| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
SYK, JAK (IC50 = 5-46 nM)
Gusacitinib targets SYK and JAK family kinases, which are key mediators of inflammatory and immune signaling pathways. It is a dual inhibitor with IC50 values of 5 nM for SYK, 46 nM for JAK1, 4 nM for JAK2, 11 nM for JAK3, and 8 nM for TYK2 in biochemical assays. By inhibiting these kinases, gusacitinib suppresses several cytokine axes (TH2/TH22/TH17/TH1) and improves epidermal barrier function. |
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| ln Vitro |
ASN-002 significantly inhibits the SYK and JAK family kinase signaling pathways, as indicated by pSTAT and pLAT levels, in mechanistic cell-based studies with IgE and cytokine stimulations. In a wide range of human cancer cell lines, such as DHL6, DHL4, OCI-LY10, H929, Pfeiffer, HT-1376, and Lovo, ASN-002 exhibits anti-proliferative activity, indicating activity in both solid and hematological tumor types[1]. |
| ln Vivo |
ASN-002 shows notable efficacy in preventing tumor growth (>95%) in a multiple myeloma (H929) xenograft model. In the human erythroleukemia (HEL) mouse model, it also markedly postpones the onset of hind limb paralysis. ASN-002 exhibits little to no inhibition of CYP450 isozymes, good oral bioavailability, metabolic stability, and is not a Pgp substrate. In toxicology studies on rats and dogs, ASN-002 exhibits a good safety profile[1]. |
| Enzyme Assay |
The in vitro enzyme assay for gusacitinib typically measures its ability to inhibit SYK and JAK kinase activity. These cell-free assays use purified recombinant kinases and peptide substrates in the presence of ATP. The compound's inhibitory potency (IC50) is determined by measuring the reduction in kinase activity. IC50 values of 5, 46, 4, 11, and 8 nM for SYK, JAK1, JAK2, JAK3, and TYK2, respectively, have been reported.
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| Cell Assay |
In vitro cellular assays for gusacitinib assess its ability to inhibit SYK and JAK-mediated signaling in cells. Cells are stimulated with IgE or cytokines, and the phosphorylation of downstream targets such as STAT and LAT (pSTAT and pLAT) is measured. The compound's anti-proliferative activity is assessed in a panel of human cancer cell lines. These assays demonstrate the compound's functional inhibition of its targets in a cellular context.
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| Animal Protocol |
In vivo animal studies for gusacitinib have been conducted in multiple myeloma (H929) xenograft models, where it showed >95% tumor growth prevention. In the human erythroleukemia (HEL) mouse model, it postponed the onset of hind limb paralysis. Toxicology studies in rats and dogs have shown a good safety profile. These studies support its development for both oncological and inflammatory indications.
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| ADME/Pharmacokinetics |
Gusacitinib is orally bioavailable with good metabolic stability. It exhibits little to no inhibition of CYP450 isozymes and is not a Pgp substrate. These favorable pharmacokinetic properties support once-daily oral dosing. The compound's oral bioavailability and metabolic stability have been confirmed in preclinical studies, and it has advanced to clinical trials.
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| Toxicity/Toxicokinetics |
Gusacitinib exhibits a good safety profile in toxicology studies on rats and dogs. It has been evaluated in clinical trials for the treatment of atopic dermatitis and nodular basal cell carcinoma. The clinical trial NCT02550678 is a study on the efficacy and safety of ASN-002 in adult patients with low-risk nodular basal cell carcinoma. Its safety profile supports further clinical development.
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| References |
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| Additional Infomation |
Gusacitinib is being investigated in the clinical trial NCT02550678 (a study on the efficacy and safety of ASN-002 in adult patients with low-risk nodular basal cell carcinoma).
Gusacitinib (ASN-002) is an orally active dual SYK/JAK kinase inhibitor with potent activity against SYK, JAK1, JAK2, JAK3, and TYK2. It has demonstrated antitumor activity in both hematological and solid tumor xenograft models. It is being investigated in clinical trials for the treatment of atopic dermatitis and nodular basal cell carcinoma. The compound suppresses inflammation, improves epidermal barrier function, and has anti-proliferative effects. It is not approved for clinical use and remains an investigational agent. |
| Molecular Formula |
C24H28N8O2
|
|---|---|
| Molecular Weight |
460.531523704529
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| Exact Mass |
460.233
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| Elemental Analysis |
C, 62.59; H, 6.13; N, 24.33; O, 6.95
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| CAS # |
1425381-60-7
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| Related CAS # |
Gusacitinib hydrochloride;2228989-14-6
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| PubChem CID |
71269142
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
2.6
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
34
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| Complexity |
775
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
NLFLXLJXEIUQDL-UHFFFAOYSA-N
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| InChi Code |
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)
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| Chemical Name |
2-[1-[4-[4-(4-hydroxypiperidin-1-yl)anilino]-5-oxo-6H-pyrimido[4,5-d]pyridazin-2-yl]piperidin-4-yl]acetonitrile
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| Synonyms |
ASN002; ASN 002; ASN-002; Gusacitinib; EN3351; EN-3351; EN 3351
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 92~100 mg/mL (199.8~217.1 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.67 mg/mL (3.63 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.67 mg/mL (3.63 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1714 mL | 10.8571 mL | 21.7141 mL | |
| 5 mM | 0.4343 mL | 2.1714 mL | 4.3428 mL | |
| 10 mM | 0.2171 mL | 1.0857 mL | 2.1714 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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