SML0715

PF-8380

≥98% (HPLC)

• Synonym(e): 4-[3-(2,3-Dihydro-2-oxo-6-benzoxazolyl)-3-oxopropyl]-1-piperazinecarboxylic acid (3,5-dichlorophenyl)methyl ester, 4-[3-Oxo-3-(2-oxo-2,3-dihydrobenzoxazol-6-yl)propyl]piperazine-1-carboxylic acid 3,5-dichlorobenzyl ester
• Empirische Formel (Hill-System): C₂₂H₂₁Cl₂N₃O₅
• CAS-Nummer: 1144035-53-9
• Molekulargewicht: 478.33
• UNSPSC Code: 12352200
• NACRES: NA.77
• Assay: ≥98% (HPLC)
• Form: powder

Eigenschaften

• Quality Segment: 100
• assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 5 mg/mL, clear (warmed)
• storage temp.: −20°C
• SMILES string: Clc1cc(cc(c1)COC(=O)N2CCN(CC2)CCC(=O)c3cc4[o][c]([nH]c4cc3)=O)Cl
• InChI: 1S/C22H21Cl2N3O5/c23-16-9-14(10-17(24)12-16)13-31-22(30)27-7-5-26(6-8-27)4-3-19(28)15-1-2-18-20(11-15)32-21(29)25-18/h1-2,9-12H,3-8,13H2,(H,25,29)
• InChI key: JMSUDQYHPSNBSN-UHFFFAOYSA-N

Beschreibung

Application

PF-8380 has been used in biological assays. It has also been used to estimate the role of intestinally-derived lysophosphatidic acid in dyslipidemia and atherosclerosis.

Biochem/physiol Actions

PF-8380 [6-(3-(piperazin-1-yl)propanoyl)benzo[d]oxazol-2(3H)-one] has the ability to change the resistant and invasive features of glioblastoma and helps to improve the response to radiation therapy.[1]

PF-8380 is a potent orally bioavailable inhibitor of autotaxin (ATX), the enzyme that synthesize lysophosphatidic acid (LPA) from lysophosphatidyl choline, and is an emerging target for treatment of inflammatory conditions, including cancer, arthritis and multiple sclerosis. PF-8380 blocks inflammation-induced LPA synthesis. PF-8380 works both in vitro and in vivo through direct inhibition of autotaxin. In human whole blood PF-8380 inhibited autotaxin with an IC₅₀ of 101 nM.

PF-8380 is a potent orally bioavailable inhibitor of autotaxin (ATX).

Sicherheitshinweise

• Lagerklasse: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable