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Gusacitinib

Cat. No. M10740
Gusacitinib Structure
Synonym:

ASN-002

Size Price Availability Quantity
25mg USD 245  USD245 In stock
50mg USD 445  USD445 In stock
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Quality Control & Documentation
Biological Activity

Gusacitinib (ASN-002) is a potent dual inhibitor of SYK kinase and JAK kinase,IC50 Values are 5-46 nM. Gusacitinib has anti-cancer activity in both solid and hematological tumors.

Chemical Information
Molecular Weight 460.53
Formula C24H28N8O2
CAS Number 1425381-60-7
Solubility (25°C) DMSO ≥ 60 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Michelle Le, et al. Front Med (Lausanne). Systematic Review on the Efficacy and Safety of Oral Janus Kinase Inhibitors for the Treatment of Atopic Dermatitis

[2] A M Cartron, et al. Clin Exp Dermatol. Janus kinase inhibitors for atopic dermatitis: a promising treatment modality

[3] Celina Dubin, et al. Ther Clin Risk Manag. Drugs for the Treatment of Chronic Hand Eczema: Successes and Key Challenges

[4] Krzysztof Szalus, et al. Microorganisms. JAK-STAT Inhibitors in Atopic Dermatitis from Pathogenesis to Clinical Trials Results

[5] Ana M Montilla, et al. Dermatol Ther (Heidelb). Scoping Review on the Use of Drugs Targeting JAK/STAT Pathway in Atopic Dermatitis, Vitiligo, and Alopecia Areata

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Keywords: Gusacitinib, ASN-002 supplier, JAK, inhibitors, activators

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