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AZD3965

Chemical Structure : AZD3965

CAS No.: 1448671-31-5

AZD3965 (AZD-3965)

Catalog No.: PC-43178Not For Human Use, Lab Use Only.

AZD3965 (AZD-3965) is a potent, selective, orally bioavailable monocarboxylate transporter 1 (MCT1) inhibitor with binding IC50 of 1.6 nM, displays 6-fold selectivity over MCT2 and does not inhibit MCT3 or MCT4.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

AZD3965 (AZD-3965) is a potent, selective, orally bioavailable monocarboxylate transporter 1 (MCT1) inhibitor with binding IC50 of 1.6 nM, displays 6-fold selectivity over MCT2 and does not inhibit MCT3 or MCT4.
AZD3965 inhibits both lactate efflux and influx into cells and causes an increase in glycolysis and an upregulation of glycolytic enzymes in SCLC and gastric cancer cell lines.
AZD3965 reduces tumor growth and increases intratumor lactate in vivo, enhances radiosensitivity by reducing lactate transport.

Physicochemical Properties

M.Wt 515.506
Formula C21H24F3N5O5S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 36 mg/mL

Chemical Name/SMILES

Thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione, 5-[[(4S)-4-hydroxy-4-methyl-2-isoxazolidinyl]carbonyl]-3-methyl-1-(1-methylethyl)-6-[[5-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]methyl]-

References

1. Polański R, et al. Clin Cancer Res. 2014 Feb 15;20(4):926-937.

2. Bola BM, et al. Mol Cancer Ther. 2014 Dec;13(12):2805-16.

3. Hong CS, et al. Cell Rep. 2016 Feb 23;14(7):1590-1601.

4. Beloueche-Babari M, et al. Cancer Res. 2017 Nov 1;77(21):5913-5924.

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