MDL | - |
---|---|
Molecular Weight | 472.58 |
Molecular Formula | C27H32N6O2 |
SMILES | O=C(N1[C@@H](C)CC[C@@H](N)C1)C2=CC(OC)=C3C(N=C(C4=CC5=CC=CN=C5N4CC6CC6)N3C)=C2 |
BMS-P5 free base is a specific and orally active peptidylarginine deiminase 4 (PAD4) inhibitor. BMS-P5 free base blocks MM-induced NET formation and delays progression of MM in a syngeneic mouse model [1] .
BMS-P5 blocks calcium ionophore-induced citrullination of histone H3
[1]
.
BMS-P5 is also able to inhibit formation of NETs induced by primary MM cells isolated from the BM of patients with MM
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay [1] .
Cell Line: | Neutrophils. |
Concentration: | 10 µM and 100 µM. |
Incubation Time: | 30 min followed by addition of DP42 or 5TGM1 CM. |
Result: | Prevented MM-induced NET formation. |
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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. |
Solid
Room temperature in continental US; may vary elsewhere.
Powder | -20°C | 3 years |
---|---|---|
4°C | 2 years | |
In solvent | -80°C | 6 months |
-20°C | 1 month |
DMSO : 250 mg/mL ( 529.01 mM ; Need ultrasonic)
Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
---|
1 mM | 2.1160 mL | 10.5802 mL | 21.1604 mL |
5 mM | 0.4232 mL | 2.1160 mL | 4.2321 mL |
10 mM | 0.2116 mL | 1.0580 mL | 2.1160 mL |