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AKR1C3 PROTAC 5

Chemical Structure : AKR1C3 PROTAC 5

CAS No.:

AKR1C3 PROTAC 5 (AKR1C3 degrader 5)

Catalog No.: PC-22253Not For Human Use, Lab Use Only.

AKR1C3 PROTAC 5 is a first-in-class Aldo-Keto reductase 1C3 (AKR1C3) PROTAC degrader with DC50 of 52 nM in 22Rv1 cells, AKR1C1/C2 DC50 of 49 nM, ARv7 DC50 of 70 nM.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

AKR1C3 PROTAC 5 is a first-in-class Aldo-Keto reductase 1C3 (AKR1C3) PROTAC degrader with DC50 of 52 nM in 22Rv1 cells, AKR1C1/C2 DC50 of 49 nM, ARv7 DC50 of 70 nM.
AKR1C3 PROTAC 5 is an effective degrader of AKR1C3, AKR1C1/2, and ARv7 in a concentration and proteasome dependent manner.
AKR1C3 PROTAC 5 reduces cell viability of in vitro prostate cancer models and potentiates enzalutamide through an AKR1C3-dependant effect.

Physicochemical Properties

M.Wt 841.88
Formula C45H43N7O10
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(E)-3-(5-((4-((1-(2-(2-(2-((2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-4-yl)amino)-2-oxoethoxy)ethoxy)ethyl)-1H-1,2,3-triazol-4-yl)methoxy)benzyl)carbamoyl)-[1,1'-biphenyl]-3-yl)acrylic acid

References

1. Carmona AV, et al. Commun Chem. 2024 Apr 29;7(1):95.

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