1. Epigenetics
    Stem Cell/Wnt
    JAK/STAT Signaling
    Protein Tyrosine Kinase/RTK
  2. JAK
    Syk
  3. Gusacitinib

Gusacitinib (Synonyms: ASN-002)

Cat. No.: HY-103018 Purity: 99.41%
Handling Instructions

Gusacitinib (ASN-002) is a potent dual inhibitor of spleen tyrosine kinase (SYK) and janus kinase (JAK) with IC50 values of 5-46 nM.

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

Gusacitinib Chemical Structure

Gusacitinib Chemical Structure

CAS No. : 1425381-60-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 605 In-stock
Estimated Time of Arrival: December 31
5 mg USD 550 In-stock
Estimated Time of Arrival: December 31
10 mg USD 850 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2850 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Description

Gusacitinib (ASN-002) is a potent dual inhibitor of spleen tyrosine kinase (SYK) and janus kinase (JAK) with IC50 values of 5-46 nM.

IC50 & Target

IC50: 5-46 nM (SYK, JAK)[1].

In Vitro

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. 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 Vivo

In a multiple myeloma (H929) xenograft model, Gusacitinib (ASN-002) exhibits significant efficacy in inhibiting tumor growth (>95%). It also significantly delays the onset of hind limb paralysis in the human erythroleukemia (HEL) mouse model. Gusacitinib (ASN-002) has good oral bioavailability, metabolic stability, is not a Pgp substrate, and shows little to no inhibition of CYP450 isozymes. Gusacitinib (ASN-002) shows a favorable safety profile in rat and dog toxicology studies[1].

Clinical Trial
Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
References
Molecular Weight

460.53

Formula

C₂₄H₂₈N₈O₂

CAS No.

1425381-60-7

SMILES

N#CCC1CCN(C2=NC(NC3=CC=C(N4CCC(O)CC4)C=C3)=C5C(C=NNC5=O)=N2)CC1

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Gusacitinib
Cat. No.:
HY-103018
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Gusacitinib

Cat. No.: HY-103018