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Gusacitinib (ASN-002) (ASN-002) is spleen tyrosine kinase (SYK) and janus kinase (JAK) inhibitor (IC50: 5-46 nM).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $35 | In Stock | |
5 mg | $81 | In Stock | |
10 mg | $125 | In Stock | |
25 mg | $198 | In Stock | |
50 mg | $369 | In Stock | |
100 mg | $549 | In Stock | |
200 mg | $789 | In Stock | |
1 mL x 10 mM (in DMSO) | $118 | In Stock |
Description | Gusacitinib (ASN-002) (ASN-002) is spleen tyrosine kinase (SYK) and janus kinase (JAK) inhibitor (IC50: 5-46 nM). |
Targets&IC50 | Syk/JAK:5-46 nM |
In vitro | 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[1]. 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. |
In vivo | Gusacitinib (ASN-002) shows a favorable safety profile in rat and dog toxicology studies[1]. Gusacitinib (ASN-002) has good oral bioavailability, metabolic stability, is not a Pgp substrate, and shows little to no inhibition of CYP450 isozymes. In a multiple myeloma (H929) xenograft model, Gusacitinib (ASN-002) exhibits significant efficacy in inhibiting tumor growth (>95%) and it also significantly delays the onset of hind limb paralysis in the human erythroleukemia (HEL) mouse model. |
Alias | ASN-002 |
Molecular Weight | 460.53 |
Formula | C24H28N8O2 |
Cas No. | 1425381-60-7 |
Smiles | OC1CCN(CC1)c1ccc(Nc2nc(nc3cn[nH]c(=O)c23)N2CCC(CC#N)CC2)cc1 |
Relative Density. | 1.47 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 95 mg/mL (206.28 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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