| CAS NO: | 1675203-84-5 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 2mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| Molecular Weight (MW) | 419.52 |
|---|---|
| Formula | C25H29N3O3 |
| CAS No. | 1675203-84-5 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 83 mg/mL (197.8 mM) |
| Water:<1 mg/mL (slightly soluble or insoluble) | |
| Ethanol: 83 mg/mL (197.8 mM) | |
| SMILES Code | CC(NCCNCC1=CC=C(OCC2=C(C)C(C3=CC=CC=C3)=CC=C2)N=C1OC)=O |
| Chemical Name | N-(2-(((2-methoxy-6-((2-methyl-[1,1'-biphenyl]-3-yl)methoxy)pyridin-3-yl)methyl)amino)ethyl)acetamide |
| Synonym | BMS-202; PD-1/PD-L1 inhibitor 2; BMS 202; BMS202; |
| In Vitro | 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). Cell Assay: The programmed death-1/programmed death-ligand 1 (PD-1/PD-L1) interaction plays a dominant role in the suppression of T cell responses, especially in a tumor microenvironment, protecting tumor cells from lysis. PD-1/PD-L1 inhibitor 2 is reported to prevent the interaction of PD-L1 with PD-1 with an IC50 value of 18 nM. |
|---|---|
| In Vivo | N/A |
| Animal model | N/A |
| Formulation & Dosage | N/A |
| References | Nat Rev Cancer. 2012 Mar 22;12(4):252-64; J Med Chem. 2017 Jul 13;60(13):5857-5867; WO 2015034820 A1 |
Structural Biology of the Immune Checkpoint Receptor PD-1 and Its Ligands PD-L1/PD-L2. Structure. 2017 Aug 1;25(8):1163-1174. |
New Directions in Designing the Therapeutics Targeting the PD-1/PD-L1 Interaction. Structure. 2017 Aug 1;25(8):1163-1174. |
Structural Basis of the PD-1/PD-L1 (PD-L2) Interaction. Structure. 2017 Aug 1;25(8):1163-1174. |
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