NIBR3049


Catalog No. size PriceQuantity
M6837-2 2mg solid $130
M6837-10 10mg solid $516

Description

Cas:1260181-14-3

Product Information

NIBR3049, also known as TCS-21311, is a potent and selective JAK3 inhibitor IC50 values of 8 nM.

 

Chemical Formula: C27H25F3N4O4

 

Exact Mass: 526.1828

 

Molecular Weight: 526.5162

 

Elemental Analysis: C, 61.59; H, 4.79; F, 10.82; N, 10.64; O, 12.15

 

Synonym:

 

TCS-21311

 

Chemical Name: 3-[5-[4-(2-Hydroxy-2-methyl-1-oxopropyl)-1-piperazinyl]-2-(trifluoromethyl)phenyl]-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione

 

InChi Key: 

CLGRAWDGLMENOD-UHFFFAOYSA-N

 

InChi Code: InChI=1S/C27H25F3N4O4/c1-26(2,38)25(37)34-11-9-33(10-12-34)15-7-8-19(27(28,29)30)17(13-15)21-22(24(36)32-23(21)35)18-14-31-20-6-4-3-5-16(18)20/h3-8,13-14,31,38H,9-12H2,1-2H3,(H,32,35,36)

 

Smiles Code:

O=C(C(C1=CC(N2CCN(C(C(C)(O)C)=O)CC2)=CC=C1C(F)(F)F)=C3C4=CNC5=C4C=CC=C5)NC3=O

 

 

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: >2 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 21311 (NIBR3049) exhibits IC50 values of 1.017, 2.550 and 8.055 μM for JAK1, JAK2 and TYK2, respectively in a enzymatic Jak assay.

TCS 21311 (NIBR3049) shows moderate activity in this cellular assay (IC50=689 nM, Jurkat cells), which is in good agreement with its enzymatic Pkc activity.

 

 

References

 

  1. Thoma G, et al. Identification of a potent Janus kinase 3 inhibitor with high selectivity within the Janus kinase family.J Med Chem. 2011 Jan 13;54(1):284-8.

 

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

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