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100128 A77 1726 - CAS 108605-62-5 - Calbiochem

100128
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Overview

Replacement Information

Key Spec Table

Empirical FormulaCAS #
C₁₂H₉F₃N₂O₂108605-62-5

Products

Catalogue NumberPackaging Qty/Pack
100128-5MG Plastic ampoule 5 mg
Description
OverviewLeflunomide metabolite that blocks TNF-dependent NF-κB activation and gene expression. Inhibits the activity of dihydroorotate dehydrogenase (DHO-DH; IC50 = 220 nM). Reported to reduce IFN-γ-induced expression of iNOS in L929 fibroblasts. Inhibits IL-1β-induced activation of COX-2 and PGE2 synthesis (IC50 = 130 nM) in A549 cells. A cell-permeable, reversible, and substrate competitive inhibitor that inhibits the IL-2-induced tyrosine phosphorylation of JAK1 and JAK3.
Catalogue Number100128
Brand Family Calbiochem®
SynonymsN-(4-Trifluoromethylphenyl)-2-cyano-3-hydroxycrotoamide
References
ReferencesJankovic, V., et al. 2000. Cell Immunol. 199, 73.
Hamilton, L.C., et al. 1999. Br. J. Pharmacol. 127, 1589.
Manna, S.K., and Aggarwal, B.B. 1999. J. Immunol. 162, 2095.
Elder, R.T., et al. 1997. J. Immunol. 159, 22.
Xu, X., et al. 1996. Biochem. Pharmacol. 52, 527.
Xu, X., et al. 1995. J. Biol. Chem. 270, 12398.
Mattar, T., et al. 1993. FEBS Lett. 334, 161.
Product Information
CAS number108605-62-5
ATP CompetitiveN
FormWhite solid
Hill FormulaC₁₂H₉F₃N₂O₂
Chemical formulaC₁₂H₉F₃N₂O₂
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary TargetDihydroorotate dehydrogenase (DHO-DH)
Primary Target IC<sub>50</sub>220 nM against DHO-DH
Purity≥97% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
R PhraseR: 40

Limited evidence of a carcinogenic effect.
S PhraseS: 22-36

Do not breathe dust.
Wear suitable protective clothing.
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Carcinogenic / Teratogenic
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications

Documentation

A77 1726 - CAS 108605-62-5 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

A77 1726 - CAS 108605-62-5 - Calbiochem Certificates of Analysis

TitleLot Number
100128

References

Reference overview
Jankovic, V., et al. 2000. Cell Immunol. 199, 73.
Hamilton, L.C., et al. 1999. Br. J. Pharmacol. 127, 1589.
Manna, S.K., and Aggarwal, B.B. 1999. J. Immunol. 162, 2095.
Elder, R.T., et al. 1997. J. Immunol. 159, 22.
Xu, X., et al. 1996. Biochem. Pharmacol. 52, 527.
Xu, X., et al. 1995. J. Biol. Chem. 270, 12398.
Mattar, T., et al. 1993. FEBS Lett. 334, 161.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision11-January-2010 RFH
SynonymsN-(4-Trifluoromethylphenyl)-2-cyano-3-hydroxycrotoamide
DescriptionLeflunomide metabolite that blocks TNF-dependent NF-κB activation and gene expression. Inhibits the activity of dihydroorotate dehydrogenase (DHO-DH; IC50 = 220 nM). Reported to reduce IFN-γ-induced expression of iNOS in L929 fibroblasts. Inhibits IL-1β-induced activation of COX-2 and PGE2 synthesis (IC50 = 130 nM) in A549 cells.A cell-permeable, reversible and substrate competitive inhibitor that inhibits the IL-2-induced tyrosine phosphorylation of JAK1 and JAK3.
FormWhite solid
Intert gas (Yes/No) Packaged under inert gas
CAS number108605-62-5
Chemical formulaC₁₂H₉F₃N₂O₂
Structure formulaStructure formula
Purity≥97% by HPLC
SolubilityDMSO (35 mg/ml)
Storage +2°C to +8°C
Protect from light
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C
Toxicity Carcinogenic / Teratogenic
ReferencesJankovic, V., et al. 2000. Cell Immunol. 199, 73.
Hamilton, L.C., et al. 1999. Br. J. Pharmacol. 127, 1589.
Manna, S.K., and Aggarwal, B.B. 1999. J. Immunol. 162, 2095.
Elder, R.T., et al. 1997. J. Immunol. 159, 22.
Xu, X., et al. 1996. Biochem. Pharmacol. 52, 527.
Xu, X., et al. 1995. J. Biol. Chem. 270, 12398.
Mattar, T., et al. 1993. FEBS Lett. 334, 161.