AZD-3965 Chemical Properties

Melting point:

>140°C (dec.)

Boiling point:

723.1±70.0 °C(Predicted)

Density 

1.483±0.06 g/cm3(Predicted)

storage temp. 

-20°C, Inert atmosphere

solubility 

DMSO (Slightly), Ethanol (Slightly), Methanol (Slightly)

form 

Solid

pka

10.92±0.50(Predicted)

color 

Off-White to Pale Yellow

AZD-3965 Usage And Synthesis

Uses

AZD 3965 is a monocarboxylate transporter 1 (MCT1) inhibitor.

Enzyme inhibitor

This orally bioavailable MCT1 inhibitor (FW = 515.51 g/mol; CASs = 733809-45-5 and 1448671-31-5), also named (S)-5-(4-hydroxy-4- methylisoxazolidine-2-carbonyl)-1-isopropyl-3-methyl-6-((3-methyl-5-(tri fluoromethyl)-1H-pyrazol-4-yl)methyl)-thieno[2,3-d]pyrimidine-2,4(1H, 3H) -dione, selectively targets the Monocarboxylate Transporter-1 (IC50 = 1.6 nM) and is ~6x less active toward MCT2. AZD3965 does not inhibit MCT4, even at 10 μM. MCT1 and MCT4 are primarily involved in lactate transport, targeting highly glycolytic cancer cells, especially those that are hypoxic. The latter property suggests that the combined use with a vascular-disrupting anticancer agent (such as combrestatin) may improve the inhibitory action of AZD-3965 against cancer cells.

AZD-3965(733809-45-5)Related Product Information

• GSK-2126458