培美曲塞二钠中间体
- CAS号:137281-23-3
- 英文名:Pemetrexed
- 中文名:培美曲塞二钠中间体
- CBNumber:CB00133895
- 分子式:C20H21N5O6
- 分子量:427.41
- MOL File:137281-23-3.mol
- 密度 :1.59±0.1 g/cm3(Predicted)
- 储存条件 :2-8°C(protect from light)
- 溶解度 :slightly sol. in Methanol
- 形态 :powder to crystal
- 酸度系数(pKa) :3.58±0.10(Predicted)
- 颜色 :White to Blue
- Merck :14,7077
- CAS 数据库 :137281-23-3(CAS DataBase Reference)
- RTECS号 :LZ9950100
- 海关编码 :2933.99.9701
- 毒害物质数据 :137281-23-3(Hazardous Substances Data)
培美曲塞二钠中间体性质、用途与生产工艺
- 生物活性 Pemetrexed (LY231514) 是一种叶酸拮抗剂 (antifolate)。Pemetrexed (LY231514) 抑制胸苷酸合成酶 (TS),二氢叶酸还原酶 (DHFR) 和甘氨酰胺核苷酸甲酰转移酶 (GARFT),Ki 分别为 1.3 nM,7.2 nM 和 65 nM。
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靶点
Ki: 1.3 nM (TS), 7.2 nM (DHFR), 65 nM (GARFT)
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体外研究
Pemetrexed (LY231514) disodium is a novel classical antifolate, the antitumor activity of which may result from simultaneous and multipie inhibition of several key folate-requiring enzymes via its polyglutamated metabolites. Pemetrexed (LY231514) is one of the best substrates that is known for the enzyme FPGS (K m =1.6 μM and V max /K m =621). It is likely that polyglutamation and the polyglutamated metabolites of LY231514 play profound roles in determining both the selectivity and the antitumor activity of this novel agent. Whereas LY23l5l4 only moderately inhibits TS (K i =340 nM, recombinant mouse), the pentaglutamate of LY23l5l4 is 100-fold more potent (K i =3.4 nM), making LY231514 one of the most potent folate-based TS inhibitors.
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体内研究
The group of mice treated with PC61 plus Pemetrexed demonstrates statistically longer survival than other groups. In a survival analysis, significantly better survival is observed in the group of mice treated with PC61 plus Pemetrexed compare with those treated with PC61 alone, rat IgG plus Pemetrexed, or no treatment.
- 更新日期:2024/08/19
- 产品编号:HY-10820
- 产品名称:培美曲塞二钠盐 Pemetrexed
- CAS编号:137281-23-3
- 包装:10mM * 1mLin DMSO
- 价格:770元
- 更新日期:2024/08/19
- 产品编号:HY-10820
- 产品名称:培美曲塞二钠盐 Pemetrexed
- CAS编号:137281-23-3
- 包装:50mg
- 价格:825元
- 公司名称:TCI Chemicals (India) Pvt. Ltd.
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