| Identification | Back Directory | [Name]
SMI-16a | [CAS]
587852-28-6 | [Synonyms]
SMI-16a
SMI-16A;SMI 16A;SMI16A
PIM1/2 Kinase Inhibitor VI
SMI-16a(PIM1/2 Kinase Inhibitor VI)
2,4-Thiazolidinedione, 5-[(4-propoxyphenyl)methylene]- | [Molecular Formula]
C13H13NO3S | [MDL Number]
MFCD31382191 | [MOL File]
587852-28-6.mol | [Molecular Weight]
263.31 |
| Chemical Properties | Back Directory | [Melting point ]
186.3-188.4 °C | [density ]
1.303±0.06 g/cm3(Predicted) | [storage temp. ]
Keep in dark place,Sealed in dry,2-8°C | [solubility ]
Ethanol:3.0(Max Conc. mg/mL);11.39(Max Conc. mM) | [form ]
A solid | [pka]
7.27±0.20(Predicted) | [color ]
Light yellow to yellow | [InChI]
1S/C13H13NO3S/c1-2-7-17-10-5-3-9(4-6-10)8-11-12(15)14-13(16)18-11/h3-6,8H,2,7H2,1H3,(H,14,15,16) | [InChIKey]
GBWOSXZUTXXXQF-UHFFFAOYSA-N | [SMILES]
S1C(=O)NC(=O)C1=Cc2ccc(cc2)OCCC |
| Hazard Information | Back Directory | [Description]
SMI-16a is a Pim-1 kinase inhibitor (IC50 = 63 nM).1 It is selective for Pim-1 over a panel of 60 kinases. SMI-16a (5 μM) inhibits phosphorylation of the Pim-1 target protein Bad in DU145-Pim cells and inhibits the growth of PC3, DU145, LNCaP, K562, and MV4-11 cancer cells. It induces apoptosis and cell cycle arrest at the G1 phase in DU145 cells. | [Uses]
SMI-16a is a selective Pim kinase inhibitor with IC50 values of 0.15, 0.02 and 48 μM for Pim1, Pim2 and PC3 cells, respectively. | [in vivo]
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 [1]. SMI-16a effectively prevents bone destruction while suppressing MM tumor growth in MM animal models[2]. | [IC 50]
PIM1; PIM2 | [References]
[1] Xia Z, et al. Synthesis and evaluation of novel inhibitors of Pim-1 and Pim-2 protein kinases. J Med Chem. 2009 Jan 8;52(1):74-86. DOI:10.1021/jm800937p
[2] Hiasa M, et al. Pim-2 kinase is an important target of treatment for tumor progression and bone loss in myeloma. Leukemia. 2015 Jan;29(1):207-17. DOI:10.1038/leu.2014.147 |
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| Company Name: |
Twochem Co.Ltd.
|
| Tel: |
021-58111628 15800915896 |
| Website: |
cn.twochem.com |
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