[CAS NO. 1648863-90-4] G-5555

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PRODUCTS SPECIFICATIONS [1648863-90-4]

Catalog

HY-19635

Brand

MCE

CAS

1648863-90-4

DESCRIPTION [1648863-90-4]

Overview

MDL	-
Molecular Weight	492.96
Molecular Formula	C25H25ClN6O3
SMILES	ClC(C=C(C1=NC(C)=CC=C1)C=C2)=C2C3=CC4=CN=C(NC)N=C4N(C[C@@H]5OC[C@@H](N)CO5)C3=O

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

4 Publications Citing Use of MCE

Summary

G-5555 is a potent p21-activated kinase 1 ( PAK1 ) inhibitor with K _i s of 3.7 nM and 11 nM for PAK1 and PAK2 , respectively.

IC50 & Target

PAK1

3.7 nM (Ki)

PAK2

11 nM (Ki)

In Vitro

G-5555 is a potent PAK1 inhibitor with a K _i of 3.7 nM. G-5555 shows excellent kinase selectivity and inhibits only eight out of the 235 kinases tested other than PAK1 with inhibition >70%: PAK2, PAK3, KHS1, Lck, MST3, MST4, SIK2, and YSK1. The IC ₅₀ s of G-5555 against SIK2, PAK2, KHS1, MST4, YSK1, MST3 and Lck are 9, 11, 10, 20, 34, 43, 52 nM, respectively. In general, G-5555 demonstrates high selectivity for the group I PAKs. There is negligible activity for G-5555 against the hERG channel with IC ₅₀ more than 10 μM in a patch clamp assay ^[1] . G-5555 potently inhibits PAK2, with a K _i of 11 nM. In an array of 23 breast cancer cell lines, G-5555 has significantly greater growth inhibitory activity in cell lines that are PAK-amplified compared to non-amplified lines ^[2] .

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

In Vivo

G-5555 exhibits low blood clearance and an acceptable half-life. Good oral exposure (AUC = 30 μM•h) and high oral bioavailability (F = 80%) are achieved ^[1] . In an H292 non-small cell lunger cancer (NSCLC) xenograft study in mice, G-5555 inhibits phosphorylation of the PAK1/2 downstream substrate mitogen-activated protein kinase 1 (MEK1) S298 and, when administered at an oral dose of 25 mg/kg b.i.d., imparts 60% tumor growth inhibition in this model13 and a PAK1 amplified breast cancer xenograft model, MDAMB-175 ^[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

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 25 mg/mL ( 50.71 mM ; ultrasonic and warming and heat to 80°C)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.0286 mL	10.1428 mL	20.2856 mL
5 mM	0.4057 mL	2.0286 mL	4.0571 mL
10 mM	0.2029 mL	1.0143 mL	2.0286 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 (5.07 mM); Clear solution
2.

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

Solubility: ≥ 2.5 mg/mL (5.07 mM); Clear solution
3.

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

Solubility: ≥ 2.5 mg/mL (5.07 mM); Clear solution

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