您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > Sovleplenib
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
Sovleplenib
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Sovleplenib图片
规格:98%
分子量:482.6
包装与价格:
包装价格(元)
5mg电议
10mg电议

产品介绍
Sovleplenib (HMPL-523) 是一种高效的、可口服的选择性 SYK 抑制剂,IC50 为 25 nM。具有抗肿瘤活性。Sovleplenib 可用于免疫性血小板减少症(ITP)的研究。
货号:ajcx37306
CAS:1415792-84-5
分子式:C24H30N6O3S
分子量:482.6
溶解度:N/A
纯度:98%
存储:Store at -20°C
库存:现货

Background:

Sovleplenib (HMPL-523) is a highly potent, orally available and selective SYK inhibitor with an IC50 of 25 nM. Anti-tumor activity. Sovleplenib can be used for the research of immune thrombocytopenia (ITP)[1].

Sovleplenib (HMPL-523) inhibits SYK, FLT3, KDR, LYN, FGFR2, and AUR A with IC50s of 0.025, 0.063, 0.390, 0.921, 3.214, 3.969 μM, respectively[1].Sovleplenib (HMPL-523) blocks phosphorylation of BLNK, downstream protein of Syk, in human mantle cell line REC-1 and human plasma cell line ARH-7777 with IC50s of 0.105 µM and 0.173 μM, respectively[2]. Sovleplenib also inhibits cell viability of Ba/F3 Tel-Syk with the IC50 of 0.033 μM[2].Sovleplenib also increases the apoptotic rate of REC-1 cells[2]. Sovleplenib shows the synergistic activities on killing human diffused large B cell lymphoma (DLBCL) in combination with other drugs such as BTK inhibitor, PI3Kδ inhibitors and Bcl2 family inhibitor[2].

Sovleplenib (HMPL-523) shows anti-tumor activity in vivo. Sovleplenib (100 mg/kg) inhibits tumor growth in REC-1 subcutaneous xenograft model[1].Sovleplenib (HMPL-523; 100 mg/kg; daily oral administration) shows potent anti-tumor activity in B cell lymphoma REC-1 (TGI: 59%) in Syk dependent xenograft models [2].

[1]. Su WG, et al. Preparation of pyridopyrazine derivatives for use as Syk inhibitors. WO2012167733 A1.
[2]. Na Yang, et al. HMPL-523, a Novel SYK Inhibitor Showed Anti-Tumor Activities In Vitro and In Vivo. Blood (2016) 128 (22): 3970.