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Gusacitinib (ASN-002)

  Cat. No.:  DC21100   Featured
Chemical Structure
1425381-60-7
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More than 5000 active chemicals with high quality for research!
Field of application
ASN-002 (Gusacitinib, ASN002) is a novel and potent dual inhibitor of SYK/JAK kinases with IC50 of 5-46 nM in biochemical assays.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1425381-60-7
Chemical Name: Gusacitinib (ASN-002)
Synonyms: Gusacitinib;ASN002;ASN-002;ASN 002
SMILES: N#CCC1CCN(C2=NC(NC3=CC=C(N4CCC(O)CC4)C=C3)=C5C(C=NNC5=O)=N2)CC1
Formula: C24H28N8O2
M.Wt: 460.542
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication: [1]. Sanjeeva Reddy, et al. Abstract 792: ASN002: A novel dual SYK/JAK inhibitor with strong antitumor activity. AACR 106th Annual Meeting 2015; April 18-22, 2015; Philadelphia, PA.
Description: ASN-002 is a potent dual inhibitor of spleen tyrosine kinase (SYK) and janus kinase (JAK) with IC50 values of 5-46 nM.
Target: IC50: 5-46 nM (SYK, JAK)[1].
In Vivo: In a multiple myeloma (H929) xenograft model, 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. ASN-002 has good oral bioavailability, metabolic stability, is not a Pgp substrate, and shows little to no inhibition of CYP450 isozymes. ASN-002 shows a favorable safety profile in rat and dog toxicology studies[1].
In Vitro: In mechanistic cell-based studies involving IgE and cytokine stimulations, ASN-002 strongly suppresses the SYK and JAK family kinase signaling pathways measured as pLAT and pSTAT levels, respectively. 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].
References: [1]. Sanjeeva Reddy, et al. Abstract 792: ASN002: A novel dual SYK/JAK inhibitor with strong antitumor activity. AACR 106th Annual Meeting 2015; April 18-22, 2015; Philadelphia, PA.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
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