Home Angiogenesis BTK inhibitor LFM-A13 For research use only.

LFM-A13

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.

LFM-A13 Chemical Structure

LFM-A13 Chemical Structure

CAS: 244240-24-2

Selleck's LFM-A13 has been cited by 6 Publications

2 Customer Reviews

Purity & Quality Control

Batch: S773401 DMSO] 72 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.98%
99.98

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Signaling Pathway

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BTK Signaling Pathway

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Sf21 cells Function assay Inhibition of xenopus recombinant Plx1 expressed in Sf21 cells by measuring autophosphorylation by 15-mins kinase assay, IC50=10.3 μM 17098432
U373 cells Function assay 100 μM Induction of aberrant monopolar and multipolar spindle formation in human U373 cells at 100 uM 17098432
BT20 cells Function assay 100 μM Induction of aberrant monopolar and multipolar spindle formation in human BT20 cells assessed as at 100 uM 17098432
PTK1 cells Proliferation assay 1 mM 50 mins Antiproliferative activity against prometaphase PTK1 cells assessed as complete arrest at 1 mM within 50 mins 17098432
Click to View More Cell Line Experimental Data

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 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]
In Vivo
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]
Animal Research Animal Models BALB/c mice bearing BCL-1 leukemia
Dosages 50 mg/kg/day, twice daily
Administration i.p.

Chemical Information & Solubility

Molecular Weight 360 Formula
C11H8Br2N2O2
 
CAS No. 244240-24-2 SDF Download LFM-A13 SDF
Smiles CC(=C(C#N)C(=O)NC1=C(C=CC(=C1)Br)Br)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 72 mg/mL ( (200.0 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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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