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AZ 3137

Catalog #: 8833 Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
8833/5

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AZ 3137 | CAS No. 2960179-55-7 | Active Degraders
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Description: Potent and selective AR and AR L702H Degrader, orally bioavailable

Chemical Name: 4-[4-[4-[4-[[4-[2-(2,6-Dioxo-3-piperidinyl)-2,3-dihydro-7-methoxy-1-oxo-1H-isoindol-5-yl]-1-piperazinyl]methyl]-1-piperidinyl]phenyl]-1-piperidinyl]-3-fluoro-2-(trifluoromethyl)benzonitrile

Purity: ≥98%

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Biological Activity

AZ 3137 is a potent and selective androgen receptor (AR) Degrader (PROTAC®)(DC50 = 22 nM in LNCaP cells). AZ 3137 can degrade L702H mutant AR (DC50 = 158 nM). AZ 3137 inhibits the proliferation of LNCaPs cells (GI50 = 74 nM). AZ 3137 inhibits AR signaling in vitro and tumor growth in vivo in a mouse prostate cancer xenograft model. AZ 3137 is orally bioavailable.

Technical Data

M.Wt:
801.89
Formula:
C43H47F4N7O4
Solubility:
Soluble to 10 mM in DMSO
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
2960179-55-7

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

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