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Apoptosis PD-1/PD-L1 PD1-PDL1 inhibitor 2

PD1-PDL1 inhibitor 2

Catalog No. T3146   CAS 1675203-84-5
Synonyms: BMS-202, PD-1/PD-L1 inhibitor 2
Purity 98.54% Datasheet MSDS

PD1-PDL1 inhibitor 2 is an inhibitor of the PD-1 (Programmed death- 1) /PD-Ll (Programmed death-ligand 1) protein/protein interaction, extracted from patent WO/2015034820 A1.

PD1-PDL1 inhibitor 2, CAS 1675203-84-5
Pack Size Availability Price/USD Quantity
2 mg In stock 64.00
5 mg In stock 114.00
10 mg In stock 182.00
25 mg In stock 359.00
50 mg In stock 642.00
100 mg In stock 1100.00
1 mL * 10 mM (in DMSO) In stock 121.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description PD1-PDL1 inhibitor 2 is an inhibitor of the PD-1 (Programmed death- 1) /PD-Ll (Programmed death-ligand 1) protein/protein interaction, extracted from patent WO/2015034820 A1.
Targets&IC50 PD-1/PD-L1 :ic50 0.018μM,  
In vitro BMS-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 Assay All 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).

Description

PD1-PDL1 inhibitor 2 is an inhibitor of the PD-1 (Programmed death- 1) /PD-Ll (Programmed death-ligand 1) protein/protein interaction, extracted from patent WO/2015034820 A1.

Targets&IC50

PD-1/PD-L1 :ic50 0.018μM

In Vitro

BMS-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 Assay

All 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).

Synonyms BMS-202, PD-1/PD-L1 inhibitor 2
Purity 98.00%
Appearance solid
Molecular Weight 419.52
Formula C25H29N3O3
CAS No. 1675203-84-5

Storage

-20℃ 3 years powder

-80℃ 2 years in solvent

Solubility Information

DMSO: 76 mg/mL (181.2 mM)

Ethanol: 83 mg/mL (197.85 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
1. Louis S. Chupak, et al. Compounds useful as immunomodulators. WO 2015034820 A1

Related Compound Libraries

This product is contained In the following compound libraries:
Bioactive Compound Library Inhibitor Library Anti-cancer Compound Library Apoptosis Compound Library Immunology/Inflammation Compound Library Cell cycle related Compound Library

Related Products

Related compounds with same targets
BMS202 hydrochloride (1675203-84-5(free base)) Phellodendrine chloride PD-1/PD-L1 inhibitor 1 Avelumab (anti- PD-L1) Atezolizumab (anti-PD-L1) BMS-1001 PD1-PDL1 inhibitor 2 Nivolumab (anti-PD-1)

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