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Cat #: V3677 CAS #: 1675204-51-9 Purity ≥ 98%
Description: BMS-242 is a novel and potent small molecule inhibitor of the PD-1/PD-L1 protein protein interaction with IC50 value in the range of 6-100 nM in cell free assays. It was first discovered by Bristol-Myers Squibb. Blockade of the PD-1/PD-L1 immune checkpoint pathway with monoclonal antibodies has provided significant advances in cancer treatment. The antibody-based immunotherapies carry a number of disadvantages such as the high cost of the antibodies, their limited half-life, and immunogenicity. Development of small-molecule PD-1/PD-L1 inhibitors that could overcome these drawbacks is slow because of the incomplete structural information for this pathway. The first chemical PD-1/PD-L1 inhibitors, BMS-1001 and its analogs, have been recently disclosed by Bristol-Myers Squibb.
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Molecular Weight (MW) | 449.59 |
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Molecular Formula | C28H35NO4 |
CAS No. | 1675204-51-9 |
Storage | -20℃ for 3 years in powder form |
-80℃ for 2 years in solvent | |
Solubility In Vitro | DMSO: 10mM |
Water: | |
Ethanol: | |
SMILES Code | CC(C)[C@@H](NCC1=C(OC)C=C(OCC2=C(C)C(C3=CC=CC=C3)=CC=C2)C=C1OC)CO |
Synonyms | BMS-242; BMS 242; BMS242 |
Protocol | In Vitro | In vitro activity: BMS-1001 is a novel and potent small molecule inhibitor of the PD-1/PD-L1 protein protein interaction with IC50 value of 2.25 nM in cell free assays. Kinase Assay: BMS disclosed recently the first nonpeptidic small molecule inhibitors against the PD-1/PD-L1 pathway that showed the activity in a homogeneous time-resolved fluorescence (HTRF) binding assay; however no further data supporting their activity were provided. Cell Assay: |
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Solvent volume to be added | Mass (the weight of a compound) | |||
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Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
1mM | 2.2242 mL | 11.1212 mL | 22.2425 mL | 44.4850 mL |
5mM | 0.4448 mL | 2.2242 mL | 4.4485 mL | 8.8970 mL |
10mM | 0.2224 mL | 1.1121 mL | 2.2242 mL | 4.4485 mL |
20mM | 0.1112 mL | 0.5561 mL | 1.1121 mL | 2.2242 mL |
This equation is commonly abbreviated as: C1 V1 = C2 V2
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.