CA-170

CA-170 : Inhibitor of CD274

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(2 ratings)

note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars.

Probe CA-170 is in the process of SERP review.

Please continue to check back for new reviews and commentary.

Information

CD274

Inhibitor

up to 1 uM

Probe Availability:

In Vitro Validations

No in Vitro Validations

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): CA-170 was profiled against a broad panel of receptors and enzymes (80-panel, CEREP profiling assay), and results indicated minimal or no interaction with any of these proteins.

Potency assay, off target (cells): CA-170 was evaluated for its activity in functional assays for other key immune pathways in the B7 ligand/receptor family such as CTLA4, PD-L2, VISTA, and immune stimulatory B7-1. In all these assays, CA-170 was able to only rescue IFNγ release from PBMC inhibited by recombinant PD-L1, PD-L2, and VISTA, and not IL-2 secretion from Jurkat cells inhibited by CTLA4-Ig.

I have extra information to add

SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

(last updated: 4 Nov 2024 )

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

CA-170 is an orally bioavailable small molecule dual inhibitor of PD-L1 and VISTA. This compound is currently investigated in Phase II clinical trial for patients with advanced solid tumors or lymphomas. CEREP panel (80 targets) indicated that this compound has minimal or no interaction with any of these proteins at 10 uM concentration. There is only one target, NeuropeptideY, to which CA-170 showed binding at 10 uM (<=78%). So it is highly recommended to use the compound at 1 uM cellular concentration but not higher. CA-170 also showed 50% oral bioavailability in mouse model at 30 mg/kg, which indicated decent profile for in vivo use.

(last updated: 16 Dec 2024 )