LFM-A13

Catalog No.S7734

LFM-A13 Chemical Structure

Molecular Weight(MW): 360

LFM-A13 is a specific Bruton's tyrosine kinase (BTK) inhibitor with IC50 of 2.5 μM, >100-fold selectivity over other protein kinases including JAK1, JAK2, HCK, EGFR,and IRK.

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1 Customer Review

  • Crosslinking FcγRIIB triggers apoptosis through Btk and p38 MAPK in human B cells. a Purified naïve, memory B cells and PCs (105/ml) from seven donors were each treated with 10 μg/ml of ICs in the presence of either 2 μM of LFM-A13 or 10 nM of ibrutinib for 24 h. Apoptotic cells were determined by Annexin V staining (Biolegend) using flow cytometry. The asterisks indicate that the differences between the groups compared are statistically significant (P < 0.05).

    J Biomed Sci, 2015, 22:87. . LFM-A13 purchased from Selleck.

Purity & Quality Control

Choose Selective BTK Inhibitors

Biological Activity

Description LFM-A13 is a specific Bruton's tyrosine kinase (BTK) inhibitor with IC50 of 2.5 μM, >100-fold selectivity over other protein kinases including JAK1, JAK2, HCK, EGFR,and IRK.
Targets
BTK [1]
(cell-free assay)
1.4 μM(Ki)
In vitro

In BTK+ B-lineage leukemic cells, LFM-A13 enhances their sensitivity to ceramide- or vincristine-induced apoptosis. [1] In BCL-1 cells, NALM-6 cells, or normal BALB/c splenocytes, LFM-13 inhibits the enzymatic activity of BTK in BCL-1 cells without affecting the BTK protein expression levels [2] In human neutrophils, LFM-A13 decreases the tyrosine phosphorylation induced by fMet-Leu-Phe and inhibits the production of superoxide anions and the stimulation of adhesion, chemotaxis, and phospholipase D activity. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Sf21 cells NFjUXFRHfW6ldHnvckBie3OjeR?= NIHQTFlKdmirYnn0bY9vKG:oIIjlco9xfXNicnXjc41jcW6jboSgVIx5OSCneIDy[ZN{\WRiaX6gV4YzOSClZXzsd{BjgSCvZXHzeZJqdmdiYYX0c5Bpd3OyaH;yfYxifGmxbjDifUAyPS2vaX7zJItqdmG|ZTDhd5NigSxiSVO1NF0yOC5|IN88US=> Ml3GNVcxQTh2M{K=
U373 cells NYnSR5pbTnWwY4Tpc44h[XO|YYm= MVyxNFAh|ryP MoDwTY5lfWO2aX;uJI9nKGGkZYLyZY51KG2xbn;wc4xieiCjbnSgcZVtfGmyb3zhdkB{eGmwZHzlJIZwem2jdHnvckBqdiCqdX3hckBWOzd|IHPlcIx{KGG2IEGwNEB2VQ>? NEPpXGQyPzB7OESzNi=>
BT20 cells Mn\uSpVv[3Srb36gZZN{[Xl? M1LwUFExOCEQvF2= MUnJcoR2[3Srb36gc4Yh[WKncoLhcpQhdW:wb4DvcIFzKGGwZDDteYx1cXCxbHHyJJNxcW6mbHWg[o9zdWG2aX;uJIlvKGi3bXHuJGJVOjBiY3XscJMh[XO|ZYPz[YQh[XNiYYSgNVAxKHWP MofpNVcxQTh2M{K=
PTK1 cells MXTQdo9tcW[ncnH0bY9vKGG|c3H5 MUGxJI1O NUjNWXRKPTBibXnudy=> M1y1WmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgdJJwdWW2YYDoZZNmKFCWS{GgZ4VtdHNiYYPz[ZN{\WRiYYOgZ49ueGyndHWgZZJz\XO2IHH0JFEhdU1id3n0bIlvKDVyIH3pcpM> Ml7TNVcxQTh2M{K=

... Click to View More Cell Line Experimental Data

In vivo In BALB/c mice bearing BCL-1 leukemia, combination of LFM-A13 (50 mg/kg/day i.p.) and the standard triple-drug VPL prolongs the median survival time. [2] In primary myeloma-bearing SCID-rab mice, LFM-A13 inhibits osteoclast activity, prevents myeloma-induced bone resorption and suppresss myeloma growth. [4]

Protocol

Animal Research:[4]
+ Expand
  • Animal Models: BALB/c mice bearing BCL-1 leukemia
  • Formulation: Suspended in 10% DMSO in PBS
  • Dosages: 50 mg/kg/day, twice daily
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 72 mg/mL warmed (200.0 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 360
Formula
C11H8Br2N2O2
 
CAS No. 244240-24-2
Storage powder
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Related Antibodies

BTK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID