A selective inhibitor of MCT1
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AZD 3965

Item No. 19912

Technical Information
Formal Name
5-[[(4S)-4-hydroxy-4-methyl-2-isoxazolidinyl]carbonyl]-3-methyl-1-(1-methylethyl)-6-[[5-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]methyl]-thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione
CAS Number
1448671-31-5
Molecular Formula
C21H24F3N5O5S
Formula Weight
Purity
≥95%
Formulation
A crystalline solid
DMF: 25 mg/mlDMSO: 25 mg/mlDMSO:PBS (pH 7.2) (1:6): 0.1 mg/mlEthanol: 20 mg/ml
λmax
228, 260 nm
SMILES
CC(C)N(C(N1C)=O)C2=C(C(C(N3C[C@](C)(O)CO3)=O)=C(CC4=C(C)NN=C4C(F)(F)F)S2)C1=O
InChi Code
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
InChi Key
PRNXOFBDXNTIFG-FQEVSTJZSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    AZD 3965 is a potent inhibitor of monocarboxylate transporter 1 (MCT1; Ki = 1.6 nM), killing tumor cells that are reliant on glycolysis by blocking lactate transport.1 It displays six-fold selectivity for MCT1 over MCT2 and is without effect against MCT4 at 10 µM. AZD 3965 increases intratumor lactate levels and decreases tumor growth in mice bearing COR-L103 small cell lung cancer (SCLC) xenografts.1 AZD 3965 also enhances radiosensitivity in mice with SCLC xenografts.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Polanski, R., Hodgkinson, C.L., Fusi, A., et alActivity of the monocarboxylate transporter 1 inhibitor AZD3965 in small cell lung cancer. Clin. Cancer Res. 20(4), (2014).

    2. Bola, B.M., Chadwick, A.L., Michopoulos, F., et alInhibition of monocarboxylate transporter-1 (MCT1) by AZD3965 enhances radiosensitivity by reducing lactate transport. Mol. Cancer. Ther. 13(12), 2805-2816 (2014).

    Product Citations

    Bonglack, E.N., Messinger, J.E., Cable, J.M., et alMonocarboxylate transporter antagonism reveals metabolic vulnerabilities of viral-driven lymphomas. Proc. Natl. Acad. Sci. USA 118(25), e2022495118 (2021).