| Identification | Back Directory | [Name]
BMS-P5 | [CAS]
1550371-22-6 | [Synonyms]
BMS-P5
BMS-P5 free base
Methanone, [(2S,5R)-5-amino-2-methyl-1-piperidinyl][2-[1-(cyclopropylmethyl)-1H-pyrrolo[2,3-b]pyridin-2-yl]-7-methoxy-1-methyl-1H-benzimidazol-5-yl]- | [Molecular Formula]
C27H32N6O2 | [MOL File]
1550371-22-6.mol | [Molecular Weight]
472.58 |
| Chemical Properties | Back Directory | [Boiling point ]
728.7±70.0 °C(Predicted) | [density ]
1.40±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMF: 20 mg/ml,DMSO: 5 mg/ml,Ethanol: 30 mg/ml,Ethanol:PBS (pH 7.2) (1:8): 0.11 mg/ml | [form ]
A crystalline solid | [pka]
9.87±0.40(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
BMS-P5 free base is a selective and orally active peptidylarginine deiminase 4 (PAD4) inhibitor with an IC50 of 98 nM. BMS-P5 free base shows selective for PAD4 over PAD1, PAD2, and PAD3. BMS-P5 free base blocks multiple myeloma (MM)-induced neutrophil extracellular trap (NET) formation and delays progression of MM in a syngeneic mouse model[1]. | [in vivo]
BMS-P5 (50 mg/kg, oral gavage) significantly improves survival of MM-bearing mice[1].
BMS-P5 (50 mg/kg, oral gavage) may attenuate the presence of pro-tumorigenic proteins in the tumor microenvironment, and thus delay tumor progression[1].
| Animal Model: | Syngeneic mouse model of MM[1]. | | Dosage: | 50 mg/kg. | | Administration: | Oral gavage, twice a day beginning on day 3 after tumor cell injection. | | Result: | Significantly delayed development of symptoms and significantly prolonged survival of MM-bearing mice. |
| [References]
[1] Marina Li, et al. A Novel Peptidylarginine Deiminase 4 (PAD4) Inhibitor BMS-P5 Blocks Formation of Neutrophil Extracellular Traps and Delays Progression of Multiple Myeloma. Mol Cancer Ther. 2020 Jul;19(7):1530-1538. DOI:10.1158/1535-7163.MCT-19-1020 |
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