PHY34

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

PHY34 Chemical Structure

PHY34 Chemical Structure

CAS No. 2130033-55-3

Purity & Quality Control

Batch: S874401 DMSO]100 mg/mL]false]Ethanol]42 mg/mL]false]Water]Insoluble]false Purity: 98.43%
98.43

PHY34 Related Products

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
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].

Cell Research 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.

In Vivo
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].

Animal Research Animal Models ICR male mice (6 weeks in age)
Dosages 3, 1, 0.6 and 0.3 mg/kg
Administration i.v.

Chemical Information & Solubility

Molecular Weight 582.55 Formula

C30H30O12

CAS No. 2130033-55-3 SDF --
Smiles COC1=CC2=C(C=C1OC)C(=C3C(=O)OCC3=C2OC4OC(CO)C5OC(C)(C)OC5C4O)C6=CC=C7OCOC7=C6
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (171.65 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 42 mg/mL

Water : Insoluble


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In vivo
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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

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