Flonoltinib TFA
Based on 1 publication(s) in Google Scholar
Flonoltinib TFA is a potent and orally active dual JAK2/FLT3 inhibitor with IC50 values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3, respectively. Flonoltinib TFA has anti-cancer activity.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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: 98.04%
- CAS 番号: 2928093-29-0
- 分子式: C27H35F4N7O3
- 分子量:581.61
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保管条件:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
MedChemExpress(MCE)の使用を引用している文献 Flonoltinib TFA
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生物活性
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JAK1 26 nM (IC50) |
JAK2 0.7 nM (IC50) |
JAK3 39 nM (IC50) |
FLT3 4 nM (IC50) |
Flonoltinib (0.008-1 μM; for 2 hours) TFA down-regulates p-FLT3 in a dose-dependent manner[1].
Flonoltinib (5-100 nM; for 2 hours) TFA has a dose-dependent effect on the induction of apoptosis in the MV4-11 cells[1].
Flonoltinib (5-100 nM; for 2 hours) TFA strongly induces cell cycle arrest with a G1/G0 percentage of 85% at 100 nM in the MV4-11 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MV4-11 and SET-2 cells
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Concentration:0.008, 0.04, 0.2, 1 μM
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Incubation Time:For 2 hours
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Result:Down-regulated p-FLT3 in a dose-dependent manner from 0.008 to 1 μM.
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Cell Line:MV4-11 cells
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Concentration:5, 10, 50, 100 nM
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Incubation Time:For 2 hours
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Result:Had a dose-dependent effect on the induction of apoptosis in the MV4-11 cells.
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Cell Line:MV4-11 cells
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Concentration:5, 10, 50, 100 nM
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Incubation Time:For 2 hours
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Result:Induced cell cycle arrest with a G1/G0 percentage of 85% at 100 nM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD/SCID mouse models[1]
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Dosage:30 and 60 mg/kg
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Administration:Oral administration; daily; for 14 days
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Result:Exhibited significant antitumor effects.
The tumor growth inhibitory rates (TGI) were respective 58% and 93% in the MV4-11-bearing mice model.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 2928093-29-0
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性状 Solid
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分子量 581.61
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分子式 C27H35F4N7O3
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Color Yellow to orange
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SMILES
OCCN(C1CCN(C2=CC=C(NC3=NC=C(C)C(C4=CN(C(C)C)N=C4)=N3)C=C2F)CC1)C.O=C(O)C(F)(F)F
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別名
JAK2/FLT3-IN-1 TFA
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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, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
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J Immunol
Tumor Environment Promotes Lnc57Rik-Mediated Suppressive Function of Myeloid-Derived Suppressor Cells. [Abstract]2022 Oct 1;209(7):1401-1413. PMID: 36038289
溶剤 & 溶解度
H2O : 33.33 mg/mL (57.31 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (275 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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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 (sealed storage, away from moisture). 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 |
|---|---|---|---|---|---|
| H2O | 1 mM | 1.7194 mL | 8.5968 mL | 17.1937 mL | 42.9841 mL |
| 5 mM | 0.3439 mL | 1.7194 mL | 3.4387 mL | 8.5968 mL | |
| 10 mM | 0.1719 mL | 0.8597 mL | 1.7194 mL | 4.2984 mL | |
| 15 mM | 0.1146 mL | 0.5731 mL | 1.1462 mL | 2.8656 mL | |
| 20 mM | 0.0860 mL | 0.4298 mL | 0.8597 mL | 2.1492 mL | |
| 25 mM | 0.0688 mL | 0.3439 mL | 0.6877 mL | 1.7194 mL | |
| 30 mM | 0.0573 mL | 0.2866 mL | 0.5731 mL | 1.4328 mL | |
| 40 mM | 0.0430 mL | 0.2149 mL | 0.4298 mL | 1.0746 mL | |
| 50 mM | 0.0344 mL | 0.1719 mL | 0.3439 mL | 0.8597 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.