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Gusacitinib (ASN-002) Syk inhibitor

Name: Gusacitinib (ASN-002)
Brand: Selleck Chemicals
SKU: S0871
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S0871

Gusacitinib (ASN-002) is a novel and potent dual inhibitor of spleen tyrosine kinase (SYK) and Janus kinases (JAK) with IC50 values of 5-46 nM in biochemical assays.

Chemical Structure

Molecular Weight: 460.53

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Quality Control

Batch: Purity: 99.81%

99.81

Related Targets	EGFR VEGFR JAK PDGFR FGFR Src HIF FLT FLT3 HER2
Other Syk Inhibitors	R406 R406 (free base) PRT062607 (P505-15) HCl Entospletinib (GS-9973) Piceatannol BAY 61-3606 dihydrochloride PRT-060318 2HCl TAK-659 Hydrochloride Lanraplenib (GS-SYK) RO9021

Solubility

In vitro
Batch:

DMSO : 92 mg/mL (199.76 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.150mg/ml (2.50mM)	Taking the 1 mL working solution as an example, add 50 μL 23 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

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.

Chemical Information, Storage & Stability

Molecular Weight	460.53	Formula	C₂₄H₂₈N₈O₂	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1425381-60-7	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1CN(CCC1CC#N)C2=NC3=C(C(=O)NN=C3)C(=N2)NC4=CC=C(C=C4)N5CCC(CC5)O

Mechanism of Action

Targets/IC₅₀/Ki	SYK JAK
References	[1] https://cancerres.aacrjournals.org/content/75/15_Supplement/792

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT06238531	Not yet recruiting	Systemic Lupus Erythematosus	National Institute of Arthritis and Musculoskeletal and Skin Diseases (NIAMS)\|National Institutes of Health Clinical Center (CC)	May 15 2024	Phase 1
NCT04416516	Completed	Basal Cell Carcinoma\|Basal Cell Nevus Syndrome	Ascend Biopharmaceuticals Ltd	July 16 2020	Phase 2
NCT03641573	Completed	Healthy Volunteer	Asana BioSciences	October 11 2018	Phase 1
NCT03208296	Suspended	Basal Cell Carcinoma in Basal Cell Nevus Syndrome	Ascend Biopharmaceuticals Ltd	December 1 2017	Phase 1\|Phase 2
NCT03139981	Completed	Dermatitis Atopic\|Dermatitis Eczema\|Dermatitis Eczematous	Asana BioSciences	April 12 2017	Phase 1
NCT02853643	Completed	Healthy Volunteers	Asana BioSciences	July 2016	Phase 1

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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