Gusacitinib hydrochloride

CAS: 2228989-14-6 F: C24H29ClN8O2 W: 496.99

Gusacitinib (ASN-002) hydrochloride is an orally active dual SYK/JAK kinase inhibitor with IC50 values of 5, 46, 4, 11 a

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Bioactivity	Gusacitinib (ASN-002) hydrochloride is an orally active dual SYK/JAK kinase inhibitor with IC50 values of 5, 46, 4, 11 and 8 nM for SYK, JAK1, JAK2, JAK3 and TYK2, respectively. Gusacitinib hydrochloride rapidly and significantly suppressed key inflammatory pathways implicated in atopic dermatitis pathogenesis. Gusacitinib hydrochloride can be used in the research of chronic hand eczema and cancers such as basal cell carcinoma[1][2].
Target	IC50: 5-46 nM (SYK, JAK).
Invitro	Gusacitinib hydrochloride 在包括 DHL6、DHL4、OCI-LY10、H929、Pfeiffer、HT-1376 和 Lovo 在内的广泛的人类癌症细胞系中显示出抗增殖活性，表明其对实体瘤和血液病类型都有活性[3]。
In Vivo	Gusacitinib hydrochloride 在多发性骨髓瘤 (H929) 异种移植模型中抑制肿瘤生长 (>95%)[3]。Gusacitinib hydrochloride 显著推迟人类红血病 (HEL) 小鼠模型中后肢瘫痪的发生[3]。Gusacitinib hydrochloride 在大鼠和狗的毒理学研究中表现出良好的安全性[3]。
Name	Gusacitinib hydrochloride
CAS	2228989-14-6
Formula	C24H29ClN8O2
Molar Mass	496.99
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Xie Z, et al. Small-Molecule Kinase Inhibitors for the Treatment of Nononcologic Diseases. J Med Chem. 2021 Feb 11;64(3):1283-1345. [2]. Garcia-Melendo C, et al. Janus Kinase Inhibitors in Dermatology: Part 1 - General Considerations and Applications in Vitiligo and Alopecia Areata. Actas Dermo-Sifiliográficas, 2021, 112(6): 503-515. [3]. Sanjeeva Reddy, et al. Abstract 792: ASN002: A novel dual SYK/JAK inhibitor with strong antitumor activity. AACR 106th Annual Meeting 2015; April 18-22, 2015; Philadelphia, PA.