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AZD3965

Cat. No. M5189
AZD3965 Structure
Size Price Availability Quantity
2mg USD 75  USD75 In stock
5mg USD 115  USD115 In stock
10mg USD 180  USD180 In stock
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Quality Control & Documentation
Biological Activity

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.

Chemical Information
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
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Bola BM, et al. Mol Cancer Ther. Inhibition of monocarboxylate transporter-1 (MCT1) by AZD3965 enhances radiosensitivity by reducing lactate transport.

[2] Polański R, et al. Clin Cancer Res. Activity of the monocarboxylate transporter 1 inhibitor AZD3965 in small cell lung cancer.

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Keywords: AZD3965 supplier, Monocarboxylate Transporter (MCT), inhibitors, activators


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