PX-316

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 406158

CAS#: 253440-95-8

Description: PX-316 is a AKT inhibior. PX-316, when administered intraperitoneally to mice at 150 mg/kg, inhibits Akt activation in HT-29 human tumor xenografts up to 78% at 10 h with recovery to 34% at 48 h. PX-316 has antitumor activity against early human MCF-7 breast cancer and HT-29 colon cancer xenografts in mice. PX-316 formulated in 20% hydroxypropyl-beta-cyclodextrin for intravenous administration is well tolerated in mice and rats with no hemolysis and no hematological toxicity. Thus, PX-316 is the lead compound of a new class of potential agents that inhibit Akt survival signaling.


Price and Availability

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PX-316 is not in stock, may be available through custom synthesis. For cost-effective reason, minimum 1 gram order is requested. The product will be characterized by NMR, HPLC and MS analysis. Purity (HPLC) is usually >98%. CoA, QC data, MSDS will be provided when product is successfully made. The estimated lead time is 2-3 months. Please send email to sales@medkoo.com to inquire quote.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 406158
Name: PX-316
CAS#: 253440-95-8
Chemical Formula: C28H57O10P
Exact Mass: 584.36893
Molecular Weight: 584.71994
Elemental Analysis: C, 57.51; H, 9.83; O, 27.36; P, 5.30


Synonym: PX-316; PX 316; PX316.

IUPAC/Chemical Name: (R)-2-methoxy-3-(octadecyloxy)propyl ((1R,2R,3S,4R,6R)-2,3,4,6-tetrahydroxycyclohexyl) hydrogen phosphate

SMILES Code: O=P(O[C@H]1[C@H](O)[C@@H](O)[C@H](O)C[C@H]1O)(OC[C@H](OC)COCCCCCCCCCCCCCCCCCC)O


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO

Shelf Life:
>5 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


Additional Information

  
 
 
 


References

1: Busch F, Mobasheri A, Shayan P, Lueders C, Stahlmann R, Shakibaei M. Resveratrol modulates interleukin-1β-induced phosphatidylinositol 3-kinase and nuclear factor κB signaling pathways in human tenocytes. J Biol Chem. 2012 Nov 2;287(45):38050-63. doi: 10.1074/jbc.M112.377028. Epub 2012 Aug 30. PubMed PMID: 22936809; PubMed Central PMCID: PMC3488075.

2: Wu PH, Lin SK, Lee BS, Kok SH, Wang JH, Hou KL, Yang H, Lai EH, Wang JS, Hong CY. Epigallocatechin-3-gallate diminishes cytokine-stimulated Cyr61 expression in human osteoblastic cells: a therapeutic potential for arthritis. Rheumatology (Oxford). 2012 Nov;51(11):1953-65. doi: 10.1093/rheumatology/kes174. Epub 2012 Jul 28. PubMed PMID: 22843790.

3: Jang ER, Kim YJ, Myung SC, Kim W, Lee CS. Different effect of protein kinase B/Akt and extracellular signal-regulated kinase inhibition on trichostatin A-induced apoptosis in epithelial ovarian carcinoma cell lines. Mol Cell Biochem. 2011 Jul;353(1-2):1-11. doi: 10.1007/s11010-011-0768-7. Epub 2011 Mar 6. PubMed PMID: 21380726.

4: Krech T, Thiede M, Hilgenberg E, Schäfer R, Jürchott K. Characterization of AKT independent effects of the synthetic AKT inhibitors SH-5 and SH-6 using an integrated approach combining transcriptomic profiling and signaling pathway perturbations. BMC Cancer. 2010 Jun 14;10:287. doi: 10.1186/1471-2407-10-287. PubMed PMID: 20546605; PubMed Central PMCID: PMC2895615.

5: Slomiany BL, Slomiany A. Constitutive nitric oxide synthase-mediated caspase-3 S-nitrosylation in ghrelin protection against Porphyromonas gingivalis-induced salivary gland acinar cell apoptosis. Inflammopharmacology. 2010 Jun;18(3):119-25. doi: 10.1007/s10787-010-0035-7. Epub 2010 Feb 13. PubMed PMID: 20155328.

6: Gessi S, Sacchetto V, Fogli E, Merighi S, Varani K, Baraldi PG, Tabrizi MA, Leung E, Maclennan S, Borea PA. Modulation of metalloproteinase-9 in U87MG glioblastoma cells by A3 adenosine receptors. Biochem Pharmacol. 2010 May 15;79(10):1483-95. doi: 10.1016/j.bcp.2010.01.009. Epub 2010 Jan 21. PubMed PMID: 20096265.

7: Sethi G, Ahn KS, Sung B, Kunnumakkara AB, Chaturvedi MM, Aggarwal BB. SH-5, an AKT inhibitor potentiates apoptosis and inhibits invasion through the suppression of anti-apoptotic, proliferative and metastatic gene products regulated by IkappaBalpha kinase activation. Biochem Pharmacol. 2008 Dec 1;76(11):1404-16. doi: 10.1016/j.bcp.2008.05.023. Epub 2008 Jul 5. PubMed PMID: 18606397.

8: Williams R, Baker AF, Ihle NT, Winkler AR, Kirkpatrick L, Powis G. The skin and hair as surrogate tissues for measuring the target effect of inhibitors of phosphoinositide-3-kinase signaling. Cancer Chemother Pharmacol. 2006 Oct;58(4):444-50. Epub 2006 Feb 17. PubMed PMID: 16485116; PubMed Central PMCID: PMC1486800.

9: Meuillet EJ, Ihle N, Baker AF, Gard JM, Stamper C, Williams R, Coon A, Mahadevan D, George BL, Kirkpatrick L, Powis G. In vivo molecular pharmacology and antitumor activity of the targeted Akt inhibitor PX-316. Oncol Res. 2004;14(10):513-27. PubMed PMID: 15559765.

10: He J, Cheung AP, Wang E, Fang K, Liu P. High-performance liquid chromatographic analysis for a non-chromophore-containing phosphatidyl inositol analog, 1-((1-O-octadecyl-2-O-methyl-sn-glycero)phospho)-1D-3-deoxy-myo-inositol, using indirect UV detection. J Chromatogr A. 2001 Apr 13;913(1-2):355-63. PubMed PMID: 11355833.