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Gusacitinib

Name: Gusacitinib
Brand: TargetMol
SKU: T14331
Price: 35 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T14331Cas No. 1425381-60-7

Alias ASN-002

Gusacitinib (ASN-002) (ASN-002) is spleen tyrosine kinase (SYK) and janus kinase (JAK) inhibitor (IC50: 5-46 nM).

Gusacitinib

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Purity: 99.94%

Catalog No. T14331Alias ASN-002Cas No. 1425381-60-7

Gusacitinib (ASN-002) (ASN-002) is spleen tyrosine kinase (SYK) and janus kinase (JAK) inhibitor (IC50: 5-46 nM).

Pack Size	Price	Availability
1 mg	$35	In Stock
5 mg	$81	In Stock
10 mg	$125	In Stock
25 mg	$198	In Stock
50 mg	$369	In Stock
100 mg	$549	In Stock
200 mg	$789	In Stock
1 mL x 10 mM (in DMSO)	$118	In Stock

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Batch Information

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Purity:99.94%

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COA HNMR LCMS

Product Introduction

Bioactivity

Description	Gusacitinib (ASN-002) (ASN-002) is spleen tyrosine kinase (SYK) and janus kinase (JAK) inhibitor (IC50: 5-46 nM).
Targets&IC50	Syk/JAK:5-46 nM
In vitro	Gusacitinib (ASN-002) shows anti-proliferative activity in a broad panel of human cancer cell lines including DHL6, DHL4, OCI-LY10, H929, Pfeiffer, HT-1376, and Lovo, suggesting activity in both solid and hematological tumor types[1]. In mechanistic cell-based studies involving IgE and cytokine stimulations, Gusacitinib (ASN-002) strongly suppresses the SYK and JAK family kinase signaling pathways measured as pLAT and pSTAT levels, respectively.
In vivo	Gusacitinib (ASN-002) shows a favorable safety profile in rat and dog toxicology studies[1]. Gusacitinib (ASN-002) has good oral bioavailability, metabolic stability, is not a Pgp substrate, and shows little to no inhibition of CYP450 isozymes. In a multiple myeloma (H929) xenograft model, Gusacitinib (ASN-002) exhibits significant efficacy in inhibiting tumor growth (>95%) and it also significantly delays the onset of hind limb paralysis in the human erythroleukemia (HEL) mouse model.
Synonyms	ASN-002

Chemical Properties

Molecular Weight	460.53
Formula	C₂₄H₂₈N₈O₂
Cas No.	1425381-60-7
Smiles	OC1CCN(CC1)c1ccc(Nc2nc(nc3cn[nH]c(=O)c23)N2CCC(CC#N)CC2)cc1
Relative Density.	1.47 g/cm3 (Predicted)

Storage & Solubility Information

Storage

store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 95 mg/mL (206.28 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.1714 mL	10.8571 mL	21.7141 mL	108.5706 mL
5 mM	0.4343 mL	2.1714 mL	4.3428 mL	21.7141 mL
10 mM	0.2171 mL	1.0857 mL	2.1714 mL	10.8571 mL
20 mM	0.1086 mL	0.5429 mL	1.0857 mL	5.4285 mL
50 mM	0.0434 mL	0.2171 mL	0.4343 mL	2.1714 mL
100 mM	0.0217 mL	0.1086 mL	0.2171 mL	1.0857 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH₂O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH₂O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc