AZD3965 free base · Synonyms: AZD-3965 · AZD 3965

AZD3965 is a selective MCT1 inhibitor.

For research use only. Not for human or veterinary use.

Target Monocarboxylate Transporter

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

AZD3965 structure

CAS No.: 1448671-31-5

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
100 mg	USD 480.00	BP-02311-100mg	In stock	Get quote
250 mg	USD 960.00	BP-02311-250mg	In stock	Get quote
500 mg	USD 1,530.00	BP-02311-500mg	In stock	Get quote
1 g	USD 2,450.00	BP-02311-1g	In stock	Get quote
2 g	USD 3,932.00	BP-02311-2g	In stock	Get quote
3 g	USD 4,710.00	BP-02311-3g	In stock	Get quote

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Description

AZD3965 is a selective MCT1 inhibitor with a Ki of 1.6 nM, showing 6-fold selectivity over MCT2.

Biological activity

In Vitro AZD3965 is designed to selectively inhibit Monocarboxylate transporter-1 (MCT1) and will therefore be expected to influence the movement of lactate into and out of cells[1]. AZD3965 treatment causes a 3.7 fold increase in intracellular lactate in hypoxic COR-L103 and 3.7 fold and 3.9 fold increases in normoxic and hypoxic NCI-H1048 cells respectively. In all other cases a <1.9 fold increase is observed. These data are consistent with AZD3965 blocking lactate transport in cells where AZD3965 also reduces cell number and is consistent with AZD3965 acting via inhibition of MCT1. When MCT1 is overexpressed the EC50 of NCI-H1048 is increased from 0.14 nM to 10.5 nM in NCI-H1048 cells. This is consistent with AZD3965 acting via MCT1 inhibition. In Vivo COR-L103 tumor bearing mice are treated with 100 mg/kg AZD3965 or vehicle BIDfor 21 days and the tumor volume monitored. Pharmacokinetic analysis demonstrates that 100 mg/kg AZD3965 BID results in concentrations of free AZD3965 predicted to inhibit lactate transport. AZD3965 treatment significantly reduces the growth of COR-L103 tumors, although tumor regression is not seen, consistent with AZD3965 only targeting the hypoxic fraction of the tumor.

Identifiers

SMILES: CC(C)N1C2=C(C(C(=O)N3C[C@](C)(O)CO3)=C(CC3=C(C)NN=C3C(F)(F)F)S2)C(=O)N(C)C1=O
InChIKey: PRNXOFBDXNTIFG-FQEVSTJZSA-N

Specifications

MW (average): 515.5060
Formula: C₂₁H₂₄F₃N₅O₅S
CAS No.: 1448671-31-5
Physical state: Solid
Color: White to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

Documents

References

[1]. Bola BM, 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.

[2]. Polanski R, et al. Activity of the monocarboxylate transporter 1 inhibitor AZD3965 in small cell lung cancer. Clin Cancer Res. 2014 Feb 15;20(4):926-37.

Same research area

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