RLY-2608
Product Specifications
UNSPSC Description
RLY-2608 is an orally active first-in-class allosteric mutant-selective inhibitor of PI3Ka with anti-tumor activity. RLY-2608 inhibits tumor growth in PIK3CA-mutant xenograft mice models with minimal impact on insulin[1][2][3].
Target Antigen
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
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 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.
Shipping Conditions
Room Temperature
Product Datasheet
http://file.medchemexpress.com/batch_PDF/HY-153306/RLY-2608-DataSheet-MedChemExpress.pdf
Product MSDS
http://file.medchemexpress.com/batch_PDF/HY-153306/RLY-2608-SDS-MedChemExpress.pdf
Clinical Information
Phase 1
CAS Number
2733573-94-7
Available Sizes
Curated Selection
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