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 SANGER
UACC-893 Growth Inhibition Assay IC50=5.19886 μM SANGER
A427 Growth Inhibition Assay IC50=5.72567 μM SANGER
OCUB-M Growth Inhibition Assay IC50=6.66102 μM SANGER
SW684 Growth Inhibition Assay IC50=7.52268 μM SANGER
SK-LMS-1 Growth Inhibition Assay IC50=9.01302 μM SANGER
CP50-MEL-B Growth Inhibition Assay IC50=9.30419 μM SANGER
NCI-H1651 Growth Inhibition Assay IC50=10.0276 μM SANGER
ABC-1 Growth Inhibition Assay IC50=10.1037 μM SANGER
OE19 Growth Inhibition Assay IC50=10.1733 μM SANGER
DSH1 Growth Inhibition Assay IC50=10.8879 μM SANGER
SW13 Growth Inhibition Assay IC50=11.9319 μM SANGER
MDA-MB-453 Growth Inhibition Assay IC50=12.1603 μM SANGER
647-V Growth Inhibition Assay IC50=12.3582 μM SANGER
NCI-H2342 Growth Inhibition Assay IC50=12.3995 μM SANGER
LB2241-RCC Growth Inhibition Assay IC50=12.5779 μM SANGER
UACC-257 Growth Inhibition Assay IC50=13.4453 μM SANGER
NCI-H661 Growth Inhibition Assay IC50=13.6449 μM SANGER
FADU Growth Inhibition Assay IC50=13.6992 μM SANGER
A2780 Growth Inhibition Assay IC50=13.8041 μM SANGER
NCI-H1793 Growth Inhibition Assay IC50=14.4085 μM SANGER
TE-8 Growth Inhibition Assay IC50=15.3465 μM SANGER
HGC-27 Growth Inhibition Assay IC50=16.1644 μM SANGER
MMAC-SF Growth Inhibition Assay IC50=17.3727 μM SANGER
Calu-6 Growth Inhibition Assay IC50=18.1513 μM SANGER
HUTU-80 Growth Inhibition Assay IC50=18.3959 μM SANGER
SAS Growth Inhibition Assay IC50=18.6455 μM SANGER
IST-MES1 Growth Inhibition Assay IC50=18.6508 μM SANGER
C3A Growth Inhibition Assay IC50=18.7919 μM SANGER
ES3 Growth Inhibition Assay IC50=18.8364 μM SANGER
HSC-2 Growth Inhibition Assay IC50=19.6541 μM SANGER
T47D Growth Inhibition Assay IC50=20.1485 μM SANGER
EW-7 Growth Inhibition Assay IC50=20.8588 μM SANGER
LN-405 Growth Inhibition Assay IC50=20.8965 μM SANGER
U031 Growth Inhibition Assay IC50=21.4802 μM SANGER
A549 Growth Inhibition Assay IC50=21.8491 μM SANGER
RMG-I Growth Inhibition Assay IC50=22.2668 μM SANGER
BT-474 Growth Inhibition Assay IC50=22.6551 μM SANGER
NB69 Growth Inhibition Assay IC50=23.152 μM SANGER
NB7 Growth Inhibition Assay IC50=24.188 μM SANGER
HCC1569 Growth Inhibition Assay IC50=24.6125 μM SANGER
MEL-JUSO Growth Inhibition Assay IC50=24.6908 μM SANGER
MDA-MB-175-VII Growth Inhibition Assay IC50=25.2517 μM SANGER
HCC1419 Growth Inhibition Assay IC50=25.6003 μM SANGER
Ca9-22 Growth Inhibition Assay IC50=25.6432 μM SANGER
KGN Growth Inhibition Assay IC50=25.7547 μM SANGER
LB373-MEL-D Growth Inhibition Assay IC50=26.1938 μM SANGER
NCI-H1755 Growth Inhibition Assay IC50=26.8841 μM SANGER
D-423MG Growth Inhibition Assay IC50=27.0715 μM SANGER
DK-MG Growth Inhibition Assay IC50=28.7846 μM SANGER
NCI-H1623 Growth Inhibition Assay IC50=28.8342 μM SANGER
KU-19-19 Growth Inhibition Assay IC50=28.995 μM SANGER
C-33-A Growth Inhibition Assay IC50=29.2198 μM SANGER
SCC-4 Growth Inhibition Assay IC50=30.3354 μM SANGER
MG-63 Growth Inhibition Assay IC50=30.5994 μM SANGER
LNCaP-Clone-FGC Growth Inhibition Assay IC50=31.4921 μM SANGER
CAPAN-1 Growth Inhibition Assay IC50=31.5286 μM SANGER
GI-ME-N Growth Inhibition Assay IC50=31.5353 μM SANGER
RERF-LC-MS Growth Inhibition Assay IC50=32.6747 μM SANGER
KLE Growth Inhibition Assay IC50=33.4334 μM SANGER
KNS-81-FD Growth Inhibition Assay IC50=33.5008 μM SANGER
DOK Growth Inhibition Assay IC50=34.6612 μM SANGER
ACHN Growth Inhibition Assay IC50=35.1588 μM SANGER
KYSE-520 Growth Inhibition Assay IC50=35.2361 μM SANGER
SBC-5 Growth Inhibition Assay IC50=35.5116 μM SANGER
NCI-H28 Growth Inhibition Assay IC50=35.6695 μM SANGER
ES7 Growth Inhibition Assay IC50=36.2249 μM SANGER
A172 Growth Inhibition Assay IC50=36.4187 μM SANGER
UM-UC-3 Growth Inhibition Assay IC50=37.8746 μM SANGER
LXF-289 Growth Inhibition Assay IC50=38.0047 μM SANGER
KP-4 Growth Inhibition Assay IC50=38.4739 μM SANGER
TE-1 Growth Inhibition Assay IC50=39.6589 μM SANGER
G-402 Growth Inhibition Assay IC50=40.061 μM SANGER
786-0 Growth Inhibition Assay IC50=40.9096 μM SANGER
K5 Growth Inhibition Assay IC50=41.3686 μM SANGER
SK-N-DZ Growth Inhibition Assay IC50=41.3823 μM SANGER
OVCAR-4 Growth Inhibition Assay IC50=41.7568 μM SANGER
T84 Growth Inhibition Assay IC50=42.1263 μM SANGER
GCIY Growth Inhibition Assay IC50=43.0803 μM SANGER
BB49-HNC Growth Inhibition Assay IC50=43.3348 μM SANGER
SNU-C2B Growth Inhibition Assay IC50=43.6436 μM SANGER
TE-6 Growth Inhibition Assay IC50=43.8894 μM SANGER
23132-87 Growth Inhibition Assay IC50=44.2978 μM SANGER
DMS-53 Growth Inhibition Assay IC50=44.3384 μM SANGER
ONS-76 Growth Inhibition Assay IC50=44.7661 μM SANGER
DMS-273 Growth Inhibition Assay IC50=44.943 μM SANGER
COLO-824 Growth Inhibition Assay IC50=45.8775 μM SANGER
DMS-114 Growth Inhibition Assay IC50=45.8927 μM SANGER
YKG-1 Growth Inhibition Assay IC50=46.0355 μM SANGER
RH-18 Growth Inhibition Assay IC50=46.3733 μM SANGER
NCI-H1355 Growth Inhibition Assay IC50=46.618 μM SANGER
NCI-H2170 Growth Inhibition Assay IC50=47.7584 μM SANGER
OC-314 Growth Inhibition Assay IC50=47.8478 μM SANGER
NCI-H2030 Growth Inhibition Assay IC50=47.8906 μM SANGER
22RV1 Growth Inhibition Assay IC50=47.9015 μM SANGER
G-401 Growth Inhibition Assay IC50=48.4415 μM SANGER
YAPC Growth Inhibition Assay IC50=49.8073 μM SANGER
SW1573 Growth Inhibition Assay IC50=50.2435 μM SANGER
COLO-792 Growth Inhibition Assay IC50=50.6237 μM SANGER
KNS-62 Growth Inhibition Assay IC50=50.7508 μM SANGER
NB5 Growth Inhibition Assay IC50=51.4509 μM SANGER
CP66-MEL Growth Inhibition Assay IC50=51.6408 μM SANGER
CaR-1 Growth Inhibition Assay IC50=52.0606 μM SANGER
CAL-54 Growth Inhibition Assay IC50=52.1102 μM SANGER
8305C Growth Inhibition Assay IC50=52.315 μM SANGER
Calu-3 Growth Inhibition Assay IC50=52.3733 μM SANGER
AU565 Growth Inhibition Assay IC50=52.5509 μM SANGER
CW-2 Growth Inhibition Assay IC50=52.8654 μM SANGER
BEN Growth Inhibition Assay IC50=53.7862 μM SANGER
NCI-H1975 Growth Inhibition Assay IC50=53.8966 μM SANGER
HCT-116 Growth Inhibition Assay IC50=54.0327 μM SANGER
SH-4 Growth Inhibition Assay IC50=54.138 μM SANGER
NCI-H1693 Growth Inhibition Assay IC50=54.2103 μM SANGER
BPH-1 Growth Inhibition Assay IC50=55.2892 μM SANGER
CAMA-1 Growth Inhibition Assay IC50=55.8116 μM SANGER
A388 Growth Inhibition Assay IC50=56.0985 μM SANGER
C2BBe1 Growth Inhibition Assay IC50=56.2634 μM SANGER
GAMG Growth Inhibition Assay IC50=56.5955 μM SANGER
MKN28 Growth Inhibition Assay IC50=56.8013 μM SANGER
VA-ES-BJ Growth Inhibition Assay IC50=56.8745 μM SANGER
HuCCT1 Growth Inhibition Assay IC50=57.0492 μM SANGER
BFTC-905 Growth Inhibition Assay IC50=57.2898 μM SANGER
LS-123 Growth Inhibition Assay IC50=57.5668 μM SANGER
LB996-RCC Growth Inhibition Assay IC50=58.0287 μM SANGER
NCI-H1048 Growth Inhibition Assay IC50=58.2188 μM SANGER
COR-L105 Growth Inhibition Assay IC50=58.7337 μM SANGER
OVCAR-8 Growth Inhibition Assay IC50=59.1716 μM SANGER
SK-N-FI Growth Inhibition Assay IC50=59.3207 μM SANGER
MES-SA Growth Inhibition Assay IC50=59.4509 μM SANGER
SCC-9 Growth Inhibition Assay IC50=59.4753 μM SANGER
EFO-27 Growth Inhibition Assay IC50=59.943 μM SANGER
GT3TKB Growth Inhibition Assay IC50=60.6048 μM SANGER
HCC38 Growth Inhibition Assay IC50=61.4379 μM SANGER
MLMA Growth Inhibition Assay IC50=61.6163 μM SANGER
D-566MG Growth Inhibition Assay IC50=63.5224 μM SANGER
SF295 Growth Inhibition Assay IC50=63.6655 μM SANGER
ES4 Growth Inhibition Assay IC50=64.4719 μM SANGER
CAKI-1 Growth Inhibition Assay IC50=64.5721 μM SANGER
OAW-28 Growth Inhibition Assay IC50=64.9647 μM SANGER
NCI-H460 Growth Inhibition Assay IC50=65.0897 μM SANGER
JAR Growth Inhibition Assay IC50=65.5516 μM SANGER
SNU-449 Growth Inhibition Assay IC50=65.7616 μM SANGER
D-392MG Growth Inhibition Assay IC50=65.9434 μM SANGER
EW-22 Growth Inhibition Assay IC50=66.395 μM SANGER
GCT Growth Inhibition Assay IC50=67.0443 μM SANGER
NOS-1 Growth Inhibition Assay IC50=67.6867 μM SANGER
RH-1 Growth Inhibition Assay IC50=68.5559 μM SANGER
HuH-7 Growth Inhibition Assay IC50=69.1002 μM SANGER
NUGC-3 Growth Inhibition Assay IC50=70.9644 μM SANGER
IST-SL1 Growth Inhibition Assay IC50=71.2324 μM SANGER
SHP-77 Growth Inhibition Assay IC50=72.119 μM SANGER
SW1116 Growth Inhibition Assay IC50=72.1407 μM SANGER
LK-2 Growth Inhibition Assay IC50=72.8612 μM SANGER
U-2-OS Growth Inhibition Assay IC50=73.1828 μM SANGER
KYSE-150 Growth Inhibition Assay IC50=73.6118 μM SANGER
U251 Growth Inhibition Assay IC50=73.8168 μM SANGER
HT-1080 Growth Inhibition Assay IC50=74.2574 μM SANGER
NCI-H1437 Growth Inhibition Assay IC50=74.6326 μM SANGER
HPAF-II Growth Inhibition Assay IC50=74.6415 μM SANGER
Becker Growth Inhibition Assay IC50=75.1105 μM SANGER
PANC-10-05 Growth Inhibition Assay IC50=75.2865 μM SANGER
TYK-nu Growth Inhibition Assay IC50=75.3102 μM SANGER
SKG-IIIa Growth Inhibition Assay IC50=75.3341 μM SANGER
NCI-H1993 Growth Inhibition Assay IC50=75.7397 μM SANGER
S-117 Growth Inhibition Assay IC50=75.755 μM SANGER
HuO9 Growth Inhibition Assay IC50=76.0048 μM SANGER
CAL-51 Growth Inhibition Assay IC50=76.1006 μM SANGER
BT-20 Growth Inhibition Assay IC50=76.2168 μM SANGER
LB831-BLC Growth Inhibition Assay IC50=76.3217 μM SANGER
LB1047-RCC Growth Inhibition Assay IC50=76.7619 μM SANGER
ES8 Growth Inhibition Assay IC50=78.0073 μM SANGER
UMC-11 Growth Inhibition Assay IC50=78.0884 μM SANGER
NCI-H226 Growth Inhibition Assay IC50=78.1315 μM SANGER
IGROV-1 Growth Inhibition Assay IC50=78.555 μM SANGER
BHY Growth Inhibition Assay IC50=79.596 μM SANGER
MKN45 Growth Inhibition Assay IC50=80.3174 μM SANGER
IA-LM Growth Inhibition Assay IC50=80.3511 μM SANGER
WM-115 Growth Inhibition Assay IC50=81.4114 μM SANGER
VMRC-RCZ Growth Inhibition Assay IC50=81.4425 μM SANGER
NCI-H2291 Growth Inhibition Assay IC50=81.6842 μM SANGER
MCF7 Growth Inhibition Assay IC50=83.2897 μM SANGER
639-V Growth Inhibition Assay IC50=84.6129 μM SANGER
RT4 Growth Inhibition Assay IC50=85.2403 μM SANGER
NCI-H2405 Growth Inhibition Assay IC50=85.2997 μM SANGER
CAL-33 Growth Inhibition Assay IC50=85.6315 μM SANGER
BT-549 Growth Inhibition Assay IC50=85.9382 μM SANGER
HT-1197 Growth Inhibition Assay IC50=88.1077 μM SANGER
G-361 Growth Inhibition Assay IC50=88.1474 μM SANGER
LS-411N Growth Inhibition Assay IC50=89.3388 μM SANGER
HT-144 Growth Inhibition Assay IC50=89.5992 μM SANGER
DJM-1 Growth Inhibition Assay IC50=89.8845 μM SANGER
CAL-12T Growth Inhibition Assay IC50=90.7895 μM SANGER
MKN7 Growth Inhibition Assay IC50=91.3551 μM SANGER
HuP-T3 Growth Inhibition Assay IC50=96.1004 μM SANGER
SK-MG-1 Growth Inhibition Assay IC50=96.1348 μM SANGER
NCI-H2347 Growth Inhibition Assay IC50=98.1042 μM SANGER
SW872 Growth Inhibition Assay IC50=100.456 μM SANGER
COLO-829 Growth Inhibition Assay IC50=100.553 μM SANGER
MC-IXC Growth Inhibition Assay IC50=100.615 μM SANGER
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 28626016
Growth inhibition assay Cell viability 30423811

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


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In vivo
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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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