Pemetrexed (357166-29-1) is a multi-targeted antifolate with antitumor activity. It potently inhibits folate-dependent enzymes involved in both purine and pyrimidine synthesis including thymidylate synthase (Ki = 109 nM), dihydrofolate reductase (Ki = 7 nM), glycinamide ribonucleotide formyltransferase (Ki = 9.3 μM), and aminoimidazole carboxamide ribonucleotide formyltransferase (Ki = 3.6 μM).1 A clinically useful anticancer agent.2 Indirectly activates the metabolic kinase AMPK and consequently influences the mTORC1 pathway in human carcinomas.3 Activation of AMPK is associated with pemetrexed resistance.4 Induces G0/G1-phase cell cycle arrest in esophageal squamous cell carcinoma cells.5 培美曲塞(357166-29-1)是一种具有抗肿瘤活性的多靶点抗叶酸剂。 它能有效抑制与嘌呤和嘧啶合成相关的叶酸依赖酶,包括胸苷酸合成酶(Ki = 109 nM)、二氢叶酸还原酶(Ki = 7 nM)、甘氨酸酰胺核糖核苷酸甲酰基转移酶(Ki = 9.3 μM)和氨基咪唑羧酰胺核糖核苷酸甲酰基转移酶(Ki = 3.6 μM) 临床有用的抗癌剂 间接激活代谢激酶AMPK,从而影响人癌mTORC1通路 AMPK的激活与培美曲塞耐药性相关 诱导食管鳞癌细胞G0/ g1期细胞周期阻滞。
References/Citations:
1) Shih et al. (1997), LY231514, a pyrrolo[2,3-d]pyrimidine-based antifolate that inhibits multiple folate-requiring enzymes; Cancer Res. 57 1116 2) Hanauske et al. (2001), Pemetrexed disodium: a novel antifolate clinically active against multiple solid tumors; Oncologist 6 363 3) Rothbart et al. (2010), Pemetrexed indirectly activates the metabolic kinase AMPK in human carcinomas; Cancer Res. 70 10299 4) Qin et al. (2019), AMPK activation induced in pemetrexed-treated cells is associated with development of drug resistance independently of target enzyme expression; Mol. Oncol. 13 1419 5) Li et al. (2019), Pemetrexed exerts anticancer effects by inducing G0/G1-phase cell cycle arrest and activating the NOXA/Mcl-1 axis in human esophageal squamous cell carcinoma cells; Oncol. Lett. 17 1851
CAS:
357166-29-1
Catalog Number:
10-2162
Activity:
Multi-targeted antifolate
Chemical Name:
N-[4-[2-(2-Amino-4,7-dihydro-4-oxo-3H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl]-L-glutamic acid, disodium salt
Molecular Weight:
597.49
Molecular Formula:
C20H19N5O6 • 2Na • 7H2O
Solubility:
Soluble in Water (up to 100 mg/ml).
Physical Properties:
White solid
Purity:
98% by TLC and HPLC
NMR (Conforms)
Storage Temperature:
-20° (des.)
Stability:
Stable for 1 year as supplied. Solutions in distilled water may be stored at -20° for up to 31month.
Shipping Code:
RT
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