Zovegalisib

Zovegalisib (RLY-2608) is an orally active first-in-class allosteric mutant-selective inhibitor of PI3Ka with anti-tumor activity. Zovegalisib inhibits tumor growth in PIK3CA-mutant xenograft mice models with minimal impact on insulin[1][2][3].

Product Specifications

CAS Number

[2733573-94-7]

Product Name Alternative

RLY-2608

UNSPSC

12352005

Target

PI3K

Type

Reference compound

Related Pathways

PI3K/Akt/mTOR

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/rly-2608.html

Concentration

10mM

Purity

99.20

Solubility

DMSO : 100 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C1N[C@@H](C2=CC(F)=CC=C2Cl)C(C1=C3)=C(NC(C4=CC(F)=CC(C(F)(F)F)=C4)=O)C=C3C5=C(C#N)N6C(C=C5)=NC=N6

Molecular Formula

C29H14ClF5N6O2

Molecular Weight

608.91

References & Citations

[1]Andreas Varkaris, et al. Discovery and clinical proof-of-concept of RLY-2608, a first-in-class mutant-selective allosteric PI3Ka inhibitor that decouples anti-tumor activity from hyperinsulinemia. Cancer Discov. 2023 Nov 2.|[2]Pazolli E, et al. RLY-2608: the first allosteric mutant-and isoform-selective inhibitor of PI3Kα, is efficacious as a single agent and drives regressions in combination with standard of care therapies in PIK3CA mutant breast cancer models[J]. Cancer Res., 2022, 82.|[3]Perez C A, et al. First-in-human global multi-center study of RLY-2608, a pan-mutant and isoform-selective PI3Kα inhibitor, as a single agent in patients with advanced solid tumors and in combination with fulvestrant in patients with advanced breast cancer[J]. 2022.