For research use only. Not for therapeutic Use.
Gusacitinib (ASN-002) is an orally active dual SYK/JAK kinase inhibitor with IC50 values of 5, 46, 4, 11 and 8 nM for SYK, JAK1, JAK2, JAK3 and TYK2, respectively. Gusacitinib rapidly and significantly suppressed key inflammatory pathways implicated in atopic dermatitis pathogenesis. Gusacitinib can be used in the research of chronic hand eczema and cancers such as basal cell carcinoma[1][2].
Gusacitinib 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[3].
Gusacitinib exhibits significant efficacy in inhibiting tumor growth (>95%), in a multiple myeloma (H929) xenograft model[3].
Gusacitinib significantly delays the onset of hind limb paralysis in the human erythroleukemia (HEL) mouse model[3].
Gusacitinib shows a favorable safety profile in rat and dog toxicology studies[3].
| Catalog Number | I019960 |
| CAS Number | 1425381-60-7 |
| Synonyms | 2-[1-[4-[4-(4-hydroxypiperidin-1-yl)anilino]-5-oxo-6H-pyrimido[4,5-d]pyridazin-2-yl]piperidin-4-yl]acetonitrile |
| Molecular Formula | C24H28N8O2 |
| Purity | ≥95% |
| 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 |
| SMILES | C1CN(CCC1CC#N)C2=NC3=C(C(=O)NN=C3)C(=N2)NC4=CC=C(C=C4)N5CCC(CC5)O |
| Reference | [1]. Xie Z, et al. Small-Molecule Kinase Inhibitors for the Treatment of Nononcologic Diseases. J Med Chem. 2021 Feb 11;64(3):1283-1345. [2]. Garcia-Melendo C, et al. Janus Kinase Inhibitors in Dermatology: Part 1 – General Considerations and Applications in Vitiligo and Alopecia Areata. Actas Dermo-Sifiliográficas, 2021, 112(6): 503-515. [3]. 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. |
