SMI-16a - Names and Identifiers
SMI-16a - Physico-chemical Properties
Molecular Formula | C13H13NO3S
|
Molar Mass | 263.31 |
Solubility | DMSO: ≥150 mg/mL |
Storage Condition | 2-8°C(protect from light) |
In vitro study | 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. |
In vivo study | 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. |
SMI-16a - Preparation solution concentration reference
| 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 |
Last Update:2024-01-02 23:10:35
SMI-16a - Introduction
SMI-16a is a chemical substance whose chemical name is (S)-N-(3-(4-methyl-1-(phenylsulfonyl)-1H-imidazol-2-yl)pyrazolo[1,5-a]pyrimidin-6-yl)-4-(methylsulfonyl)benzamide.
In terms of properties, SMI-16a is a white solid with a high melting point and boiling point. It is stable under acidic conditions but easily degrades under alkaline conditions. This compound is well soluble in solvents such as dimethyl sulfoxide (DMSO) and methylene chloride.
The main use of SMI-16a is as a selective protein kinase D(PKD) inhibitor. PKD is an important protein kinase associated with cancer development and progression, so SMI-16a have potential applications in anti-cancer research. It can inhibit the development of tumor by inhibiting the activity of PKD to interfere with the process of cell proliferation, migration and invasion.
The method of preparing SMI-16a is relatively complicated, and usually requires multiple reactions to form the target compound. The synthesis method requires the use of a series of intermediates and reagents, and also needs to control the reaction temperature and pH value and other factors, so it needs to be carried out in the Synthesis Laboratory.
Regarding safety information, since SMI-16a is a laboratory-synthesized compound, its toxicity and safety have not been fully studied. Therefore, it is necessary to strictly follow the safe operation procedures of the chemical laboratory and take necessary personal protective measures, such as wearing protective glasses, gloves and laboratory coats. At the same time, it is necessary to store this compound in a dry, cool place and avoid contact with oxidants and strong alkali substances to avoid unsafe chemical reactions. When using and handling the SMI-16a, the relevant safety operation guidelines and rules and regulations must be strictly observed.
Last Update:2024-04-09 21:11:58