[CAS NO. 319492-82-5] GAKinhibitor49

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PRODUCTS SPECIFICATIONS [319492-82-5]

Catalog

HY-124793

Brand

MCE

CAS

319492-82-5

DESCRIPTION [319492-82-5]

Overview

MDL	MFCD29701419
Molecular Weight	370.40
Molecular Formula	C20H22N2O5
SMILES	COC1=C(OC)C(OC)=CC(NC2=CC=NC3=CC(OC)=C(OC)C=C23)=C1

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

Summary

GAK inhibitor 49 is a potent, ATP-competitive and highly selective cyclin G associated kinase (GAK) inhibitor with a K _i of 0.54 nM and a cell IC ₅₀ of 56 nM. GAK inhibitor 49 also shows binding to RIPK2 ^[1] .

In Vitro

GAK inhibitor 49 (compound 49) shows a weak inhibitory effect on AAK1, BMP2K and STK16, with IC ₅₀ s of 28, 63 and >100 μM, respectively ^[1] .

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 : 50 mg/mL ( 134.99 mM ; ultrasonic and warming and heat to 80°C)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.6998 mL	13.4989 mL	26.9978 mL
5 mM	0.5400 mL	2.6998 mL	5.3996 mL
10 mM	0.2700 mL	1.3499 mL	2.6998 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: ≥ 2.08 mg/mL (5.62 mM); Clear solution
2.

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

Solubility: 2.08 mg/mL (5.62 mM); Suspended solution; Need ultrasonic
3.

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

Solubility: ≥ 2.08 mg/mL (5.62 mM); Clear solution

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

References

[1] Asquith CRM, et al. Identification and Optimization of 4-Anilinoquinolines as Inhibitors of Cyclin G Associated Kinase. ChemMedChem. 2018;13(1):48-66.