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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:
AG 2037
- 库存:
货期:1-2天
- 供应商:
MedChemExpress LLC
- CAS号:
446022-33-9
- 规格:
10 mM * 1 mL/1 mg/5 mg
| 规格: | 10 mM * 1 mL | 产品价格: | ¥ |
|---|---|---|---|
| 规格: | 1 mg | 产品价格: | ¥2320.0 |
| 规格: | 5 mg | 产品价格: | ¥5800.0 |
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Pelitrexol
CAS No. : 446022-33-9
MCE 国际站:Pelitrexol
产品活性:Pelitrexol (AG 2037) 是甘氨酰胺核糖核苷酸甲酰转移酶 (GARFT) 的抑制剂。Pelitrexol 还通过降低 GTP 结合的 Rheb (mTORC1 专性激活剂) 水平来抑制 mTORC1。Pelitrexol 在小鼠模型中显示出强大的肿瘤生长抑制作用。
研究领域:Cell Cycle/DNA Damage
作用靶点:Antifolate
In Vitro: Pelitrexo (150 nM; 24 h) profoundly inhibits mTORC1 activity by reducing intracellular guanine nucleotides level as well as GTP-bound Rheb protein level in A549 cells.
Pelitrexo (0-1000 mM; 16 h) strongly inhibits the phosphorylation level of ribosomal protein S6 (S6RP), S6K1, and Chk1 in a dose-dependent manner in NCI-H460 cells.
Pelitrexo (100 nM; 48 h) arrests cell cycle at G1 phase in NCI-H460 cells.
In Vivo: Pelitrexo (10 mg/kg, 20 mg/kg; i.p.; every 4 days for 3 weeks) provokes both mTORC1 inhibition and robust tumor growth suppression in mice bearing nonsmall-cell lung cancer (NSCLC) xenografts.
Pelitrexo (20 mg/kg; i.p.; every 4 days for 3 weeks) inhibits GARFT-dependent purine biosynthesis and blocks mTORC1 function.
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