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PF-4708671

Cat. No. M2271
PF-4708671 Structure
Synonym:

PF-04708671

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mg USD 80 In stock
50mg USD 310 In stock
100mg USD 580 In stock
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Quality Control
Biological Activity

PF-4708671 is a novel cell-permeable inhibitor of S6K1 (p70 ribosomal S6 kinase 1) which 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, 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. PF-4708671 was also found to induce phosphorylation of the T-loop and hydrophobic motif of S6K1, an effect that is dependent upon mTORC1 (mTOR complex 1). PF-4708671 displays no effect on the activity of RSK and MSK in vivo. PF-4708671 exhibits no significant inhibition of S6K2 or other AGC kinases (e.g. Akt, PKA and ROCK) in vitro. PF-4708671 is the first S6K1-specific inhibitor to be reported and will be a useful tool for delineating S6K1-specific roles downstream of mTOR.

Customer Product Validations & Biological Datas
Source Front Neurol (2018). Figure 2. PF-4708671
Method Cumulative analysis
Cell Lines Lesion mice
Concentrations 50 mg/kg in 5 mL/kg volume
Incubation Time 1 h
Results Cumulative analysis showed that the increase in immobility time produced by the 6-OHDA lesion was reverted by rapamycin, but not by PF-4708671
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 390.41
Formula C19H21F3N6
CAS Number 1255517-76-0
Purity >99%
Solubility DMSO 20 mg/mL
Storage at -20°C
References

Characterization of PF-4708671, a novel and highly specific inhibitor of p70 ribosomal S6 kinase (S6K1).
Pearce LR, et al. Biochem J. 2010 Oct 15;431(2):245-55. PMID: 20704563.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: PF-4708671, PF-04708671 supplier, S6 Kinase, inhibitors

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