Description
Gusacitinib (ASN-002) is an orally active and potent dual inhibitor of spleen tyrosine kinase (SYK) and janus kinase (JAK) with IC50 values of 5-46 nM. Gusacitinib has anti-cancer activity in both solid and hematological tumor types.
Product information
CAS Number: 1425381-60-7
Molecular Weight: 460.53
Formula: C24H28N8O2
Chemical Name: 2-[1-(4-{[4-(4-hydroxypiperidin-1-yl)phenyl]amino}-5-oxo-5H,6H-pyrimido[4,5-d]pyridazin-2-yl)piperidin-4-yl]acetonitrile
Smiles: N#CCC1CCN(CC1)C1N=C2C=NNC(=O)C2=C(NC2=CC=C(C=C2)N2CCC(O)CC2)N=1
InChiKey: NLFLXLJXEIUQDL-UHFFFAOYSA-N
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)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 100 mg/mL (217.14 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
In mechanistic cell-based studies involving IgE and cytokine stimulations, Gusacitinib (ASN-002) strongly suppresses the SYK and JAK family kinase signaling pathways measured as pLAT and pSTAT levels, respectively. Gusacitinib (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.
In Vivo:
In a multiple myeloma (H929) xenograft model, Gusacitinib (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. Gusacitinib (ASN-002) has good oral bioavailability, metabolic stability, is not a Pgp substrate, and shows little to no inhibition of CYP450 isozymes. Gusacitinib (ASN-002) shows a favorable safety profile in rat and dog toxicology studies.
Products are for research use only. Not for human use.
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