RLY-2608

RLY-2608 : Allosteric Inhibitor of PIK3CA

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(0 ratings)

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Probe RLY-2608 is in the process of SERP review.

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Information

PIK3CA (Mutant:WT, H1047R, E542K, E545K)

Allosteric

up to 100 nM

In Vitro Validations

Uniprot ID: P42336

Target Class: Kinase

Target SubClass: PI3/PI4-kinase

Potency: IC50

Potency Value: 4 nM

Potency Assay: Biochemical assay using H1047R mutant

PDB ID for probe-target interaction (3D structure): 8TSD

Target aliases:

Phosphatidylinositol 4,5-bisphosphate 3-kinase cat ...

DOI Reference: 10.1158/2159-8290.CD-23-0944

Uniprot ID: P42336

Target Class: Kinase

Target SubClass: PI3/PI4-kinase

Potency: IC50

Potency Value: 48 nM

Potency Assay: Biochemical assay using WT protein

PDB ID for probe-target interaction (3D structure): 8TSD

Target aliases:

Phosphatidylinositol 4,5-bisphosphate 3-kinase cat ...

DOI Reference: 10.1158/2159-8290.CD-23-0944

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency assay (off target): In vitro kinome profile of RLY-2608. RLY-2608 was tested at a concentration of 10 μM by SelectScreen

Potency assay, off target (cells): tested on various cells lines for target engagement and cell proliferation

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SERP ratings and comments

SERP Ratings

In Cell Rating

SERP Comments:

Clinically active compound with a >10-fold window to PI3Ka WT. Highly selective for the alpha isoform. Quality tool.

(last updated: 7 Jan 2025 )