PHY34

Catalog No.S8744 Batch:S874401

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Technical Data

Formula

C30H30O12
Molecular Weight 582.55 CAS No. 2130033-55-3
Solubility (25°C)* In vitro DMSO 100 mg/mL (171.65 mM)
Ethanol 42 mg/mL (72.09 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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 (from reference)

Cell Assay:

[1]
  • 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.
Animal Study:

[1]
  • Animal Models

    ICR male mice (6 weeks in age)

  • Dosages

    3, 1, 0.6 and 0.3 mg/kg

  • Administration

    i.v.

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.