TCS 359
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.
TCS 359是一种有效的fms样酪氨酸激酶-3(FLT3)抑制剂[1][2],IC50值为0.042 ±0.03 M[2]。
FLT3是一种受体酪氨酸激酶。通过造血调控,FLT3在急性髓性白血病(AML)的发病机制中扮演重要角色[3]。
对于MV4-11细胞系(表达组成性活化的突变FLT3的人类急性髓性白血病细胞系)的增殖,TCS 359的IC50值为0.34 M[2]。
TCS359在小鼠中可阻断FLT3配体促进双细胞胚胎发育到孵化囊胚期的能力。TCS 359也可降低FLT3配体在四细胞期后早期胚胎中的表达。如果没有外源的FLT3配体,TCS 359不能对胚胎发育造成影响[4]。使用另一种FLT3抑制剂SU5416,22个被分析的病人中有21个有FLT3蛋白表达,17个有基线水平的磷酸化FLT3表达。在这17个表达磷酸化FLT3的病人中,相对于基线抑制50%以上的有七例,相对于基线抑制范围为20-50%的则有另外三例。大部分使用SU5416治疗的AML病人的全血裂解液中发现FLT3磷酸化现象。约有50%的AML病人的骨髓穿刺液中可检出活化的FLT3[5]。
参考文献:
[1]. Trzcinska-Daneluti A.M., Nguyen L., Jiang C., et al. Use of Kinase Inhibitors to Correct ΔF508-CFTR Function. Molecular & Cellular Proteomics, 2012, 11(9):745-757.
[2]. Patch R.J., Baumann C.A., Liu J., et al. Identification of 2-acylaminothiophene-3-carboxamides as potent inhibitors of FLT3. Bioorganic & Medicinal Chemistry Letters, 2006, 16: 3282-3286.
[3]. Kar R.K., Suryadevara P., Roushan R., et al. Quantifying the Structural Requirements for Designing Newer FLT3 Inhibitors. Medicinal Chemistry, 2012, 8:913-927.
[4]. Nishijima C., Kawamura K., Okamoto N., et al. Regulation of Preimplantation Embryo Development in Mice by FMS-like Tyrosine Kinase 3 Ligand. Journal of Mammalian Ova Research, 2014, 31(1):45-51.
[5]. O'Farrell A.M., Yuen H.A., Smolich B., et al. Effects of SU5416, a small molecule tyrosine kinase receptor inhibitor, on FLT3 expression and phosphorylation in patients with refractory acute myeloid leukemia. Leuk. Res., 2004, 28(7):679-89.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 360.43 |
Cas No. | 301305-73-7 |
Formula | C18H20N2O4S |
Solubility | insoluble in EtOH; insoluble in H2O; ≥9 mg/mL in DMSO |
Chemical Name | 2-[(3,4-dimethoxybenzoyl)amino]-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxamide |
SDF | Download SDF |
Canonical SMILES | COC1=C(C=C(C=C1)C(=O)NC2=C(C3=C(S2)CCCC3)C(=O)N)OC |
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。 |
Description | TCS 359是一种有效的FLT3受体酪氨酸激酶抑制剂,IC50值为42 nM。 | |||||
靶点 | FLT3 | |||||
IC50 | 42 nM |
质量控制和MSDS
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