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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
5mg USD 45  USD45 In stock
10mg USD 65  USD65 In stock
25mg USD 125  USD125 In stock
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Quality Control & Documentation
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
Chemical Information
Molecular Weight 390.41
Formula C19H21F3N6
CAS Number 1255517-76-0
Solubility (25°C) DMSO 20 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Pearce LR, et al. Biochem J. Characterization of PF-4708671, a novel and highly specific inhibitor of p70 ribosomal S6 kinase (S6K1).

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


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