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GDC-2992

GDC-2992 (Compound 28A) is an orally bioavailable androgen receptor (AR) PROTAC degrader. GDC-2992 degrads AR with a DC50 value of 2.7 nM and inhibits proliferation with an IC50 valude of 9.7 nM in VCaPcells. GDC-2992 can be used for prostatic cancer study. (Structure Note: Pink: target protein ligand (HY-130845) ; Blue: E3 ligase ligand (HY-W1003189A) ; Black: linker (HY-169975) ; E3 ligase ligand +linker (HY-169976A) ) [1].

Product Specifications

CAS Number

[2753651-10-2]

Product Name Alternative

RO7656594

UNSPSC

12352005

Target

Androgen Receptor; PROTACs

Related Pathways

PROTAC; Vitamin D Related/Nuclear Receptor

Applications

Cancer-programmed cell death

Field of Research

Cancer

Purity

99.38

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

N#CC1=CC=C(O[C@H]2C(C)(C)[C@H](NC(C3=CC=C(N4CCC(CN5CCN(C6=CC(C=NN([C@@H]7C(NC(CC7)=O)=O)C8=O)=C8C=C6)CC5)CC4)C=C3)=O)C2(C)C)C=C1Cl

Molecular Formula

C45H51ClN8O5

Molecular Weight

819.39

References & Citations

[1]HF Lu, et al. Phthalazinone compound, and preparation method therefor and medical use thereof. WO2021249534A1.|[2]Ciara Metcalfe, et al. Abstract ND02: GDC-2992: A heterobifunctional Androgen Receptor (AR) antagonist and degrader for the treatment of AR wild-type and mutant prostate cancer. Cancer Res (2025) 85 (8_Supplement_2) : ND02.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Reference compound1

Clinical Information

Phase 1

Available Sizes

Curated Selection

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