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AZD3965
Axon 4070
CAS:
1448671-31-5
- Optical Purity: 99% e.e.
- Soluble in DMSO
- MF: C21H24F3N5O5S
- MW: 515.51
Description
AZD3965 is a first-in-class, cell permeable high affinity ligand of monocarboxylate transporter 1 (MCT1), binding to the protein with a Ki value of 1.6 nM, with 6 fold selectivity over the closely related MCT2, and does not bind to MCT4 at a concentration of 10 μM.
More Information
| Parent CAS No. | 1448671-31-5 |
|---|---|
| Chemical Name | (S)-5-(4-hydroxy-4-methylisoxazolidine-2-carbonyl)-1-isopropyl-3-methyl-6-((5-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl)methyl)thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione |
| extra_info | Sold in collaboration with Chemietek |
| SMILES | C1(=O)N(C(C)C)C2SC(CC3=C(C)NN=C3C(F)(F)F)=C(C(N3OC[C@@](C)(O)C3)=O)C=2C(=O)N1C |&1:25,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C21H24F3N5O5S/c1-9(2)29-18-14(16(30)27(5)19(29)32)13(17(31)28-7-20(4,33)8-34-28)12(35-18)6-11-10(3)25-26-15(11)21(22,23)24/h9,33H,6-8H2,1-5H3,(H,25,26)/t20-/m0/s1 |
| InChiKey | PRNXOFBDXNTIFG-FQEVSTJZSA-N |
| CID | 10369242 |
| Short Description | MCT1 inhibitor |
References
- R Polański et al. Activity of the monocarboxylate transporter 1 inhibitor AZD3965 in small cell lung cancer. Clin Cancer Res. 2014 Feb 15;20(4):926-937.
- BM Bola et al. Inhibition of monocarboxylate transporter-1 (MCT1) by AZD3965 enhances radiosensitivity by reducing lactate transport. Mol Cancer Ther. 2014 Dec;13(12):2805-16.
