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PHY34 Autophagy inhibitor

Cat.No.S8744

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

Chemical Structure

Molecular Weight: 582.55

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Quality Control

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

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (171.65 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 42 mg/mL

Water : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 582.55 Formula

C30H30O12

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 2130033-55-3 -- Storage of Stock Solutions

Synonyms N/A Smiles COC1=CC2=C(C=C1OC)C(=C3C(=O)OCC3=C2OC4OC(CO)C5OC(C)(C)OC5C4O)C6=CC=C7OCOC7=C6

Mechanism of Action

Targets/IC50/Ki
autophagy
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 (this compound IC50 in MDA-MB-435 = 23 nM, this compound IC50 in MDA-MB-231 = 5.2 nM). This compound treatment (100 nM) results in significant increases in early and late apoptotic cells in OVCAR3.
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 of this compound, the observed IP bioavailability (F) for this compound 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 this chemical (0.25 hr) suggests very fast absorption of this compound orally. This compound reduces tumor burden (OVCAR8 cells) in vivo.
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