TCS PIM-1 4aA selective and ATP-competitive Pim kinase inhibitor

TCS PIM-1 4a (CAS 438190-29-5)

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Synonym: (5Z)-5-[[3-(Trifluoromethyl)phenyl]methylene]-2,4-thiazolidinedione thiazolidine-2,4-dione, 4a; SMI-4a
Application: A selective and ATP-competitive Pim kinase inhibitor
CAS Number: 438190-29-5
Purity: >98%
Molecular Weight: 273.23
Molecular Formula: C11H6F3NO2S
* Refer to Certificate of Analysis for lot specific data (including water content).
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TCS PIM-1 4a is a selective and ATP-competitive Pim kinase inhibitor (IC50 values = 24 and 100 nM for Pim-1 and Pim-2, respectively). TCS PIM-1 4a has been shown to display selectivity over a panel of approximately 50 other kinases tested. This compound also exhibits cytotoxicity in PC3 prostate carcinoma cells in vitro. TCS PIM-1 4a is an inhibitor of Aldose Reductase and Cox-2.


References

Xia et al (2009) Synthesis and evaluation of novel inhibitors of Pim-1 and Pim-2 protein kinases. J.Med.Chem. 52 74.

Appearance :
Powder
Physical State :
Solid
Solubility :
Soluble in DMSO (55 mg/ml at 25 °C), ethanol (32 mg/ml at 25 °C), and water (slightly at 25 °C).
Storage :
Desiccate at 4° C
Density :
~1.53 g/cm3 (Predicted)
Refractive Index :
n20D ~1.60 (Predicted)
IC50 :
Pim-1: IC50 = 24 nM (human); Pim-2: IC50 = 0.1 µM (human); PC-3: IC50 = 17 µM (human); DLD-1: IC50 = 17.8 µM (human); HT-29: IC50 = 31.4 µM (human)
Ki Data :
Pim-1: Ki= 24 nM (human); Pim-2: Ki= 0.1 µM (human)
pK Values :
pKa: 7.38 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
1361334
MDL Number :
MFCD01152003
SMILES :
C1=CC(=CC(=C1)C(F)(F)F)/C=C\2/C(=O)NC(=O)S2

Download SDS (MSDS)

Certificate of Analysis

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