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CA-170 | CA-170 : Inhibitor of CD274
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (2 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
CD274
    • EC50:15.4 ± 1.3 nM
    Inhibitor
    up to 1 uM

    Selectivity

    In Vitro Selectivity Assessment
    Potency Assay Off-Target:
    CA-170 was profiled against a broad panel of receptors and enzymes (80-panel, CEREP profiling assay) ...
    In Cell Selectivity Assessment
    Potency Assay Off-Target:
    CA-170 was evaluated for its activity in functional assays for other key immune pathways in the B7 l ...

    Potency
    Cellular
    In Vitro

    CD274

    Mode of Action: Inhibitor

    Structure-Activity-Relationship data available? No

    DOI Reference: 10.1038/s42003-021-02191-1

    In Vivo Validations

    Mouse
    Dose: 1 mg/Kg IV, 30 mg/Kg PO
    Route of delivery: Intravenous, Oral
    Systemic clearance: 723 mL/hr/kg
    Cmax: 1723 ng/mL
    Area Under the Curve:: 4205 hr*ng/mL IV, 19574 hr*ng/mL PO
    Bioavailability: 50%

    DOI Reference: 10.1038/s42003-021-02191-1

    Chemical Information

    Molecular Formula C12H20N6O7
    SMILEs C[C@@H](O)[C@H](NC(=O)N[C@@H](CC(N)=O)c1nc([C@H](N)CO)no1)C(=O)O
    InChI InChI=1S/C12H20N6O7/c1-4(20)8(11(22)23)16-12(24)15-6(2-7(14)21)10-17-9(18-25-10)5(13)3-19/h4-6,8,19-20H,2-3,13H2,1H3,(H2,14,21)(H,22,23)(H2,15,16,24)/t4-,5-,6+,8+/m1/s1
    Molecular weight 360.14 Da
    AlogP 0.0
    HBond acceptors 13
    HBond donors 9
    Atoms 45

    References

    Publications

    Cross References

    canSARChEMBLBindingDB

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    Expert Reviews

    by SERP
    (on 4 Nov 2024 )
    Cellular Use Rating
    In Model Organisms
    ( The reviewer did not leave any comments )
    by SERP
    (on 16 Dec 2024 )
    Cellular Use Rating
    In Model Organisms
    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....
    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. Read more about our evaluation criteria