ON 146040
Based on 1 Customer Validation
ON 146040 is a potent PI3Kα and PI3Kδ (IC50≈14 and 20 nM, respectively) inhibitor. ON 146040 also inhibits Abl1 (IC50<150 nM).
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 95.05%
- CAS 番号: 1404231-34-0
- 分子式: C24H23N7O3S
- 分子量:489.55
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保管条件:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
生物活性
製品説明
IC50 & Target
[1]|
PI3Kα 14 nM (IC50) |
PI3Kδ 20 nM (IC50) |
PI3Kγ 1 μM (IC50) |
PI3Kβ 3 μM (IC50) |
体外実験
In biochemical testing, ON 146040 inhibits PI3Kα/ PI3Kδ isoforms (IC50≈14 and 20 nM, respectively) without having a major effect on PI3Kβ/ PI3Kγ isoforms (IC50≈3 and 1 μM, respectively). ON 146040 is also found to inhibit Abl1 and several mutant versions of this kinase (IC50<150 nM), although ON 146040 is not found to be active against the T315I mutant. ON 146040 represents the first dual PI3K and BCR-ABL inhibitor that targets the STAT3 and STAT5 pathways. ON 146040 disrupts the oncogenic activity of both STAT3 and STAT5 by targeting upstream activators, including PI3K α and δ isoforms as well as wild type and mutant BCR-ABL. ON 146040 is highly potent in killing hematologic tumor cells with IC50 values in the 150 to 1,000 nM range. Following treatment with ON 146040, STAT3 and STAT5 phosphorylation are down-regulated in leukemia and myeloma cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
化学情報
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CAS 番号 1404231-34-0
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性状 Solid
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分子量 489.55
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分子式 C24H23N7O3S
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Color Brown to reddish brown
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SMILES
CN(CC1)CCN1C(C=C2)=CC=C2NC3=NC(S/C(C(N4)=O)=C\C5=CC=C([N+]([O-])=O)C=C5)=C4C=N3
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶剤 & 溶解度
体外:
DMSO : 25 mg/mL (51.07 mM; ultrasonic and warming and heat to 60°C; 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). 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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (273 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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取扱説明書 (2659 KB)
参考文献
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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0427 mL | 10.2135 mL | 20.4269 mL | 51.0673 mL |
| 5 mM | 0.4085 mL | 2.0427 mL | 4.0854 mL | 10.2135 mL | |
| 10 mM | 0.2043 mL | 1.0213 mL | 2.0427 mL | 5.1067 mL | |
| 15 mM | 0.1362 mL | 0.6809 mL | 1.3618 mL | 3.4045 mL | |
| 20 mM | 0.1021 mL | 0.5107 mL | 1.0213 mL | 2.5534 mL | |
| 25 mM | 0.0817 mL | 0.4085 mL | 0.8171 mL | 2.0427 mL | |
| 30 mM | 0.0681 mL | 0.3404 mL | 0.6809 mL | 1.7022 mL | |
| 40 mM | 0.0511 mL | 0.2553 mL | 0.5107 mL | 1.2767 mL | |
| 50 mM | 0.0409 mL | 0.2043 mL | 0.4085 mL | 1.0213 mL |