PHY34

Catalog No.S8744

PHY34 Chemical Structure

Molecular Weight(MW): 582.55

PHY34 is a late-stage autophagy inhibitor with nanomolar potency and significant antitumor efficacy as a single agent against HGSOC in vivo.

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Biological Activity

Description PHY34 is a late-stage autophagy inhibitor with nanomolar potency and significant antitumor efficacy as a single agent against HGSOC in vivo.
Targets
autophagy [1]
()
In vitro

PHY34 is a cytotoxic compound in both HGSOC cell lines with an IC50 of 4 nM. It has nanomolar IC50s in both MDA-MB-435 and MDAMB-231 cell lines and is more cytotoxic against MDA-MB-231 (PHY34 IC50 in MDA-MB-435 = 23 nM, PHY34 IC50 in MDA-MB-231 = 5.2 nM). PHY34 treatment (100 nM) results in significant increases in early and late apoptotic cells in OVCAR3[1].

In vivo

PHY34 is bioavailable through intraperitoneal administration in vivo where it significantly inhibits the growth of cancer cell lines in hollow fibers, as well as reduces ovarian tumor burden in a xenograft model. Mice are dosed with 0.6 mg/kg IV, 1.8 mg/kg IP, or 75 mg/kg PO PHY34, the observed IP bioavailability (F) for PHY34 is 56.6% and for PO is 2.5%. Systemic clearance (Cl) following PO dose is 194.1 L/hr/kg, roughly 40 times the mouse liver blood flow, suggesting significant extrahepatic clearance. The Tmax of PHY34 (0.25 hr) suggests very fast absorption of this compound orally. PHY34 reduces tumor burden (OVCAR8 cells) in vivo[1].

Protocol

Cell Research:

[1]

+ Expand
  • Cell lines: OVCAR8 and OVCAR3 cells
  • Concentrations: 100 nM or 1 μM
  • Incubation Time: 24 h
  • Method:

    OVCAR8 and OVCAR3 cells are treated with PHY34 for 24 hours at 100 nM or 1 μM, respectively, and stained with either Lysotracker Red or acridine orange to monitor changes in the lysosomes due to autophagy inhibition using live confocal microscopy.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: ICR male mice (6 weeks in age)
  • Formulation: 50% PEG300:50% saline
  • Dosages: 3, 1, 0.6 and 0.3 mg/kg
  • Administration: i.v.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (171.65 mM)
Ethanol 42 mg/mL (72.09 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 582.55
Formula

C30H30O12

CAS No. 2130033-55-3
Storage powder
in solvent
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Autophagy Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID