product name LFM-A13
Description: LFM-A13 is a specific Brutons 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 inhibited recombinant BTK expressed in a baculovirus expression vector system. Besides its remarkable potency in BTK kinase assays, LFM-A13 was also found to be a highly specific inhibitor of BTK. Even at very high concentrations, LFM-A13 did not affect the activity of other protein tyrosine kinases.
References: J Biol Chem. 1999 Apr 2;274(14):9587-99; Clin Cancer Res. 2002 May;8(5):1224-33; Am J Hematol. 2013 Jun;88(6):463-71.
360
Formula
C11H8Br2N2O2
CAS No.
244240-24-2
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 72 mg/mL (200.0 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19401386
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: |
|---|---|
| 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. |
| Animal model | |
| Formulation & Dosage | |
| References | J Biol Chem. 1999 Apr 2;274(14):9587-99; Clin Cancer Res. 2002 May;8(5):1224-33; Am J Hematol. 2013 Jun;88(6):463-71. |
Related Posts
product name LFM-A13
Description: LFM-A13 is a specific Brutons 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 inhibited recombinant BTK expressed in a baculovirus expression vector system. Besides its remarkable potency in BTK kinase assays, LFM-A13 was also found to be a highly specific inhibitor of BTK. Even at very high concentrations, LFM-A13 did not affect the activity of other protein tyrosine kinases.
References: J Biol Chem. 1999 Apr 2;274(14):9587-99; Clin Cancer Res. 2002 May;8(5):1224-33; Am J Hematol. 2013 Jun;88(6):463-71.
360
Formula
C11H8Br2N2O2
CAS No.
244240-24-2
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 72 mg/mL (200.0 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19401386
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: |
|---|---|
| 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. |
| Animal model | |
| Formulation & Dosage | |
| References | J Biol Chem. 1999 Apr 2;274(14):9587-99; Clin Cancer Res. 2002 May;8(5):1224-33; Am J Hematol. 2013 Jun;88(6):463-71. |