Name: PF-8380
Brand: SIGMA

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About This Item

经验公式（希尔记法）:

C₂₂H₂₁Cl₂N₃O₅

CAS Number:

1144035-53-9

分子量:

478.33

UNSPSC代码:

12352200

NACRES:

NA.77

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质量水平

100

方案

≥98% (HPLC)

表单

powder

颜色

white to beige

溶解性

DMSO: 5 mg/mL, clear (warmed)

储存温度

−20°C

SMILES字符串

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

应用

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.

生化/生理作用

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.

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).