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).
別名:
LFM-A13, α-Cyano-β-hydroxy-β-methyl-N-(2,5-dibromophenyl)propenamide, BTK Inhibitor I, Bruton′s Tyrosine Kinase Inhibitor I
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この商品について
実験式（ヒル表記法）:
C11H8Br2N2O2
CAS番号:
分子量:
360.00
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥97% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
Quality Segment
assay
≥97% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
light brown
solubility
DMSO: 200 mg/mL
shipped in
ambient
storage temp.
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)
InChI key
UVSVTDVJQAJIFG-UHFFFAOYSA-N
General description
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 Actions
Cell permeable: yes
Primary Target
Human Bruton′s Tyrosine Kinase (BTK)
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
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
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.
Mahajan, S., et al. 1999. J. Biol. Chem. 274, 9587.
Vassilev, A., et al. 1999. J. Biol. Chem. 274, 1646.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
保管分類
11 - Combustible Solids
wgk
WGK 1
flash_point_f
Not applicable
flash_point_c
Not applicable
適用法令
試験研究用途を考慮した関連法令を主に挙げております。化学物質以外については、一部の情報のみ提供しています。 製品を安全かつ合法的に使用することは、使用者の義務です。最新情報により修正される場合があります。WEBの反映には時間を要することがあるため、適宜SDSをご参照ください。
Deleterious substance
pdsc
435300-5RMG: + 435300-5MG:
jan