Nolatrexed dihydrochloride

Nolatrexed dihydrochloride (AG 337) is an orally active and non-competitive lipophilic inhibitor of thymidylate synthase with a Ki of 11 nM for human thymidylate synthase. Nolatrexed dihydrochloride interacts at the folate cofactor binding site of the enzyme. Nolatrexed dihydrochloride increases sulfotransferases. Nolatrexed dihydrochloride induces cell cycle arrest in S phase of cancer cells. Nolatrexed dihydrochloride exhibits anticancer activity against cervical cancer.

Product Specifications

CAS Number

[152946-68-4]

Product Name Alternative

AG 337

UNSPSC

12352005

Hazard Statement

H341, H361

Target

Thymidylate Synthase

Type

Reference compound

Related Pathways

Apoptosis

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/Nolatrexed_dihydrochloride.html

Concentration

10mM

Purity

98.38

Solubility

DMSO : 41.67 mg/mL (ultrasonic) |H2O : 50 mg/mL (ultrasonic)

Smiles

[H]Cl.O=C1N=C(N)NC2=C1C(SC3=CC=NC=C3)=C(C)C=C2.[H]Cl

Molecular Formula

C14H14Cl2N4OS

Molecular Weight

357.26

Precautions

H341, H361

References & Citations

[1]Webber S, et al. AG337, a novel lipophilic thymidylate synthase inhibitor: in vitro and in vivo preclinical studies. Cancer Chemother Pharmacol. 1996;37 (6) :509-17.|[2]McGuire JJ, et al. Characterization of the effect of AG337, a novel lipophilic thymidylate synthase inhibitor, on human head and neck and human leukemia cell lines.|[3]Maiti S, et al. Regulations of expressions of rat/human sulfotransferases by anticancer drug, nolatrexed, and micronutrients. Anticancer Drugs. 2022 Jan 1;33 (1) :e525-e533.|[4]Wang G F, et al. Measurement of plasma concentration and bioavailability of nolatrexed dihydrochloride in mice. Nan Fang yi ke da xue xue bao= Journal of Southern Medical University, 2008, 28 (11) : 1993-1995.|[5]Webber S, et al. AG337, a novel lipophilic thymidylate synthase inhibitor: in vitro and in vivo preclinical studies. Cancer Chemother Pharmacol. 1996;37 (6) :509-17.