1425381-60-7
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
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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. |
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| 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 |
| Molecular Formula | C24H28N8O2 |
|---|---|
| Molecular Weight | 460.53 |