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PX-866

Cat. No. M3682
PX-866 Structure
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

PX-866 inhibits the production of the secondary messenger phosphatidylinositol-3,4,5-trisphosphate (PIP3) and activation of the PI3K/Akt signaling pathway, which may result in inhibition of tumor cell growth and survival in susceptible tumor cell populations. PX-866 exhibits single agent in vivo anti-tumor activity and increases the anti-tumor effects of cisplatin and radiation treatment. In cancer cells grown in three-dimensional cultures, PX 866 reduces cell growth and motility without causing cytotoxicity. PX-866 and wortmannin both inhibit spheroid growth without causing cytotoxicity, similar to known cytostatic agents, such as rapamycin. PX-866 also inhibits cancer cell motility at subnanomolar concentrations.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 525.59
Formula C29H35NO8
CAS Number 502632-66-8
Purity >99%
Solubility DMSO 200 mg/mL
Ethanol 200 mg/mL
Storage at -20°C
References

The phosphatidylinositol 3-kinase inhibitor, PX-866, is a potent inhibitor of cancer cell motility and growth in three-dimensional cultures.
Howes AL, et al. Mol Cancer Ther. 2007 Sep;6(9):2505-14. PMID: 17766839.

Molecular pharmacology and antitumor activity of PX-866, a novel inhibitor of phosphoinositide-3-kinase signaling.
Ihle NT, et al. Mol Cancer Ther. 2004 Jul;3(7):763-72. PMID: 15252137.

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Keywords: PX-866 supplier, PI3K, inhibitors

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