Gusacitinib-ASN-002-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEGusacitinibCat. No.: HY-103018CAS No.: 1425381-60-7Synonyms: ASN-002分式: CHNO分量: 460.53作靶点: JAK; Syk作通路: Epigenetics; JAK/STAT Signaling; Stem Cell/Wnt; ProteinTyrosine Kinase/RTK储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C

2、6 months-20C 1 month溶解性数据体外实验 DMSO : 100 mg/mL (217.14 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.1714 mL 10.8571 mL 21.7141 mL5 mM 0.4343 mL 2.1714 mL 4.3428 mL10 mM 0.2171 mL 1.0857 mL 2.1714 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验 请根据您的实验动物和给药式选择适当的溶解案，配制前

3、请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 1.67 mg/mL (3.63 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 1.67 mg/mL (3.63 mM); Clear solution1

4、/2 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 Gusacitinib (ASN-002)种有效的、SYK 激酶和 JAK 激酶的双抑制剂，其 IC50 值为 5-46 nM。IC50 & Target IC50: 5-46 nM (SYK, JAK) 1.体外研究 In mechanistic cell-based studies involving IgE and cytokine stimulations, Gusacitinib (ASN-002) stronglysuppresses the

5、 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 celllines including DHL6, DHL4, OCI-LY10, H929, Pfeiffer, HT-1376, and Lovo, suggesting activity in both solidand hem

6、atological tumor types 1.体内研究 In a multiple myeloma (H929) xenograft model, Gusacitinib (ASN-002) exhibits significant efficacy ininhibiting tumor growth (95%). It also significantly delays the onset of hind limb paralysis in the humanerythroleukemia (HEL) mouse model. Gusacitinib (ASN-002) has good

7、 oral bioavailability, metabolic stability,is not a Pgp substrate, and shows little to no inhibition of CYP450 isozymes. Gusacitinib (ASN-002) shows afavorable safety profile in rat and dog toxicology studies 1.REFERENCES1. Sanjeeva Reddy, et al. Abstract 792: ASN002: A novel dual SYK/JAK inhibitor with strong antitumor activity. AACR 106th AnnualMeeting 2015; April 18-22, 2015; Philadelphia, PA.McePdfHeightCaution: Product has not been fully validated for medical applications.For resea