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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. |
| Synonyms | 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 | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 95 mg/mL (206.28 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.34 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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