ASN-002
- Gusacitinib
- Soluble in DMSO
- MF: C24H28N8O2
- MW: 460.53
Description
ASN-002 is a orally available potent dual inhibitor of SYK (Spleen Tyrosine Kinase) and pan-JAK (Janus kinases) with IC50 values of 5-46 nM in biochemical assays. In mechanistic cell-based studies involving IgE and cytokine stimulations, ASN002 strongly suppressed the SYK and JAK family kinase signaling pathways measured as pLAT and pSTAT levels, respectively. The compound showed 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. In a multiple myeloma (H929) xenograft model, ASN002 exhibited significant efficacy in inhibiting tumor growth (>95%). It also significantly delayed the onset of hind limb paralysis in the human erythroleukemia (HEL) mouse model.
More Information
| Parent CAS No. | 1425381-60-7 |
|---|---|
| Chemical Name | 2-(1-(4-(4-(4-Hydroxypiperidin-1-yl)phenylamino)-5-oxo-5,6-dihydropyrimido[5,4-d]pyridazin-2-yl)piperidin-4-yl)acetonitrile |
| extra_info | Sold in collaboration with Chemietek |
| SMILES | N1=CC2=NC(N3CCC(CC#N)CC3)=NC(NC3C=CC(N4CCC(O)CC4)=CC=3)=C2C(=O)N1 |
| MFCD | N.A. |
| InChi | InChI=1S/C24H28N8O2/c25-10-5-16-6-11-32(12-7-16)24-28-20-15-26-30-23(34)21(20)22(29-24)27-17-1-3-18(4-2-17)31-13-8-19(33)9-14-31/h1-4,15-16,19,33H,5-9,11-14H2,(H,30,34)(H,27,28,29) |
| InChiKey | NLFLXLJXEIUQDL-UHFFFAOYSA-N |
| CID | 71269142 |
| Short Description | SYK and JAK inhibitor |
References
- NS Rao, et al, ASN002: A Potent Dual SYK/JAK Inhibitor Currently in a Phase I/II Study Shows Strong Antitumor Activity in Preclinical Studies, Blood 2015 vol. 126 no. 23 4009.
- S. 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.
- AB Pavel et al. Oral Janus kinase/SYK inhibition (ASN002) suppresses inflammation and improves epidermal barrier markers in patients with atopic dermatitis. J Allergy Clin Immunol. 2019 Oct;144(4):1011-1024.
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