Home Metabolism Serine/threonin kinase inhibitor SGC-GAK-1 For research use only.

SGC-GAK-1

SGC-GAK-1 is a potent, selective, and cell-active inhibitor of cyclin G-associated kinase (GAK) with Ki value of 3.1 nM and >50-fold selectivity over nearest kinase.

SGC-GAK-1 Chemical Structure

SGC-GAK-1 Chemical Structure

CAS No. 2226517-76-4

Purity & Quality Control

Batch: S671001 DMSO]78 mg/mL]false]Ethanol]39 mg/mL]false]Water]Insoluble]false Purity: 99.96%
99.96

SGC-GAK-1 Related Products

Biological Activity

Description SGC-GAK-1 is a potent, selective, and cell-active inhibitor of cyclin G-associated kinase (GAK) with Ki value of 3.1 nM and >50-fold selectivity over nearest kinase.
Targets
GAK [1]
3.1 nM(Ki)
In vitro
In vitro

SGC-GAK-1 shows strong growth inhibition in LNCaP, VCaP, and 22Rv1 cells at 10 μM, but minimal effect in PC3 and DU145 cells. In dose response SGC-GAK-1 shows potent antiproliferative activity in LNCaP and 22Rv1 cells at a similar dose range that it engages GAK[1].

Chemical Information & Solubility

Molecular Weight 389.24 Formula

C18H17BrN2O3
CAS No. 2226517-76-4 SDF --
Smiles COC1=CC(=CC(=C1OC)OC)NC2=C3C=C(C=CC3=NC=C2)Br
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 78 mg/mL ( (200.39 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 39 mg/mL

Water : Insoluble


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In vivo
Batch:

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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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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.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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