TCS PIM-11


Catalog No. size PriceQuantity
M6447-2 2mg solid $110
M6447-10 10mg solid $436

Description

Cas:491871-58-0

Product Information

TCS PIM-1 1 is an ATP-competitive Pim-1 kinase inhibitor.

 

Chemical Formula: C18H11BrN2O2

 

Exact Mass: 366.0004

 

Molecular Weight: 367.2

 

Elemental Analysis: C, 58.88; H, 3.02; Br, 21.76; N, 7.63; O, 8.71

 

Synonym: 

 

TCS PIM-1 1

SC204330

SC-204330

SC 204330

 

Chemical Name:  

3-Cyano-4-phenyl-6-(3-bromo-6-hydroxy)phenyl-2(1H)-pyridone

 

InChi Key:

SVSYJTYGPLVUOZ-UHFFFAOYSA-N

 

InChi Code:   InChI=1S/C18H11BrN2O2/c19-12-6-7-17(22)14(8-12)16-9-13(11-4-2-1-3-5-11)15(10-20)18(23)21-16/h1-9,22H,(H,21,23)

 

Smiles Code:

O=C1C(C#N)=C(C2=CC=CC=C2)C=C(C3=C(O)C=CC(Br)=C3)N1

 

 

Technical Data:

 

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >3 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

 

In Vitro

TCS PIM-1 1 (compound 1), a substituted pyridone scaffold, binds convincingly within the ATP-binding site of Pim-1 suggesting an ATP-competitive inhibitory mechanism. Preliminary data further suggests that TCS PIM-1 1 lacked in vitro inhibitory activity toward related serine/threonine kinases Pim-2 and MEK1/2. Hence, small molecules similar to TCS PIM-1 1 may serve as useful starting scaffolds for the development of other improved yet selective Pim-1 inhibitors. TCS PIM-1 1 serves both as a starting point for SAR chemical syntheses and was used for co-crystallization with Pim-1 protein.

 

 

References

 

  1. Cheney et al (2007) Identification and structure-activity relationships of substituted pyridones as inhibitors of Pim-1 kinase. Bioorg.Med.Chem.Letts. 17 1679 PMID: 17251021

 

Products are for research use only. Not for human use.

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