[CAS NO. 244240-24-2] LFM-A13
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PRODUCTS SPECIFICATIONS [244240-24-2]
Store
Catalog
SLK-S7734
Brand
Selleck
CAS
244240-24-2
DESCRIPTION [244240-24-2]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 360 |
| Molecular Formula | C11H8Br2N2O2 |
| SMILES | - |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7778 mL | 13.8889 mL | 27.7778 mL |
| 5 mM | 0.5556 mL | 2.7778 mL | 5.5556 mL |
| 10 mM | 0.2778 mL | 1.3889 mL | 2.7778 mL |
| 50 mM | 0.0556 mL | 0.2778 mL | 0.5556 mL |
Description
LFM-A13 is a specific Bruton's tyrosine kinase () inhibitor with 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. 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 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.
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. In primary myeloma-bearing SCID-rab mice, LFM-A13 inhibits osteoclast activity, prevents myeloma-induced bone resorption and suppresss myeloma growth.
References
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