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AZ'3137

AZ‘3137 is an orally active PROTAC-type androgen receptor (AR) degrader with a DC50 value of 22 nM. AZ‘3137 can degrade L702H mutant AR (DC50 of 92 nM) . AZ'3137 can inhibit cell proliferation of LNCaP, with a GI50 value of 74 nM. AZ'3137 can inhibit AR signaling and tumor growth in prostate cancer mice (Pink: AR Ligand (HY-172954) ; Blue: CRBN ligand (HY-172955) ; Black: linker (HY-W262798) ; E3 Ligand+Linker: HY-172956) [1].

Product Specifications

CAS Number

[2960179-55-7]

UNSPSC

12352005

Target

Androgen Receptor; PROTACs

Type

Reference compound

Related Pathways

PROTAC; Vitamin D Related/Nuclear Receptor

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/az-3137.html

Purity

99.90

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

COC1=CC(N2CCN(CC3CCN(C4=CC=C(C5CCN(C6=CC=C(C#N)C(C(F)(F)F)=C6F)CC5)C=C4)CC3)CC2)=CC7=C1C(N(C8CCC(NC8=O)=O)C7)=O

Molecular Formula

C43H47F4N7O4

Molecular Weight

801.87

References & Citations

[1]Bagal SK, et al. Discovery of a Series of Orally Bioavailable Androgen Receptor Degraders for the Treatment of Prostate Cancer. J Med Chem. 2024 Jul 25;67 (14) :11732-11750.

Shipping Conditions

Blue Ice

Storage Conditions

-20°C, 3 years (Powder)

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Available Sizes

Curated Selection

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