VU 0364739 hydrochloride

Modify Date: 2024-02-06 17:24:18

VU 0364739 hydrochloride Structure
VU 0364739 hydrochloride structure
Common Name VU 0364739 hydrochloride
CAS Number 1244640-48-9 Molecular Weight 482.978
Density N/A Boiling Point N/A
Molecular Formula C26H28ClFN4O2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of VU 0364739 hydrochloride


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].

 Names

Name VU 0364739 hydrochloride
Synonym More Synonyms

 VU 0364739 hydrochloride Biological Activity

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
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.  

 Chemical & Physical Properties

Molecular Formula C26H28ClFN4O2
Molecular Weight 482.978
Exact Mass 482.188477

 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)