CAS 1675203-84-5|PD-L1 inhibitor 1

Introduction:Basic information about CAS 1675203-84-5|PD-L1 inhibitor 1, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
Common NamePD-L1 inhibitor 1
CAS Number1675203-84-5Molecular Weight419.516
Density1.1±0.1 g/cm3Boiling Point611.4±55.0 °C at 760 mmHg
Molecular FormulaC25H29N3O3Melting Point/
MSDS/Flash Point323.6±31.5 °C

Names

NameN-[2-[[[2-Methoxy-6-[(2-methyl[1,1'-biphenyl]-3-yl)methoxy]-3-pyridinyl]methyl]amino]ethyl]acetamide
SynonymMore Synonyms

PD-L1 inhibitor 1 BiologicalActivity

DescriptionBMS-202 is an inhibitor of the PD-1/PD-L1 protein/protein interaction with an IC50 of 18 nM.
Related CatalogSignaling Pathways >>Immunology/Inflammation >>PD-1/PD-L1Research Areas >>Cancer
Target

18 nM (PD-1/PD-L1)[1]

In VitroBMS-202 inhibits PD-1/PD-Ll interaction, and may augment therapeutic immune response to a number of histologically distinct tumors. Blockade of the PD-1/PD-Ll ligation using antibodies to PD-Ll has been shown to restore and augment T cell activation in many systems[1].
Kinase AssayAll binding studies are performed in an HTRF assay buffer consisting of dPBS supplemented with 0.1% (with v) bovine serum albumin and 0.05% (v/v) Tween-20. For the PD-l-Ig/PD-Ll-His binding assay, inhibitors are pre-incubated with PD-Ll-His (10 nM final) for 15 m in 4 μL of assay buffer, followed by addition of PD-l-Ig (20 nM final) in 1 μL of assay buffer and further incubation for 15 m. PD-L1 from either human, cyno, or mouse are used. HTRF detection is achieved using europium crypate-labeled anti- Ig (1 nM final) and allophycocyanin (APC) labeled anti-His (20 nM final). Antibodies are diluted in HTRF detection buffer and 5 μL is dispensed on top of binding reaction. The reaction mixture is allowed to equilibrate for 30 minutes and signal (665 nm/620 nm ratio) is obtained using an En Vision fluorometer. Additional binding assays are established between PD-1-Ig/PD-L2-His (20, 5 nM, respectively), CD80-His/PD-Ll-Ig (100, 10 nM, respectively) and CD80-His/CTLA4-Ig (10, 5 nM, respectively).
References

[1]. Louis S. Chupak, et al. Compounds useful as immunomodulators. WO 2015034820 A1

Chemical & Physical Properties

Density1.1±0.1 g/cm3
Boiling Point611.4±55.0 °C at 760 mmHg
Molecular FormulaC25H29N3O3
Molecular Weight419.516
Flash Point323.6±31.5 °C
Exact Mass419.220886
LogP3.99
Vapour Pressure0.0±1.8 mmHg at 25°C
Index of Refraction1.575
InChIKeyJEDPSOYOYVELLZ-UHFFFAOYSA-N
SMILESCOc1nc(OCc2cccc(-c3ccccc3)c2C)ccc1CNCCNC(C)=O
Storage condition-20℃

Synonyms

Acetamide, N-[2-[[[2-methoxy-6-[(2-methyl[1,1'-biphenyl]-3-yl)methoxy]-3-pyridinyl]methyl]amino]ethyl]-
N-{2-[({2-Methoxy-6-[(2-methyl-3-biphenylyl)methoxy]-3-pyridinyl}methyl)amino]ethyl}acetamide
PD-L1 inhibitor 1
BMS-202
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