PX-866 Inhibitor CAS No. 502632-66-8

Cat. No.	Name	Size	Price
KI2091	PX-866	5 mg	$390
	PX-866	10 mg	$676
	PX-866	25 mg	$1170
	PX-866	50 mg	$1820

Chemical Characteristic

Product Name	PX-866
Synonyms	PX866
CAS No.	502632-66-8
Molecular Weight	525.2
Formula	C₂₉H₃₅NO₈
Chemical Name	(1e,4s,4ar,5r,6as,9ar)-5-(acetyloxy)-1-((di-2-propen-1-ylamino)methylene)-4,4a,5,6,6a,8,9,9a-octahydro-11-hydroxy-4-(methoxymethyl)-4a,6a-dimethyl-cyclopenta(5,6)naphtho(1,2-c)pyran-2,7,10(1h)-trione
Smiles	[C@H]1([C@]2(C(=C(C(=O)C3=C2[C@@H](C[C@]2([C@H]3CCC2=O)C)OC(=O)C)O)/C(=C\N(CC=C)CC=C)/C(=O)O1)C)COC
Chemical Structure

Biological activities

PX-866, a derivative of wortmannin, is a potent PI3 Kinase inhibitor. PX-866 inhibits purified PI3 Kinase with an IC50 of 0.1 nM and PI3 Kinase signaling measured by phospho-Ser473-Akt levels in HT-29 colon cancer cells with an IC50 of 20 nM. In vivo in HT-29 colon tumor xenografts, PX-866 administration (10 mg/kg) inhibits phospho-Ser473-Akt up to 80% with recovery taking >48 hours after p.o. administration but more rapidly after i.v. or i.p. administration. In vivo, PX-866 administration also enhances the antitumor activity of cisplatin against A-549 xenografts and radiation treatment against OvCar-3 xenografts.^[1]

Protocols

In vivo: For iv administration to mice, PX-866 is dissolved at 10 mg/mL in 5% ethanol in 0.9% NaCl and for oral administration at 5 mg/mL in 5% ethanol in water.^[2]

References

[1] Ihle NT, et al. Molecular pharmacology and antitumor activity of PX-866, a novel inhibitor of phosphoinositide-3-kinase signaling. Mol Cancer Ther. 2004, 3(7): 763-772. [2] Ihle NT, et al. The phosphatidylinositol-3-kinase inhibitor PX-866 overcomes resistance to the epidermal growth factor receptor inhibitor gefitinib in A-549 human non-small cell lung cancer xenografts. Mol Cancer Ther. 2005, 4(9): 1349-1357.

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