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BMS-202

Catalog No. T3146 CAS 1675203-84-5

Synonyms: PD1-PDL1 inhibitor 2, PD-1/PD-L1 inhibitor 2

BMS-202 (PD1-PDL1 inhibitor 2) is an inhibitor of the PD-1 (Programmed death- 1) /PD-Ll (Programmed death-ligand 1) protein/protein interaction.

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BMS-202, CAS 1675203-84-5

Pack Size	Availability	Price/USD
2 mg	In stock	$ 57.00
5 mg	In stock	$ 102.00
10 mg	In stock	$ 163.00
25 mg	In stock	$ 323.00
50 mg	In stock	$ 577.00
100 mg	In stock	$ 634.00
1 mL * 10 mM (in DMSO)	In stock	$ 108.00

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Purity: 99.09%

Purity: 98.54%

Purity: 98.24%

Purity: 97.92%

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Storage & Solubility Information

Description	BMS-202 (PD1-PDL1 inhibitor 2) is an inhibitor of the PD-1 (Programmed death- 1) /PD-Ll (Programmed death-ligand 1) protein/protein interaction.
Targets&IC50	PD-1/PD-L1:0.018 μM
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	PD1-PDL1 inhibitor 2, PD-1/PD-L1 inhibitor 2
Molecular Weight	419.52
Formula	C25H29N3O3
CAS No.	1675203-84-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 76 mg/mL(181.2 mM)

Ethanol: 83 mg/mL (197.85 mM)

References and Literature

1. Louis S. Chupak, et al. Compounds useful as immunomodulators. WO 2015034820 A1 2. Yang X, Cheng B, Xiao Y, et al. Discovery of Novel CA-4 Analogs as Dual Inhibitors of Tubulin Polymerization and PD-1/PD-L1 Interaction for Cancer Treatment[J]. European Journal of Medicinal Chemistry. 2020: 113058.

Citations

1. Dai W, Wu J, Peng X, et al. CDK12 orchestrates super‐enhancer‐associated CCDC137 transcription to direct hepatic metastasis in colorectal cancer. Clinical and Translational Medicine. 2022, 12(10): e1087. 2. Yang X, Cheng B, Xiao Y, et al. Discovery of Novel CA-4 Analogs as Dual Inhibitors of Tubulin Polymerization and PD-1/PD-L1 Interaction for Cancer Treatment. European Journal of Medicinal Chemistry. 2021 Mar 5;213:113058. doi: 10.1016 3. Zhang H, Zhou S, Plewka J, et al.Design, Synthesis, and Antitumor Activity Evaluation of 2-Arylmethoxy-4-(2, 2′-dihalogen-substituted biphenyl-3-ylmethoxy) Benzylamine Derivatives as Potent PD-1/PD-L1 Inhibitors.Journal of Medicinal Chemistry.2023 4. Zhang H, Zhou S J, Shen C F, et al.PD-L1 dimerisation induced by biphenyl derivatives mediates anti-breast cancer activity via the non-immune PD-L1–AKT–mTOR/Bcl2 pathway.Journal of Enzyme Inhibition and Medicinal Chemistry.2023, 38(1): 2230388.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Inhibitor Library Anti-Cancer Compound Library PPI Inhibitor Library Apoptosis Compound Library CNS-Penetrant Compound Library Anti-Breast Cancer Compound Library Anti-COVID-19 Compound Library Bioactive Compounds Library Max Bioactive Compound Library

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Keywords

BMS-202 1675203-84-5 Apoptosis Cell Cycle/Checkpoint Immunology/Inflammation PD-1/PD-L1 BMS202 antitumor PD1-PDL1 inhibitor 2 PD-1/PD-L1 inhibitor 2 dimeric anti-proliferation BMS 202 nonpeptidic immune-response Thermal stabilization Inhibitor inhibit hydrophobic inhibitor

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