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LFM-A13 is a potent and selective inhibitor of Bruton's tyrosine kinase (BTK). LFM-A13 inhibits recombinant BTK with an IC50 value of 2.5 μM and has no activity on other protein kinases ( including JAK1, JAK3, HCK, EGFR kinase and insulin receptor kinase) at concentrations of up to 278 μM. 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, LFM-A13 inhibits osteoclast activity in primary myeloma-bearing SCID-rab mice, prevents myeloma-induced bone resorption and suppresss myeloma growth.
| Cell Experiment | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
|---|---|
| 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. |
| Molecular Weight | 360.0 |
| Formula | C11H8Br2N2O2 |
| CAS Number | 244240-24-2 |
| Solubility (25°C) | DMSO: ≥ 40 mg/mL warmed |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related BTK Products |
|---|
| BCPyr
BCPyr is a new candidate BTK degradation agent (DC50 = 800 nM). |
| BMS-986143
BMS-986143 is a potent, reversible inhibitor of tyrosine kinase (BTK), which has been successfully targeted by a number of irreversible tumor compounds. |
| BIIB091
The reversible BTK kinase inhibitor BIIB091 is a highly selective phase I clinical candidate compound for multiple sclerosis. |
| TAK-020
TAK-020 is a highly selective oral covalent BTK inhibitor with a promising safety and tolerability profile for both hematologic malignancies and autoimmune diseases. |
| BTK inhibitor 1 (Compound 27)
BTK inhibitor 1 (compound 27) is an inhibitor of BTK with an IC50 of 0.11 nM for Btk and inhibits B cell activation in hWB with an IC50 of 2 nM. |
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