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1425381-60-7

1425381-60-7 structure
1425381-60-7 structure
  • Name: ASN-002
  • Chemical Name: ASN-002
  • CAS Number: 1425381-60-7
  • Molecular Formula: C24H28N8O2
  • Molecular Weight: 460.53
  • Catalog: Signaling Pathways Protein Tyrosine Kinase/RTK Syk
  • Create Date: 2018-06-25 12:08:02
  • Modify Date: 2024-01-02 10:18:54
  • ASN-002 is a potent dual inhibitor of spleen tyrosine kinase (SYK) and janus kinase (JAK) with IC50 values of 5-46 nM.

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

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

Molecular Formula C24H28N8O2
Molecular Weight 460.53