[CAS NO. 2930378-91-7] GAKinhibitor49hydrochloride

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PRODUCTS SPECIFICATIONS [2930378-91-7]

Catelog

HY-124793A

Brand

MCE

CAS

2930378-91-7

DESCRIPTION [2930378-91-7]

Overview

MDL	-
Molecular Weight	406.86
Molecular Formula	C20H23ClN2O5
SMILES	COC1=C(OC)C(OC)=CC(NC2=CC=NC3=CC(OC)=C(OC)C=C23)=C1.[H]Cl

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

Summary

GAK inhibitor 49 hydrochloride 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 hydrochloride also shows binding to RIPK2 ^[1] .

In Vitro

GAK inhibitor 49 (compound 49) hydrochloride shows a weak inhibitory effect on AAK1, BMP2K and STK16, with IC ₅₀ s of 28, 63 and >100μM, 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

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 : 14.29 mg/mL ( 35.12 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.4578 mL	12.2892 mL	24.5785 mL
5 mM	0.4916 mL	2.4578 mL	4.9157 mL
10 mM	0.2458 mL	1.2289 mL	2.4578 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: ≥ 1.43 mg/mL (3.51 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.