PIM1/2 KINASE INHIBITOR VI
中文名称 | PIM1/2 KINASE INHIBITOR VI |
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中文同义词 | PIM激酶抑制剂(SMI-16A);化合物SMI-16A;5-(4-丙氧基亚苄基)噻唑烷-2,4-二酮 |
英文名称 | SMI-16a |
英文同义词 | SMI-16a;PIM1/2 Kinase Inhibitor VI;SMI-16a(PIM1/2 Kinase Inhibitor VI);SMI-16A;SMI 16A;SMI16A;2,4-Thiazolidinedione, 5-[(4-propoxyphenyl)methylene]-;SMI-16a,SMI 16a,inhibit,SMI16a,Pim,Inhibitor,Pim kinases;5-(4-propoxybenzylidene)thiazolidine-2,4-dione |
CAS号 | 587852-28-6 |
分子式 | C13H13NO3S |
分子量 | 263.31 |
EINECS号 | |
相关类别 | 细胞生物学试剂 |
Mol文件 | 587852-28-6.mol |
结构式 |
PIM1/2 KINASE INHIBITOR VI 性质
熔点 | 186.3-188.4 °C |
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密度 | 1.303±0.06 g/cm3(Predicted) |
储存条件 | 2-8°C(protect from light) |
溶解度 | 乙醇:3.0(最大浓度 mg/mL);11.39(最大浓度 mM) |
形态 | 固体 |
酸度系数(pKa) | 7.27±0.20(Predicted) |
颜色 | 浅黄至黄色 |
Target | Value |
Pim2
() | 20 nM |
Pim1
() | 150 nM |
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.
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.
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
---|---|---|---|---|---|
2024/08/19 | HY-101947 | SMI-16a | 1 mg | 304元 | |
2024/08/19 | HY-101947 | PIM1/2 KINASE INHIBITOR VI SMI-16a | 587852-28-6 | 5mg | 790元 |