Padnarsertib
Based on 3 publication(s) in Google Scholar
Padnarsertib (KPT-9274) is an orally bioavailable, dual PAK4/Nicotinamide phosphoribosyltransferase (Nampt) inhibitor, with IC50s of <100 nM and 120 nM, respectively.
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: 99.58%
- CAS 番号: 1643913-93-2
- 分子式: C35H29F3N4O3
- 分子量:610.63
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保管条件: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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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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MedChemExpress（MCE）の使用を引用している文献 Padnarsertib
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Bio/Physico-chemical Assay
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Flow Cytometry
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Cell Proliferation/Viability Assay
生物活性
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PAK4 100 nM (IC50) |
Nampt 120 nM (IC50) |
Padnarsertib attenuates the PAK4/β-catenin pathway, results in NAD depletion, and attenuates viability, invasion, and migration in several RCC cell lines. Inhibition of NAMPT in a cell-free enzymatic assay using recombinant NAMPT shows an IC50 of approximately 120 nM for Padnarsertib. Padnarsertib attenuates G2–M transit and induces apoptosis in RCC cell lines[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Padnarsertib is currently being investigated in a phase I human clinical trial of patients with advanced solid malignancies and NHL[2].
Padnarsertib (oral administation; 100mg/kg or 200 mg/kg; twice a day; 14 days) demonstrates a decrement of xenograft growth without no significant weight loss. 8 hours after, Padnarsertib are measured at the end of the experiment in mouse plasma and tumors with 10757 ng/mL and 10647 ng/mL, respectively[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mice[1]
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Dosage:100mg/kg or 200 mg/kg
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Administration:Oral administation; 100mg/kg or 200 mg/kg; twice a day; 14 days
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Result:Showed a significant decrease of xenograft growth in KPT-9274 treated mouse.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1643913-93-2
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性状 Solid
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分子量 610.63
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分子式 C35H29F3N4O3
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Color White to light yellow
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SMILES
FC(C=C1)=CC=C1C2=C(OC(CNC(/C=C/C3=CN=C(N)C=C3)=O)=C4)C4=CC(C5=CC=C(C(N6CCC(F)(F)CC6)=O)C=C5)=C2
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別名
KPT-9274
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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J Exp Clin Cancer Res
CYP3A5 promotes glioblastoma stemness and chemoresistance through fine-tuning NAD+/NADH ratio. [Abstract]2025 Jan 3;44(1):3. PMID: 39754188
Padnarsertib purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2025 Jan 3;44(1):3. [Abstract]
Padnarsertib (KPT-9274) (0.25 μM) led to the mitigation of the facilitating effect of CYP3A5 overexpression on the neurosphere number in GSCs.
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Adv Sci (Weinh)
Functional Phosphoproteomics in Cancer Chemoresistance Using CRISPR-Mediated Base Editors. [Abstract]2022 Oct;9(30):e2200717. PMID: 36045417
Padnarsertib purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2022 Oct;9(30):e2200717. [Abstract]
Apoptotic analysis of Hct116 cells treated with Padnarsertib (KPT-9274; PAK4i) (2-10 μM).
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Biochim Biophys Acta Mol Basis Dis
Metabolic reprogramming represents a targetable mechanism to overcome acquired resistance to venetoclax in acute myeloid leukemia. [Abstract]2026 Jan;1872(1):168065. PMID: 41043531
Padnarsertib purchased from MedChemExpress. Usage Cited in: Biochim Biophys Acta Mol Basis Dis. 2026 Jan;1872(1):168065. [Abstract]
Padnarsertib (KPT-9274) (50-200 nM; 72 h) enhanced venetoclax-induced cell death in MV4-11VR and MOLM- 13VR cells.
溶剤 & 溶解度
DMSO : 100 mg/mL (163.77 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, 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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.08 mg/mL (3.41 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (3.41 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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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取扱説明書 (2659 KB)
参考文献
[1]. WO2015003166A1
[2]. Abu Aboud O, et al. Dual and Specific Inhibition of NAMPT and PAK4 By KPT-9274 Decreases Kidney Cancer Growth. Mol Cancer Ther. 2016 Sep;15(9):2119-29. [Content Brief]
[3]. Abu Aboud O, et al. Dual and Specific Inhibition of NAMPT and PAK4 By KPT-9274 Decreases Kidney Cancer Growth.Mol Cancer Ther. 2016 Sep;15(9):2119-29. [Content Brief]
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 |
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| DMSO | 1 mM | 1.6377 mL | 8.1883 mL | 16.3765 mL | 40.9413 mL |
| 5 mM | 0.3275 mL | 1.6377 mL | 3.2753 mL | 8.1883 mL | |
| 10 mM | 0.1638 mL | 0.8188 mL | 1.6377 mL | 4.0941 mL | |
| 15 mM | 0.1092 mL | 0.5459 mL | 1.0918 mL | 2.7294 mL | |
| 20 mM | 0.0819 mL | 0.4094 mL | 0.8188 mL | 2.0471 mL | |
| 25 mM | 0.0655 mL | 0.3275 mL | 0.6551 mL | 1.6377 mL | |
| 30 mM | 0.0546 mL | 0.2729 mL | 0.5459 mL | 1.3647 mL | |
| 40 mM | 0.0409 mL | 0.2047 mL | 0.4094 mL | 1.0235 mL | |
| 50 mM | 0.0328 mL | 0.1638 mL | 0.3275 mL | 0.8188 mL | |
| 60 mM | 0.0273 mL | 0.1365 mL | 0.2729 mL | 0.6824 mL | |
| 80 mM | 0.0205 mL | 0.1024 mL | 0.2047 mL | 0.5118 mL | |
| 100 mM | 0.0164 mL | 0.0819 mL | 0.1638 mL | 0.4094 mL |
Padnarsertib 関連分類
HY-12793 関連分類
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