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

| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 1 mg | $41 | In Stock | In Stock | |
| 5 mg | $102 | In Stock | In Stock | |
| 10 mg | $163 | In Stock | In Stock | |
| 25 mg | $323 | In Stock | In Stock | |
| 50 mg | $538 | In Stock | In Stock | |
| 100 mg | $633 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $108 | In Stock | In Stock |
| Description | BMS-202 (PD1-PDL1 inhibitor 2) is a non-peptide PD-1/PD-L complex inhibitor with an IC50 of 18 nM and a KD of 8 μM. BMS-202 binds to PD-L1 with high affinity and blocks human PD-1/PD-L interactions, exhibiting antitumor activity. |
| Targets & IC50 | PD-1/PD-L1:0.018 μM |
| In vitro | Methods: HFB cell monolayers were treated with BMS-202 (0, 1, 2.5, 5 nM) for 24 hours, and scratch area measurements at 0h and 24h were compared. HFB monolayer cells were treated with BMS-202 (0, 1, 2.5, 5 nM) for 24 hours. After treatment, 0.5 μCi [³H]-proline was added, and incubation continued for 24 hours. Radioactive incorporation was then measured. Results: BMS-202 concentration-dependently inhibited HFB migration and collagen synthesis. [1] Methods: A375 melanoma cells were treated with BMS-202 (5 μM) or mitochondrial pyruvate carrier inhibitor GW604714X (10 μM) for 24 hours. Cell viability was assessed using the CCK-8 assay. Results: Combined treatment exhibited stronger cell viability suppression and apoptosis induction than either agent alone, indicating that mitochondrial dysfunction potentiates the antitumor effects of BMS-202. [2] |
| In vivo | Methods: A375 cells were subcutaneously implanted into nude mice to establish a melanoma xenograft model. Once tumors became palpable, BMS-202 (20 mg/kg) was administered via intraperitoneal injection every 3 days. Mice were euthanized on the third day after the third injection. Results: Tumor growth was significantly slowed in the BMS-202-treated group, with a marked reduction in the proportion of Ki-67-positive cells in tumor tissue, confirming an antiproliferative effect in vivo. [2] |
| Synonyms | PD1-PDL1 inhibitor 2, PD-1/PD-L1 inhibitor 2 |
| 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). |
| Molecular Weight | 419.52 |
| Formula | C25H29N3O3 |
| Cas No. | 1675203-84-5 |
| Smiles | COc1nc(OCc2cccc(c2C)-c2ccccc2)ccc1CNCCNC(C)=O |
| Relative Density. | 1.133 g/cm3 (Predicted) |
| Storage | Store at low temperature Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 45 mg/mL (107.27 mM), Sonication is recommended. Ethanol: 83 mg/mL (197.85 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4.5 mg/mL (10.73 mM), Solution. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO/Ethanol
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | ||||||||||||||||||||||||||||||||||||
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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