产品说明书

Penfluridol

Print
Chemical Structure| 26864-56-2 同义名 : R-16341
CAS号 : 26864-56-2
货号 : A179670
分子式 : C28H27ClF5NO
纯度 : 98%
分子量 : 523.965
MDL号 : MFCD00866714
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(200.4 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • D1 receptor

    Dopamine receptor, Ki:1.6 μM
描述 Penfluridol has robust antipsychotic efficacy and is a first-generation diphenylbutylpiperidine. Its effects last for several days after a single oral dose and it can be administered once a week to provide better compliance and symptom control. In addition; the anti-cancer effects of penfluridol have been demonstrated in vivo: results showed slight changes in the volume and weight of organs at doses tested in animals[3]. Penfluridol concentration-dependently suppressed the cell viability of AML cells with FLT3-WT (Fms-like tyrosine kinase 3) (HL-60 and U937) and FLT3-ITD (MV4-11); penfluridol's augmentation of intracellular ROS levels was critical for the penfluridol-induced autophagic response. The combination of penfluridol with an autophagy inhibitor may be a novel strategy for AML (acute myeloid leukemia) harboring FLT3-WT and FLT3-ITD[4]. Penfluridol treatment suppressed the growth of BxPC-3 tumor xenografts by 48% as compared to 17% when treated in combination with chloroquine. Similarly, penfluridol suppressed the growth of AsPC-1 tumors by 40% versus 16% when given in combination with chloroquine[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.91mL

0.38mL

0.19mL

9.54mL

1.91mL

0.95mL

19.09mL

3.82mL

1.91mL
参考文献

[1]Flaim SF, Brannan MD, et al. Neuroleptic drugs attenuate calcium influx and tension development in rabbit thoracic aorta: effects of pimozide, penfluridol, chlorpromazine, and haloperidol. Proc Natl Acad Sci U S A. 1985 Feb;82(4):1237-41.

[2]Creese I, Burt DR, Snyder SH. Dopamine receptor binding predicts clinical and pharmacological potencies of antischizophrenic drugs. Science. 1976 Apr 30;192(4238):481-3.

[3]Tuan NM, Lee CH. Penfluridol as a Candidate of Drug Repurposing for Anticancer Agent. Molecules. 2019;24(20):3659.

[4]Wu SY, Wen YC, Ku CC, et al. Penfluridol triggers cytoprotective autophagy and cellular apoptosis through ROS induction and activation of the PP2A-modulated MAPK pathway in acute myeloid leukemia with different FLT3 statuses. J Biomed Sci. 2019;26(1):63.

[5]Ranjan A, Srivastava SK. Penfluridol suppresses pancreatic tumor growth by autophagy-mediated apoptosis. Sci Rep. 2016;6:26165.