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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 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 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; 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; reduces tumor growth and increases intratumor lactate in vivo, enhances radiosensitivity by reducing lactate transport.

Solid Tumors

Phase 1 Clinical

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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