培美曲塞二鈉鹽

生物活性靶點體外研究體內(nèi)研究 用途與合成方法 MSDS 培美曲塞二鈉鹽價格(試劑級) 上下游產(chǎn)品信息 專題

中文名稱	培美曲塞二鈉鹽
中文同義詞	培美曲塞酸;二鈉培美曲塞;N-[4-[2-(2-氨基-4,7-二氫-4-氧代-3H-吡咯并[2,3-D]嘧啶-5-基)乙基]苯甲酰基]-L-谷氨酸;培美曲唑;N-[4-[2-(2-氨基-4,7-二氫-4-氧代-1H-吡咯并[2,3-D]嘧啶-5-基)乙基]苯甲?；鵠-L-谷氨酸;培美曲塞酸 (N-(4-[2-(2-氨基-4,7-二氫-4-氧-1H-吡咯[2,3-D]嘧啶-5-基)乙基]苯甲酰)-L-谷氨酸);N-[4-[2-(2-胺基-4,7-二氫-4-氧-1H吡咯[2,3-D]嘧啶-5基)乙基]苯甲酰]-L-谷氨酸;培美曲賽雜質(zhì)1
英文名稱	Pemetrexed
英文同義詞	(S)-2-(4-(2-(2-AMino-4-oxo-4,7-dihydro-1H-pyrrolo[2,3-d]pyriMidin-5-yl)ethyl)benzaMido)pentanedioic acid;PeMetrexed-13C5;PeMetrexed-15C5;N-[4-[2-(2-aMino-4,7-dihydro-4-oxo-3H-pyrrolo[2,3-d]pyriMidin-5-yl)ethyl]benzoyl]L-GlutaMic acid (PeMetrexed acid);N-[4-[2-(2-AMino-4,7-dihydro-4-oxo-1H-pyrrolo[2,3-d]pyriMidin-5-yl)ethyl]benzoyl]-L-glutaMic acid;(S)-2-(4-(2-(2-Amino-4-oxo-4,7-dihydro-1H-pyrrolo-[2,3-d]pyrimidin-5-yl)ethyl)benzamido)pentanedi;N-[4-[2-(2-Amino-4,7;(2R)-2-{[4-(2-{2-aMino-4-oxo-1H,4H,7H-pyrrolo[2,3-d]pyriMidin-5-yl}ethyl)phenyl]forMaMido}pentanedioic acid
CAS號	137281-23-3
分子式	C20H21N5O6
分子量	427.41
EINECS號	680-625-9
相關類別	原料藥;中間體;醫(yī)藥原料;培美中六;小分子抑制劑;培美曲塞二鈉中間體;醫(yī)藥中間體;細胞凋亡;藥物雜質(zhì)及中間體;化藥雜質(zhì)-培美曲塞;原料藥及中間體;化學試劑;API;CIALIS;Anti-cancer & immunity;標準品;生物化工
Mol文件	137281-23-3.mol
結構式

培美曲塞二鈉鹽 性質(zhì)

培美曲塞二鈉鹽 用途與合成方法

生物活性

Pemetrexed (LY231514) 是一種葉酸拮抗劑 (antifolate)。Pemetrexed (LY231514) 抑制胸苷酸合成酶 (TS)，二氫葉酸還原酶 (DHFR) 和甘氨酰胺核苷酸甲酰轉移酶 (GARFT)，Ki 分別為 1.3 nM，7.2 nM 和 65 nM。

靶點

Ki: 1.3 nM (TS), 7.2 nM (DHFR), 65 nM (GARFT)

體外研究

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.

體內(nèi)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.

安全信息

MSDS信息

培美曲塞二鈉鹽 價格(試劑級)

培美曲塞二鈉鹽 上下游產(chǎn)品信息