mL | 0.8447 mL | 2.1117 mL | |
| 30 mM | 0.0704 mL | 0.3520 mL | 0.7039 mL | 1.7598 mL | |
| 40 mM | 0.0528 mL | 0.2640 mL | 0.5279 mL | 1.3198 mL | |
| 50 mM | 0.0422 mL | 0.2112 mL | 0.4223 mL | 1.0559 mL | |
| 60 mM | 0.0352 mL | 0.1760 mL | 0.3520 mL | 0.8799 mL |
ETP-46321 Related Classifications
HY-12340 Related Classifications
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