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435300

Sigma-Aldrich

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(s):

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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About This Item

Empirical Formula (Hill Notation):
C11H8Br2N2O2
CAS Number:
Molecular Weight:
360.00
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77

Pricing and availability is not currently available.

Quality Level

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)

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This Item
435930L6920189406
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).

435300

LFM-A13

LFM-A13 ≥98% (HPLC), powder

L6920

LFM-A13

assay

≥97% (HPLC)

assay

≥95% (HPLC)

assay

≥98% (HPLC)

assay

≥97% (HPLC)

form

solid

form

powder

form

powder

form

solid

Quality Level

100

Quality Level

100

Quality Level

100

Quality Level

100

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

-

manufacturer/tradename

Calbiochem®

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

2-8°C

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, protect from light

storage condition

-

storage condition

OK to freeze, protect from light

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)
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

Warning

Toxicity: Standard Handling (A)

Reconstitution

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.

Legal Information

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

Storage Class

11 - Combustible Solids

wgk_germany

WGK 1

flash_point_f

Not applicable

flash_point_c

Not applicable


Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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