[CAS NO. 1255517-76-0] PF-4708671

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PRODUCTS SPECIFICATIONS [1255517-76-0]

Catalog

HY-15773

Brand

MCE

CAS

1255517-76-0

DESCRIPTION [1255517-76-0]

Overview

MDL	MFCD18086922
Molecular Weight	390.41
Molecular Formula	C19H21F3N6
SMILES	FC(C1=CC=C2N=C(CN3CCN(C4=NC=NC=C4CC)CC3)NC2=C1)(F)F

For research use only. We do not sell to patients.

14 Publications Citing Use of MCE

Summary

PF-4708671 is a potent cell-permeable S6K1 inhibitor with a K _i of 20 nM and IC ₅₀ of 160 nM.

In Vitro

PF-4708671 inhibits the activity of full-length S6K1 in vitro with a K _i of 20 nM, and S6K1 isolated from IGF1-stimulated HEK293 cells with an IC ₅₀ of 0.16 μM, and only inhibits very weakly the closely related S6K2 isoform (IC ₅₀ of 65 μM). PF-4708671 inhibits RSK1 (IC ₅₀ of 4.7 μM) and RSK2 (IC ₅₀ of 9.2 μM) over 20-fold less potently than S6K1. PF4708671 inhibits MSK1 (IC ₅₀ of 0.95 μM) 4-fold more weakly than S6K1 ^[1] . HCT116 cells are treated with (i) vehicle (DMSO), (ii) OSI-906 (5 μM), (iii) PF-4708671 (10 μM), and (iv) OSI-906 (5 μM)+PF-4708671 (10 μM) for various amounts of time. HCT116 cells treated with OSI-906 alone (closed square) or PF4708671 alone (open circle) slightly inhibit cell growth. In contrast, proliferation in HCT116 cells is significantly inhibited after a 2-day treatment with the combination of OSI-906 and PF-4708671 (closed circle). A similar result is also observed when SW480 cells are treated with the combination of OSI-906 and PF-4708671. Colony formation also significantly reduces in OSI-906+PF-4708671-treated cells comparing with vehicle, OSI-906 alone, or PF-4708671 alone treated HCT116 or SW480 cells ^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

The tumor growth rate in mice treated with the combination of OSI-906+PF-4708671 is significantly slower than that of OSI-906 alone (P=0.0189) or PF4708671 alone (P=0.0165) treated mice. The average tumor volume in the OSI-906+PF-4708671-treated mice is approximately 50% of that in mice treated with OSI-906 (P=0.0056) or PF-4708671 alone (P<0.001) at the end of a 15-day treatment ^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 33.33 mg/mL ( 85.37 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.5614 mL	12.8070 mL	25.6141 mL
5 mM	0.5123 mL	2.5614 mL	5.1228 mL
10 mM	0.2561 mL	1.2807 mL	2.5614 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (6.40 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (6.40 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (6.40 mM); Clear solution

* All of the co-solvents are available by MCE.