| LFM-A13BTK-specific tyrosine kinase inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
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- Purity = 99.79%
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| Cas No. | 244240-24-2 | SDF | Download SDF |
| Synonyms | N/A | ||
| Chemical Name | (Z)-2-cyano-N-(2,5-dibromophenyl)-3-hydroxybut-2-enamide | ||
| Canonical SMILES | C/C(O)=C(C#N)/C(NC1=C(C=CC(Br)=C1)Br)=O | ||
| Formula | C11H8Br2N2O2 | M.Wt | 360 |
| Solubility | ≥36mg/mL in DMSO | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
Description:
IC50: 17.2 μM
Bruton’s tyrosine kinase (BTK), a member of the BTK/Tec family of protein tyrosine kinases, is a cytoplasmic PTK involved in signal transduction pathways regulating growth and differentiation of B-lineage lymphoid cells. BTK participates in signal transduction pathways initiated by the binding of a variety of extracellular ligands to their cell-surface receptors. LFM-A13 is a BTK-specific tyrosine kinase inhibitor.
In vitro: 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 [1].
In vivo: LFM-A13 exhibited a favorable pharmacokinetic behavior which was not adversely affected by the standard chemotherapy drugs and significantly improved the chemotherapy response and survival outcome of BCL-1 leukemia cells challenged mice. While only 14% of mice treated with the standard triple-drug combination treatment became long-term survivors, 41% of mice treated with this combination plus LFM-A13 survived long-term [2].
Clinical trial: Up to now, LFM-A13 is still in the preclinical development stage.
Reference:[1] Mahajan S, Ghosh S, Sudbeck EA, Zheng Y, Downs S, Hupke M, Uckun FM. Rational design and synthesis of a novel anti-leukemic agent targeting Bruton"s tyrosine kinase (BTK), LFM-A13 [alpha-cyano-beta-hydroxy-beta-methyl-N-(2, 5-dibromophenyl)propenamide]. J Biol Chem. 1999 Apr 2;274(14):9587-99.[2] Uckun FM, Zheng Y, Cetkovic-Cvrlje M, Vassilev A, Lisowski E, Waurzyniak B, Chen H, Carpenter R, Chen CL. In vivo pharmacokinetic features, toxicity profile, and chemosensitizing activity of alpha-cyano-beta-hydroxy-beta- methyl-N-(2,5-dibromophenyl)propenamide (LFM-A13), a novel antileukemic agent targeting Bruton"s tyrosine kinase. Clin Cancer Res. 2002 May;8(5):1224-33.
