435300

LFM-A13

A potent, cell-permeable, reversible, substrate competitive, and specific inhibitor of Bruton′s Tyrosine Kinase (BTK; IC₅₀ = 17.2 µM for human BTK in vitro and IC₅₀ = 2.5 µM for recombinant BTK).

• Synonym(e): LFM-A13, α-Cyano-β-hydroxy-β-methyl-N-(2,5-dibromophenyl)propenamide, BTK Inhibitor I, Bruton′s Tyrosine Kinase Inhibitor I
• Empirische Formel (Hill-System): C₁₁H₈Br₂N₂O₂
• CAS-Nummer: 62004-35-7
• Molekulargewicht: 360.00
• UNSPSC-Code: 12352200
• NACRES: NA.77

Eigenschaften

• Qualitätsniveau: 100
• Assay: ≥97% (HPLC)
• Form: solid
• Hersteller/Markenname: Calbiochem^®
• Lagerbedingungen: OK to freeze; protect from light
• Farbe: light brown
• Löslichkeit: DMSO: 200 mg/mL
• Versandbedingung: ambient
• Lagertemp.: 2-8°C
• InChI: 1S/C11H8Br2N2O2/c1-6(16)8(5-14)11(17)15-10-4-7(12)2-3-9(10)13/h2-4,16H,1H3,(H,15,17)
• InChIKey: UVSVTDVJQAJIFG-UHFFFAOYSA-N

Beschreibung

Allgemeine Beschreibung

A potent, cell-permeable, reversible, substrate competitive, and specific inhibitor of Bruton’s Tyrosine Kinase (BTK; IC₅₀ = 17.2 µM for human BTK in vitro and IC₅₀ = 2.5 µM for recombinant BTK). Also inhibits Polo-like kinase in an ATP-competitive manner (IC₅₀ = 10 µM and 61 µM for Plx1 and Plk3, respectively), and displays antitumor properties. Does not affect the enzymatic activity of other protein tyrosine kinases, including EGFR, HCK, IRK JAK1, and JAK3 even at concentrations of 278 µM. Enhances the chemosensitivity of BTK-positive B-lineage leukemia cells to ceramide- and vincristine-induced apoptosis.

A potent, cell-permeable, reversible, substrate competitive, and specific inhibitor of Bruton′s tyrosine kinase (BTK; IC₅₀ = 17.2 µM for human BTK in vitro and IC₅₀ = 2.5 µM for recombinant BTK). Also inhibits Polo-like kinase in an ATP-competitive manner (IC₅₀ = 10 µM and 61 µM for Plx1 and Plk3, respectively), and displays antitumor properties. Does not affect the enzymatic activity of other protein tyrosine kinases, including EGFR, HCK, IRK JAK1, and JAK3 even at concentrations of 278 µM. Enhances the chemosensitivity of BTK-positive B-lineage leukemia cells to ceramide- and vincristine-induced apoptosis.

Biochem./physiol. Wirkung

Cell permeable: yes

Primary Target
Human Bruton′s Tyrosine Kinase (BTK)

Product competes with ATP.

Reversible: yes

Target IC₅₀: 17.2 µM for human BTK in vitro and 2.5 µM for recombinant BTK

Verpackung

Packaged under inert gas

Warnhinweis

Toxicity: Standard Handling (A)

Rekonstituierung

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Sonstige Hinweise

Uckun, F.M., et al. 2006. Bioorg. Med. Chem. In press.
Mahajan, S., et al. 1999. J. Biol. Chem. 274, 9587.
Vassilev, A., et al. 1999. J. Biol. Chem. 274, 1646.

Rechtliche Hinweise

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 1
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable