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AZD3965 is a potent, selective and orally available monocarboxylate transporter 1 (MCT1) inhibitor with a binding affinity of 1.6 nM. AZD3965 potently inhibits lactate transport and cell growth in lymphoma cell lines that preferentially express MCT1. In H526, HGC27 cells and DMS114 cells, AZD3965 increases intracellular lactate and significantly reduces lactate uptake. In mice bearing H526 tumors, AZD3965 (100 mg/kg, p.o.) causes increased lactate concentration, a reduction in growth and increased radiation sensitivity. AZD3965 (100 mg/kg, p.o.) in nonobese diabetic scid-γ mice bearing COR-L103 xenografts reduces tumor growth and increased intratumor lactate.
| Molecular Weight | 515.51 |
| Formula | C21H24F3N5O5S |
| CAS Number | 1448671-31-5 |
| Solubility (25°C) | DMSO 100 mg/mL Ethanol 100 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Monocarboxylate Transporter (MCT) Products |
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| Silicristin
Silychristin is a flavonoid rich in milk thistle fruits, which has antioxidant effects. Silychristin is an effective inhibitor of thyroid hormone transporter MCT8 and can strongly inhibit T3 uptake with IC50 of 110 nM. |
| 7ACC1
7ACC1(DEAC; Coumarin D 1421; D 1421) selectively interfere with lactate fluxes in the lactate-rich tumor microenvironment; inhibits lactate influx but not efflux in tumor cells expressing MCT1 and MCT4 transporters. |
| 7ACC2
7ACC2 is a new potent MCT inhibitor with IC50 of 11 nM for inhibition of [14C]-lactate influx; new antitumor treatment targeting lactate transport in cancer cells. IC50 value: 11 nM ([14C]-lactate influx). |
| α-cyano-4-hydroxy-cinnamic acid
α-Cyano-4-hydroxycinnamic acid (α-CHCA) is a potent and non-competitive inhibitor of monocarboxylate transporters (MCTs). α-Cyano-4-hydroxycinnamic acid inhibits mitochondrial pyruvate transporter with a Ki of 6.3 μM. |
| UK-5099
UK-5099 (PF-1005023) is a potent inhibitor of the mitochondrial pyruvate carrier (MPC), it inhibits pyruvate-dependent O2 consumption with an IC50 of 50 nM. UK-5099 is also a cuproptosis inhibitor. |
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