PF-4708671
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 406432

CAS#: 1255517-76-0

Description: PF-4708671 is a novel cell-permeable inhibitor of S6K1. PF-4708671 specifically inhibits the S6K1 isoform with a Ki of 20 nM and IC50 of 160 nM. PF-4708671 prevents the S6K1-mediated phosphorylation of S6 protein in response to IGF-1 (insulin-like growth factor 1), while having no effect upon the PMA-induced phosphorylation of substrates of the highly related RSK (p90 ribosomal S6 kinase) and MSK (mitogen- and stress-activated kinase) kinases.


Price and Availability

Size
Price

5mg
USD 120
50mg
USD 450
500mg
USD 1650
5g
USD 5250
Size
Price

10mg
USD 150
100mg
USD 650
1g
USD 2650
10g
Ask price
Size
Price

25mg
USD 250
200mg
USD 950
2g
USD 3950

PF-4708671, purity > 98%, is in stock. The same day shipping out after order is received. Delivery time: overnight (USA/Canada); 3-5 days (worldwide). Shipping fee: $30.00 (USA); from $45.00 (Canada); from $70.00 (international). Lead time for order of > 200mg is about 2 weeks.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 406432
Name: PF-4708671
CAS#: 1255517-76-0
Chemical Formula: C19H21F3N6
Exact Mass: 390.17798
Molecular Weight: 390.40545
Elemental Analysis: C, 58.45; H, 5.42; F, 14.60; N, 21.53


Synonym: PF4708671; PF-4708671; PF 4708671.

IUPAC/Chemical Name: 2-((4-(5-ethylpyrimidin-4-yl)piperazin-1-yl)methyl)-5-(trifluoromethyl)-1H-benzo[d]imidazole

SMILES Code: FC(C1=CC=C2NC(CN3CCN(C4=NC=NC=C4CC)CC3)=NC2=C1)(F)F


Technical Data

Appearance:
solid powder

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

Certificate of Analysis:

Safety Data Sheet (MSDS):

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 to 50 mM in DMSO and to 50 mM in ethanol, not soluble in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in ethanol: PF-4708671 was dissolved in ethanol and subsequently diluted in soya bean oil. (see Biochem J. 2012 Jan 1;441(1):199-207.)

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

 S6K1 (p70 ribosomal S6 kinase 1) is activated by insulin and growth factors via the PI3K (phosphoinositide 3-kinase) and mTOR (mammalian target of rapamycin) signalling pathways. S6K1 regulates numerous processes, such as protein synthesis, growth, proliferation and longevity, and its inhibition has been proposed as a strategy for the treatment of cancer and insulin resistance. 
 
 
 


References

1: Leontieva OV, Demidenko ZN, Blagosklonny MV. S6K in geroconversion. Cell Cycle. 2013 Oct 15;12(20):3249-52. doi: 10.4161/cc.26248. Epub 2013 Sep 9. PubMed PMID: 24036549.

2: Allard EK, Grujic M, Fisone G, Kristensson K. Prion formation correlates with activation of translation-regulating protein 4E-BP and neuronal transcription factor Elk1. Neurobiol Dis. 2013 Oct;58:116-22. doi: 10.1016/j.nbd.2013.05.014. Epub 2013 Jun 3. PubMed PMID: 23742760.

3: Parker WE, Orlova KA, Parker WH, Birnbaum JF, Krymskaya VP, Goncharov DA, Baybis M, Helfferich J, Okochi K, Strauss KA, Crino PB. Rapamycin prevents seizures after depletion of STRADA in a rare neurodevelopmental disorder. Sci Transl Med. 2013 Apr 24;5(182):182ra53. doi: 10.1126/scitranslmed.3005271. PubMed PMID: 23616120; PubMed Central PMCID: PMC3720125.

4: Rajan MR, Fagerholm S, Jönsson C, Kjølhede P, Turkina MV, Strålfors P. Phosphorylation of IRS1 at serine 307 in response to insulin in human adipocytes is not likely to be catalyzed by p70 ribosomal S6 kinase. PLoS One. 2013;8(4):e59725. doi: 10.1371/journal.pone.0059725. Epub 2013 Apr 2. PubMed PMID: 23565163; PubMed Central PMCID: PMC3614923.

5: Choi HN, Jin HO, Kim JH, Hong SE, Kim HA, Kim EK, Lee JK, Park IC, Noh WC. Inhibition of S6K1 enhances glucose deprivation-induced cell death via downregulation of anti-apoptotic proteins in MCF-7 breast cancer cells. Biochem Biophys Res Commun. 2013 Mar 1;432(1):123-8. doi: 10.1016/j.bbrc.2013.01.074. Epub 2013 Jan 29. PubMed PMID: 23376066.

6: Di R, Wu X, Chang Z, Zhao X, Feng Q, Lu S, Luan Q, Hemmings BA, Li X, Yang Z. S6K inhibition renders cardiac protection against myocardial infarction through PDK1 phosphorylation of Akt. Biochem J. 2012 Jan 1;441(1):199-207. doi: 10.1042/BJ20110033. PubMed PMID: 21906027.

7: Rosner M, Schipany K, Hengstschläger M. p70 S6K1 nuclear localization depends on its mTOR-mediated phosphorylation at T389, but not on its kinase activity towards S6. Amino Acids. 2012 Jun;42(6):2251-6. doi: 10.1007/s00726-011-0965-4. Epub 2011 Jun 28. PubMed PMID: 21710263.

8: Bilanges B, Vanhaesebroeck B. A new tool to dissect the function of p70 S6 kinase. Biochem J. 2010 Oct 15;431(2):e1-3. doi: 10.1042/BJ20101445. PubMed PMID: 20874709.

9: Pearce LR, Alton GR, Richter DT, Kath JC, Lingardo L, Chapman J, Hwang C, Alessi DR. Characterization of PF-4708671, a novel and highly specific inhibitor of p70 ribosomal S6 kinase (S6K1). Biochem J. 2010 Oct 15;431(2):245-55. doi: 10.1042/BJ20101024. PubMed PMID: 20704563.