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.


Chemical Structure

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PX-316
CAS# 253440-95-8

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

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

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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

InChi Key: GJZGRYXGQBWBEB-AVMFAVRISA-N

InChi Code: InChI=1S/C28H57O10P/c1-3-4-5-6-7-8-9-10-11-12-13-14-15-16-17-18-19-36-21-23(35-2)22-37-39(33,34)38-28-25(30)20-24(29)26(31)27(28)32/h23-32H,3-22H2,1-2H3,(H,33,34)/t23-,24-,25-,26+,27-,28-/m1/s1

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

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).

HS Tariff Code: 2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 584.71994 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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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.

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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.



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