PF-4708671

PF-4708671 is a cell-permeable inhibitor of p70 ribosomal S6 kinase (S6K1 isoform) with Ki/IC50 of 20 nM/160 nM in cell-free assays, 400-fold greater selectivity for S6K1 than S6K2, and 4- and >20-fold selectivity for S6K1 than MSK1 and RSK1/2, respectively. PF-4708671 induces autophagy. First S6K1-specific inhibitor to be reported.

PF-4708671 Chemical Structure

PF-4708671 Chemical Structure

CAS No. 1255517-76-0

Purity & Quality Control

PF-4708671 Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
BHT-101 Growth Inhibition Assay IC50=0.82024 μM
UACC-893 Growth Inhibition Assay IC50=5.19886 μM
A427 Growth Inhibition Assay IC50=5.72567 μM
OCUB-M Growth Inhibition Assay IC50=6.66102 μM
SW684 Growth Inhibition Assay IC50=7.52268 μM
SK-LMS-1 Growth Inhibition Assay IC50=9.01302 μM
CP50-MEL-B Growth Inhibition Assay IC50=9.30419 μM
NCI-H1651 Growth Inhibition Assay IC50=10.0276 μM
ABC-1 Growth Inhibition Assay IC50=10.1037 μM
OE19 Growth Inhibition Assay IC50=10.1733 μM
DSH1 Growth Inhibition Assay IC50=10.8879 μM
SW13 Growth Inhibition Assay IC50=11.9319 μM
MDA-MB-453 Growth Inhibition Assay IC50=12.1603 μM
647-V Growth Inhibition Assay IC50=12.3582 μM
NCI-H2342 Growth Inhibition Assay IC50=12.3995 μM
LB2241-RCC Growth Inhibition Assay IC50=12.5779 μM
UACC-257 Growth Inhibition Assay IC50=13.4453 μM
NCI-H661 Growth Inhibition Assay IC50=13.6449 μM
FADU Growth Inhibition Assay IC50=13.6992 μM
A2780 Growth Inhibition Assay IC50=13.8041 μM
NCI-H1793 Growth Inhibition Assay IC50=14.4085 μM
TE-8 Growth Inhibition Assay IC50=15.3465 μM
HGC-27 Growth Inhibition Assay IC50=16.1644 μM
MMAC-SF Growth Inhibition Assay IC50=17.3727 μM
Calu-6 Growth Inhibition Assay IC50=18.1513 μM
HUTU-80 Growth Inhibition Assay IC50=18.3959 μM
SAS Growth Inhibition Assay IC50=18.6455 μM
IST-MES1 Growth Inhibition Assay IC50=18.6508 μM
C3A Growth Inhibition Assay IC50=18.7919 μM
ES3 Growth Inhibition Assay IC50=18.8364 μM
HSC-2 Growth Inhibition Assay IC50=19.6541 μM
T47D Growth Inhibition Assay IC50=20.1485 μM
EW-7 Growth Inhibition Assay IC50=20.8588 μM
LN-405 Growth Inhibition Assay IC50=20.8965 μM
U031 Growth Inhibition Assay IC50=21.4802 μM
A549 Growth Inhibition Assay IC50=21.8491 μM
RMG-I Growth Inhibition Assay IC50=22.2668 μM
BT-474 Growth Inhibition Assay IC50=22.6551 μM
NB69 Growth Inhibition Assay IC50=23.152 μM
NB7 Growth Inhibition Assay IC50=24.188 μM
HCC1569 Growth Inhibition Assay IC50=24.6125 μM
MEL-JUSO Growth Inhibition Assay IC50=24.6908 μM
MDA-MB-175-VII Growth Inhibition Assay IC50=25.2517 μM
HCC1419 Growth Inhibition Assay IC50=25.6003 μM
Ca9-22 Growth Inhibition Assay IC50=25.6432 μM
KGN Growth Inhibition Assay IC50=25.7547 μM
LB373-MEL-D Growth Inhibition Assay IC50=26.1938 μM
NCI-H1755 Growth Inhibition Assay IC50=26.8841 μM
D-423MG Growth Inhibition Assay IC50=27.0715 μM
DK-MG Growth Inhibition Assay IC50=28.7846 μM
NCI-H1623 Growth Inhibition Assay IC50=28.8342 μM
KU-19-19 Growth Inhibition Assay IC50=28.995 μM
C-33-A Growth Inhibition Assay IC50=29.2198 μM
SCC-4 Growth Inhibition Assay IC50=30.3354 μM
MG-63 Growth Inhibition Assay IC50=30.5994 μM
LNCaP-Clone-FGC Growth Inhibition Assay IC50=31.4921 μM
CAPAN-1 Growth Inhibition Assay IC50=31.5286 μM
GI-ME-N Growth Inhibition Assay IC50=31.5353 μM
RERF-LC-MS Growth Inhibition Assay IC50=32.6747 μM
KLE Growth Inhibition Assay IC50=33.4334 μM
KNS-81-FD Growth Inhibition Assay IC50=33.5008 μM
DOK Growth Inhibition Assay IC50=34.6612 μM
ACHN Growth Inhibition Assay IC50=35.1588 μM
KYSE-520 Growth Inhibition Assay IC50=35.2361 μM
SBC-5 Growth Inhibition Assay IC50=35.5116 μM
NCI-H28 Growth Inhibition Assay IC50=35.6695 μM
ES7 Growth Inhibition Assay IC50=36.2249 μM
A172 Growth Inhibition Assay IC50=36.4187 μM
UM-UC-3 Growth Inhibition Assay IC50=37.8746 μM
LXF-289 Growth Inhibition Assay IC50=38.0047 μM
KP-4 Growth Inhibition Assay IC50=38.4739 μM
TE-1 Growth Inhibition Assay IC50=39.6589 μM
G-402 Growth Inhibition Assay IC50=40.061 μM
786-0 Growth Inhibition Assay IC50=40.9096 μM
K5 Growth Inhibition Assay IC50=41.3686 μM
SK-N-DZ Growth Inhibition Assay IC50=41.3823 μM
OVCAR-4 Growth Inhibition Assay IC50=41.7568 μM
T84 Growth Inhibition Assay IC50=42.1263 μM
GCIY Growth Inhibition Assay IC50=43.0803 μM
BB49-HNC Growth Inhibition Assay IC50=43.3348 μM
SNU-C2B Growth Inhibition Assay IC50=43.6436 μM
TE-6 Growth Inhibition Assay IC50=43.8894 μM
23132-87 Growth Inhibition Assay IC50=44.2978 μM
DMS-53 Growth Inhibition Assay IC50=44.3384 μM
ONS-76 Growth Inhibition Assay IC50=44.7661 μM
DMS-273 Growth Inhibition Assay IC50=44.943 μM
COLO-824 Growth Inhibition Assay IC50=45.8775 μM
DMS-114 Growth Inhibition Assay IC50=45.8927 μM
YKG-1 Growth Inhibition Assay IC50=46.0355 μM
RH-18 Growth Inhibition Assay IC50=46.3733 μM
NCI-H1355 Growth Inhibition Assay IC50=46.618 μM
NCI-H2170 Growth Inhibition Assay IC50=47.7584 μM
OC-314 Growth Inhibition Assay IC50=47.8478 μM
NCI-H2030 Growth Inhibition Assay IC50=47.8906 μM
22RV1 Growth Inhibition Assay IC50=47.9015 μM
G-401 Growth Inhibition Assay IC50=48.4415 μM
YAPC Growth Inhibition Assay IC50=49.8073 μM
SW1573 Growth Inhibition Assay IC50=50.2435 μM
COLO-792 Growth Inhibition Assay IC50=50.6237 μM
KNS-62 Growth Inhibition Assay IC50=50.7508 μM
NB5 Growth Inhibition Assay IC50=51.4509 μM
CP66-MEL Growth Inhibition Assay IC50=51.6408 μM
CaR-1 Growth Inhibition Assay IC50=52.0606 μM
CAL-54 Growth Inhibition Assay IC50=52.1102 μM
8305C Growth Inhibition Assay IC50=52.315 μM
Calu-3 Growth Inhibition Assay IC50=52.3733 μM
AU565 Growth Inhibition Assay IC50=52.5509 μM
CW-2 Growth Inhibition Assay IC50=52.8654 μM
BEN Growth Inhibition Assay IC50=53.7862 μM
NCI-H1975 Growth Inhibition Assay IC50=53.8966 μM
HCT-116 Growth Inhibition Assay IC50=54.0327 μM
SH-4 Growth Inhibition Assay IC50=54.138 μM
NCI-H1693 Growth Inhibition Assay IC50=54.2103 μM
BPH-1 Growth Inhibition Assay IC50=55.2892 μM
CAMA-1 Growth Inhibition Assay IC50=55.8116 μM
A388 Growth Inhibition Assay IC50=56.0985 μM
C2BBe1 Growth Inhibition Assay IC50=56.2634 μM
GAMG Growth Inhibition Assay IC50=56.5955 μM
MKN28 Growth Inhibition Assay IC50=56.8013 μM
VA-ES-BJ Growth Inhibition Assay IC50=56.8745 μM
HuCCT1 Growth Inhibition Assay IC50=57.0492 μM
BFTC-905 Growth Inhibition Assay IC50=57.2898 μM
LS-123 Growth Inhibition Assay IC50=57.5668 μM
LB996-RCC Growth Inhibition Assay IC50=58.0287 μM
NCI-H1048 Growth Inhibition Assay IC50=58.2188 μM
COR-L105 Growth Inhibition Assay IC50=58.7337 μM
OVCAR-8 Growth Inhibition Assay IC50=59.1716 μM
SK-N-FI Growth Inhibition Assay IC50=59.3207 μM
MES-SA Growth Inhibition Assay IC50=59.4509 μM
SCC-9 Growth Inhibition Assay IC50=59.4753 μM
EFO-27 Growth Inhibition Assay IC50=59.943 μM
GT3TKB Growth Inhibition Assay IC50=60.6048 μM
HCC38 Growth Inhibition Assay IC50=61.4379 μM
MLMA Growth Inhibition Assay IC50=61.6163 μM
D-566MG Growth Inhibition Assay IC50=63.5224 μM
SF295 Growth Inhibition Assay IC50=63.6655 μM
ES4 Growth Inhibition Assay IC50=64.4719 μM
CAKI-1 Growth Inhibition Assay IC50=64.5721 μM
OAW-28 Growth Inhibition Assay IC50=64.9647 μM
NCI-H460 Growth Inhibition Assay IC50=65.0897 μM
JAR Growth Inhibition Assay IC50=65.5516 μM
SNU-449 Growth Inhibition Assay IC50=65.7616 μM
D-392MG Growth Inhibition Assay IC50=65.9434 μM
EW-22 Growth Inhibition Assay IC50=66.395 μM
GCT Growth Inhibition Assay IC50=67.0443 μM
NOS-1 Growth Inhibition Assay IC50=67.6867 μM
RH-1 Growth Inhibition Assay IC50=68.5559 μM
HuH-7 Growth Inhibition Assay IC50=69.1002 μM
NUGC-3 Growth Inhibition Assay IC50=70.9644 μM
IST-SL1 Growth Inhibition Assay IC50=71.2324 μM
SHP-77 Growth Inhibition Assay IC50=72.119 μM
SW1116 Growth Inhibition Assay IC50=72.1407 μM
LK-2 Growth Inhibition Assay IC50=72.8612 μM
U-2-OS Growth Inhibition Assay IC50=73.1828 μM
KYSE-150 Growth Inhibition Assay IC50=73.6118 μM
U251 Growth Inhibition Assay IC50=73.8168 μM
HT-1080 Growth Inhibition Assay IC50=74.2574 μM
NCI-H1437 Growth Inhibition Assay IC50=74.6326 μM
HPAF-II Growth Inhibition Assay IC50=74.6415 μM
Becker Growth Inhibition Assay IC50=75.1105 μM
PANC-10-05 Growth Inhibition Assay IC50=75.2865 μM
TYK-nu Growth Inhibition Assay IC50=75.3102 μM
SKG-IIIa Growth Inhibition Assay IC50=75.3341 μM
NCI-H1993 Growth Inhibition Assay IC50=75.7397 μM
S-117 Growth Inhibition Assay IC50=75.755 μM
HuO9 Growth Inhibition Assay IC50=76.0048 μM
CAL-51 Growth Inhibition Assay IC50=76.1006 μM
BT-20 Growth Inhibition Assay IC50=76.2168 μM
LB831-BLC Growth Inhibition Assay IC50=76.3217 μM
LB1047-RCC Growth Inhibition Assay IC50=76.7619 μM
ES8 Growth Inhibition Assay IC50=78.0073 μM
UMC-11 Growth Inhibition Assay IC50=78.0884 μM
NCI-H226 Growth Inhibition Assay IC50=78.1315 μM
IGROV-1 Growth Inhibition Assay IC50=78.555 μM
BHY Growth Inhibition Assay IC50=79.596 μM
MKN45 Growth Inhibition Assay IC50=80.3174 μM
IA-LM Growth Inhibition Assay IC50=80.3511 μM
WM-115 Growth Inhibition Assay IC50=81.4114 μM
VMRC-RCZ Growth Inhibition Assay IC50=81.4425 μM
NCI-H2291 Growth Inhibition Assay IC50=81.6842 μM
MCF7 Growth Inhibition Assay IC50=83.2897 μM
639-V Growth Inhibition Assay IC50=84.6129 μM
RT4 Growth Inhibition Assay IC50=85.2403 μM
NCI-H2405 Growth Inhibition Assay IC50=85.2997 μM
CAL-33 Growth Inhibition Assay IC50=85.6315 μM
BT-549 Growth Inhibition Assay IC50=85.9382 μM
HT-1197 Growth Inhibition Assay IC50=88.1077 μM
G-361 Growth Inhibition Assay IC50=88.1474 μM
LS-411N Growth Inhibition Assay IC50=89.3388 μM
HT-144 Growth Inhibition Assay IC50=89.5992 μM
DJM-1 Growth Inhibition Assay IC50=89.8845 μM
CAL-12T Growth Inhibition Assay IC50=90.7895 μM
MKN7 Growth Inhibition Assay IC50=91.3551 μM
HuP-T3 Growth Inhibition Assay IC50=96.1004 μM
SK-MG-1 Growth Inhibition Assay IC50=96.1348 μM
NCI-H2347 Growth Inhibition Assay IC50=98.1042 μM
SW872 Growth Inhibition Assay IC50=100.456 μM
COLO-829 Growth Inhibition Assay IC50=100.553 μM
MC-IXC Growth Inhibition Assay IC50=100.615 μM
Click to View More Cell Line Experimental Data

Biological Activity

Description PF-4708671 is a cell-permeable inhibitor of p70 ribosomal S6 kinase (S6K1 isoform) with Ki/IC50 of 20 nM/160 nM in cell-free assays, 400-fold greater selectivity for S6K1 than S6K2, and 4- and >20-fold selectivity for S6K1 than MSK1 and RSK1/2, respectively. PF-4708671 induces autophagy. First S6K1-specific inhibitor to be reported.
Targets
p70 S6K1 [1]
(Cell-free assay)
160 nM
In vitro
In vitro PF-4708671 is a piperazinyl-pyrimidine analogue and the first S6K1-specific inhibitor. PF-4708671 does not significantly inhibit the activity of the closely related S6K2 isoform or a number of other AGC kinases (Akt1, Akt2, PKA, PKCα, PKCϵ, PRK2, ROCK2, RSK1, RSK2 or SGK1) . 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. PF-4708671 is 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 does not affect activity of mTORC1. [1]
Experimental Result Images Methods Biomarkers Images PMID
Western blot pS6 / S6 / pS6K / S6K1 / pAKT / AKT p-mTOR / mTOR / p-p70S6K / p70S6K S2163-WB1 28626016
Growth inhibition assay Cell viability S2163-viability1 30423811
  • https://pubmed.ncbi.nlm.nih.gov/20704563/

Chemical Information & Solubility

Molecular Weight 390.41 Formula

C19H21F3N6

CAS No. 1255517-76-0 SDF Download PF-4708671 SDF
Smiles CCC1=CN=CN=C1N2CCN(CC2)CC3=NC4=C(N3)C=C(C=C4)C(F)(F)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 30 mg/mL ( (76.84 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 8 mg/mL

Water : Insoluble


Molecular Weight Calculator

In vivo
Batch:

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In vivo Formulation Calculator

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Molarity Calculator

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

Question 1:
Whether the in vivo formula "30% PEG400+0.5% Tween80+5% Propylene glycol" for S2163 is suitable for i.p. or not?

Answer:
The formula "30% PEG400+0.5% Tween80+5% Propylene glycol" on our website is an oral one. It is a suspension.

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