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. |
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 |
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