Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Sovleplenib (HMPL523) 是一种可口服且具有选择性和高效性的脾酪氨酸激酶 SYK 抑制剂,IC50 为 25 nM。Sovleplenib 具有抗肿瘤活性,可用于免疫性血小板减少症(ITP)的研究。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 1,680 | 现货 | ||
5 mg | ¥ 3,970 | 现货 | ||
10 mg | ¥ 5,760 | 现货 | ||
25 mg | ¥ 8,570 | 现货 | ||
50 mg | ¥ 11,500 | 现货 | ||
100 mg | ¥ 15,500 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 4,360 | 现货 |
产品描述 | Sovleplenib (HMPL523) is an orally available, selective and potent inhibitor of the splenic tyrosine kinase SYK with an IC50 of 25 nM.Sovleplenib has antitumor activity and may be used in studies of immune thrombocytopenia (ITP). |
靶点活性 | Syk:25 nM |
体外活性 |
Sovleplenib (HMPL-523) exhibits inhibitory activity with IC50 values of 0.025 μM, 0.063 μM, 0.390 μM, 0.921 μM, 3.214 μM, and 3.969 μM against SYK, FLT3, KDR, LYN, FGFR2, and AUR A, respectively.[2] Sovleplenib effectively blocks the phosphorylation of BLNK, a downstream protein of Syk, in human mantle cell line REC-1 and human plasma cell line ARH-7777, with IC50 values of 0.105 μM and 0.173 μM, respectively.[2] Sovleplenib also significantly reduces cell viability in Ba/F3 Tel-Syk cells with an IC50 of 0.033 μM and increases the rate of apoptosis in REC-1 cells.[2] Sovleplenib demonstrates synergistic effects in combination with other drugs, including BTK inhibitors, PI3Kδ inhibitors, and Bcl2 family inhibitors, in killing human-diffuse large B cell lymphoma (DLBCL).[2] |
体内活性 |
Sovleplenib (HMPL-523) (10 and 100 mg/kg; once daily for 8 days; Balb/c nude mice with subcutaneously implanted REC-1 cells or intravenously injected BA/F3 cells or BA/F3 TEL-SYK cells) Inhibited tumor growth in REC-1 subcutaneous xenograft model at 100 mg/kg.[1] Sovleplenib (HMPL-523; 100 mg/kg; daily oral administration; for 8 days) shows potent anti-tumor activity in B cell lymphoma REC-1 (TGI: 59%) in Syk-dependent xenograft models.[2] |
别名 | HMPL 523, HMPL523, HMPL-523 |
分子量 | 482.6 |
分子式 | C24H30N6O3S |
CAS No. | 1415792-84-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 14.48 mg/mL (30 mM), Sonication and heating are recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.0721 mL | 10.3605 mL | 20.7211 mL | 51.8027 mL |
5 mM | 0.4144 mL | 2.0721 mL | 4.1442 mL | 10.3605 mL | |
10 mM | 0.2072 mL | 1.0361 mL | 2.0721 mL | 5.1803 mL | |
20 mM | 0.1036 mL | 0.518 mL | 1.0361 mL | 2.5901 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Sovleplenib 1415792-84-5 Angiogenesis Tyrosine Kinase/Adaptors Syk HMPL 523 HMPL523 HMPL-523 Inhibitor inhibitor inhibit