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PF-4708671 S6 Kinase inhibitor

Name: PF-4708671
Brand: Selleck Chemicals
SKU: S2163
Availability: InStock
Rating: 5 (59 reviews)

Cat.No.S2163

PF-4708671 is a cell-permeable inhibitor of p70 ribosomal S6 kinase (S6K1 isoform) with K_i/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. This compound induces autophagy. It is the first S6K1-specific inhibitor to be reported.

Chemical Structure

Molecular Weight: 390.41

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Quality Control

Batch: Purity: 99.97%

99.97

Related Targets	PI3K Akt mTOR GSK-3 ATM/ATR DNA-PK AMPK PDPK1 PTEN PP2A
Other S6 Kinase Inhibitors	BI-D1870 LY2584702 LY2584702 Tosylate LJI308 LJH685 3'-Hydroxypterostilbene BRD7389 S6K-18 L-Norvaline Gingerenone A

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Activity Description
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

Solubility

In vitro
Batch:

DMSO : 30 mg/mL (76.84 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 8 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	30%PEG400 1 0.5%Tween80 2 5%propylene glycol Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	30.000mg/ml (76.84mM)	Taking the 1 mL working solution as an example, add 300 μL of 100 mg/ml clarified PEG400 stock solution to 5 μL of Tween80, mix evenly to clarify it; add 50 μL Propylene glycol to the above system, mix evenly to clarify it; then continue to add 645 μL ddH2O to adjust the volume. to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (12.81mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	390.41	Formula	C₁₉H₂₁F₃N₆	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1255517-76-0	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CCC1=CN=CN=C1N2CCN(CC2)CC3=NC4=C(N3)C=C(C=C4)C(F)(F)F

Mechanism of Action

Targets/IC₅₀/Ki	p70 S6K1 (Cell-free assay) 160 nM
In vitro	PF-4708671 is a piperazinyl-pyrimidine analogue and the first S6K1-specific inhibitor. This compound 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). It 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. This chemical 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). It does not affect activity of mTORC1.
References	[1] https://pubmed.ncbi.nlm.nih.gov/20704563/

Applications

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

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Frequently Asked Questions

Question 1:
Whether the in vivo formula "30% PEG400+0.5% Tween80+5% Propylene glycol" for it 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 for this compound. It is a suspension.

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C6=C5/X	C6:	LOG(C6):
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