1244640-48-9

1244640-48-9 structure

Name: VU 0364739 hydrochloride
Chemical Name: VU 0364739 hydrochloride
CAS Number: 1244640-48-9
Molecular Formula: C₂₆H₂₈ClFN₄O₂
Molecular Weight: 482.978
Catalog: Signaling Pathways Metabolic Enzyme/Protease Phospholipase
Create Date: 2021-05-04 08:40:22
Modify Date: 2024-02-06 17:24:18
VU 0364739 hydrochloride is a highly selective phospholipase D2 (PLD2) inhibitor with IC50s of 20 and 1500 nM for PLD2 and PLD1, respectively. VU 0364739 hydrochloride induces apoptosis and it can be used for cancer research[1].

Name	VU 0364739 hydrochloride
Synonyms	N-{2-[1-(3-Fluorophenyl)-4-oxo-1,3,8-triazaspiro[4.5]dec-8-yl]ethyl}-2-naphthamide hydrochloride (1:1) 2-Naphthalenecarboxamide, N-[2-[1-(3-fluorophenyl)-4-oxo-1,3,8-triazaspiro[4.5]dec-8-yl]ethyl]-, hydrochloride (1:1)

Description	VU 0364739 hydrochloride is a highly selective phospholipase D2 (PLD2) inhibitor with IC50s of 20 and 1500 nM for PLD2 and PLD1, respectively. VU 0364739 hydrochloride induces apoptosis and it can be used for cancer research[1].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> Metabolic Enzyme/Protease >> Phospholipase
Target	PLD2:20 nM (IC50) PLD1:1500 nM (IC50)
In Vitro	VU 0364739 (1，5 和 10 μM；24，48，72 和 96 小时) 在无血清条件下时间和剂量依赖性地降低 MDA-MB-231 细胞活力[1]。 VU 0364739 (1，10 和 100 μM；48 小时) 增加 Caspase 3 和 Caspase 7 活性。 Cell Proliferation Assay[1] Cell Line: MDA-MB-231 cell line Concentration: 10 μM Incubation Time: 24 hours Result: Inhibited cell proliferation of MDA-MB-231 cells. Apoptosis Analysis[1] Cell Line: MDA-MB-231 cell line Concentration: 1, 10 and 100 μM Incubation Time: 48 hours Result: Induced cell apoptosis at a dose of 10 μM under serum-free condition or 10% FBS containg condition.
In Vivo	1.19Pharmacokinetic Properties of VU 0364739 in Rats[1]. Rats IV 1 mg/kg Rats PO 10 mg/kg CL (mL/min/kg) 61.5 t1/2 (h) 1.52 Vdss (L/kg) 8.1 plasma (ng/mL) 39.9 brain (ng/mL) 29
References	[1]. Lavieri RR, et al. Design, synthesis, and biological evaluation of halogenated N-(2-(4-oxo-1-phenyl-1,3,8-triazaspiro[4.5]decan-8-yl)ethyl)benzamides: discovery of an isoform-selective small molecule phospholipase D2 inhibitor. J Med Chem. 2010 Sep 23;53(18):6706-19.