587852-28-6
SMI-16a(SMI-16a)
CAS: 587852-28-6
化学式: C13H13NO3S
<"" ="xl" "">中文名 | SMI-16a |
英文名 | SMI-16a |
别名 | 化合物SMI-16A PIM激酶抑制剂(SMI-16A) 5-(4-丙氧基亚苄基)噻唑烷-2,4-二酮 |
英文别名 | SMI16A SMI-16A SMI-16a SMI 16A 2,4-Thiazolidinedione, 5-[(4-propoxyphenyl)methylene]- |
CAS | 587852-28-6 |
化学式 | C13H13NO3S |
分子量 | 263.31 |
溶解度 | DMSO: ≥ 150 mg/mL |
存储条件 | 2-8°C(protect from light) |
体外研究 | SMI-16a has excellent potency for inhibition of both Pim-1 and Pim-2. Treatment with Pim-2 short-interference RNA as well as the Pim inhibitor SMI-16a successfully restores osteoblastogenesis suppressed by all the above inhibitory factors and MM cells. The SMI-16a treatment potentiates BMP-2-mediated anabolic signaling while suppressing TGF-β signaling. |
体内研究 | Mice tolerate intraperitoneal dose of SMI-16a is 50 mg/kg daily for 5 days, while 100 mg/kg is overtly toxic. Treatment of the animals with SMI-16a for 5 days per week reduces the growth of tumors by approximately 50% and does not cause a loss of body weight. Subchronic dosing with SMI-16a does not affect the levels of red, white blood cells, including lymphocytes, monocytes, and granulocytes, indicating that the compound does not have myelosuppressive effects. SMI-16a does not have toxicity toward the liver as the albumin, alkaline phosphatase, and alanine aminotransferase levels are unchanged . SMI-16a effectively prevents bone destruction while suppressing MM tumor growth in MM animal models. |
587852-28-6 - 配置溶液浓度参考
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.798 ml | 18.989 ml | 37.978 ml |
5 mM | 0.76 ml | 3.798 ml | 7.596 ml |
10 mM | 0.38 ml | 1.899 ml | 3.798 ml |
5 mM | 0.076 ml | 0.38 ml | 0.76 ml |
587852-28-6 - 简介
SMI-16a是一种化学物质,其化学名称是(S)-N-(3-(4-methyl-1-(phenylsulfonyl)-1H-imidazol-2-yl)pyrazolo[1,5-a]pyrimidin-6-yl)-4-(methylsulfonyl)benzamide。它在酸性条件下稳定,但在碱性条件下容易降解。这种化合物在溶剂中能很好地溶解,如二甲基亚砜(DMSO)和二氯甲烷。
SMI-16a的主要用途是作为一种选择性蛋白激酶D(PKD)抑制剂。PKD是一种与癌症发展和进展相关的重要蛋白激酶,SMI-16a在抗癌研究中具有潜在的应用价值。它可以通过抑制PKD的活性来干扰细胞的增殖、迁移和侵袭等过程,从而抑制肿瘤的发展。
制备SMI-16a的方法比较复杂,通常需要多步反应来形成目标化合物。该合成方法需要使用一系列的中间体和试剂,还需要控制反应的温度和pH值等因素,需要在合成实验室中进行。
安全信息:SMI-16a是一种实验室合成的化合物,对其毒性和安全性的研究尚不充分。使用时需要严格遵守化学实验室的安全操作规程,并采取必要的个人防护措施,例如佩戴防护眼镜、手套和实验室外套。需要将此化合物储存在干燥、阴凉的地方,并避免与氧化剂和强碱物质接触,以避免发生不安全的化学反应。在使用和处理SMI-16a时,必须严格遵守相关的安全操作指南和规章制度。最后更新:2024-04-09 21:11:58