LFM-A13
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
IC50:17.2 μM
布鲁顿氏酪氨酸激酶(BTK)属于蛋白酪氨酸激酶BTK/Tec家族,是一种细胞质PTK,参与信号转导途径,调节B-谱系淋巴样细胞生长与分化.BTK参与由多种细胞外配体结合其细胞表面受体而介导的信号转导途径.LFM-A13是一种BTK特异性酪氨酸激酶抑制剂.
体外:LFM-A13抑制表达于杆状病毒表达载体系统的重组BTK.在BTK激酶实验中,除了LFM-A13的显著效力,LFM-A13也是BTK的高特异性抑制剂.即使在极高浓度下,LFM-A13对其它蛋白酪氨酸激酶活性无效[1].
体内:LFM-A13显示出良好的药物动力学特征,不受标准化疗药物的不利影响,显著地增强BCL-1白血病细胞挑战的小鼠中的化疗疗效及存活率.在接受标准3种药物联合治疗的小鼠中,只有14%能长期存活.在同时接受上述治疗以及LFM-A13治疗的小鼠中,41%小鼠能长期存活[2].
临床试验:截至目前,LFM-A13还处于临床前开发阶段.
参考文献：
[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.
| Storage | Store at -20°C |
| M.Wt | 360 |
| Cas No. | 244240-24-2 |
| Formula | C11H8Br2N2O2 |
| Solubility | ≥36 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH |
| Chemical Name | (Z)-2-cyano-N-(2,5-dibromophenyl)-3-hydroxybut-2-enamide |
| SDF | Download SDF |
| Canonical SMILES | C/C(O)=C(C#N)/C(NC1=C(C=CC(Br)=C1)Br)=O |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
质量控制和MSDS
- 批次:
化学结构
