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- 2025年12月05日
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- 详细信息
- 技术资料
- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 英文名：
KPT-9274
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
1643913-93-2
- 规格：
10 mM * 1 mL/1 mg/5 mg/10 mg/25 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥2418.0 |
|---|---|---|---|
| 规格： | 1 mg | 产品价格： | ￥700.0 |
| 规格： | 5 mg | 产品价格： | ￥1800.0 |
| 规格： | 10 mg | 产品价格： | ￥2900.0 |
| 规格： | 25 mg | 产品价格： | ￥4800.0 |
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Padnarsertib
CAS No. : 1643913-93-2
MCE 国际站：Padnarsertib
产品活性：Padnarsertib (KPT-9274) 是口服有效的 PAK4/烟酰胺磷酸核糖基转移酶 (Nampt) 抑制剂，IC50 分别 <100 和 125 nM。
研究领域：Cell Cycle/DNA Damage | Cytoskeleton | Metabolic Enzyme/Protease
In Vitro: 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.
In Vivo: Padnarsertib demonstrates a decrement of xenograft growth comparable with that of Sunitinib (HY-10255A). There are minimal Padnarsertib effects on the normal human RPTECs and no apparent toxicity in vivo.
Padnarsertib is currently being investigated in a phase I human clinical trial of patients with advanced solid malignancies and NHL.
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.
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