AZD-3514 Inhibitor CAS No. 1240299-33-5

Cat. No.	Name	Size	Price
KI2787	AZD-3514	50 mg	$752
	AZD-3514	100 mg	$1232
	AZD-3514	200 mg	$1972
	AZD-3514	1 g	$7888

Chemical Characteristic

Product Name	AZD-3514
CAS No.	1240299-33-5
Molecular Weight	519.56
Formula	C₂₅H₃₂F₃N₇O₂
Chemical Name	1-[4-[2-[4-[1-[3-(trifluoromethyl)-7,8-dihydro-[1,2,4]triazolo[4,3-b]pyridazin-6-yl]piperidin-4-yl]phenoxy]ethyl]piperazin-1-yl]ethanone
Smiles	C(=O)(C)N1CCN(CC1)CCOc1ccc(cc1)C1CCN(CC1)C1=Nn2c(CC1)nnc2C(F)(F)F
Chemical Structure

Biological activities

AZD-3514 is an a small-molecule androgen receptor(AR) inhibitor.^[1] The IC50 of AZD-3514 against AR is 2.2 μM.^[2] In vitro, AZD-3514 inhibits cell growth in prostate cancer cells expressing wild-type (VCaP) and mutated (T877A) AR (LNCaP). In vivo, in the Hershberger castrated rat, oral dosing of AZD-3514 (100mg/kg once-daily for 7 days) significantly inhibits testosterone-induced growth of sexual accessory organs.^[3]

Protocols

In vitro, AZD-3514 is dissolved in DMSO.^[3]

References

[1] Leibowitz-Amit R, et al. Targeting the androgen receptor in the management of castration-resistant prostate cancer: rationale, progress, and future directions. Curr Oncol. 2012, 19 (Suppl 3): S22-31. [2] Bradbury RH, et al. Discovery of AZD3514, a small-molecule androgen receptor downregulator for treatment of advanced prostate cancer. Bioorg Med Chem Lett. 2013, 23 (7): 1945-1948. [3] Loddick S, Bradbury R, Broadbent N, et al. Preclinical profile of AZD3514: A small molecule-targeting androgen receptor function with a novel mechanism of action and the potential to treat castration-resistant prostate cancer. Cancer Res. 2012, 72 (8 Supplement): 3848.

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