Radotinib(IY-5511)
![mRNA synthesis](/media/diy/images/page/figure1-mrna.png)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
![Tyramine Signal Amplification (TSA)](/media/diy/images/page/figure2-01.png)
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
![screening library](/media/diy/images/page/figure3-01.png)
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
![Cell Counting Kit-8 (CCK-8)](/media/diy/images/page/CCK-8.jpg)
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
![SYBR Safe DNA Gel Stain](/media/diy/images/page/SYBR Safe DNA Gel Stain.png)
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
![Inhibitor Cocktails](/media/diy/images/page/Inhibitor Cocktails.jpg)
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Radotinib(IY-5511)是Bcl-Abl酪氨酸激酶的新型选择性抑制剂[1].
Bcl-Abl是一种组成型活化的嵌合酪氨酸激酶,在患者慢性粒细胞白血病(CML)中其基因异常表达.
体外实验,radotinib与Bcr-Abl偶联,减少Bcr-Abl靶蛋白CrkL的磷酸化.临床前研究表明,在野生型和突变型BCR-ABL1阳性CML细胞系中,radotinib比伊马替尼有更好的效果[1].
在I期临床试验中,剂量高达1000 mg/day的radotinib没有剂量限制性毒性.II期研究证明,在对Bcr-Abl1酪氨酸激酶抑制剂耐受或不耐受的慢性期慢性粒细胞性白血病患者中,radotinib具有有效性和良好的耐受性[1].
参考文献:
1. Kim SH, Menon H, Jootar S et al. Efficacy and safety of radotinib in chronic phase chronic myeloid leukemia patients with resistance or intolerance to BCR-ABL1 tyrosine kinase inhibitors. Haematologica. 2014 Jul;99(7):1191-6.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 530.5 |
Cas No. | 926037-48-1 |
Formula | C27H21F3N8O |
Solubility | ≥13.73mg/ml in DMSO with warming; insoluble in EtOH; insoluble in H2O |
Chemical Name | (Z)-4-methyl-N-(3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl)-3-((4-(pyrazin-2-yl)pyrimidin-2-yl)amino)benzimidic acid |
SDF | Download SDF |
Canonical SMILES | CC1=C(NC2=NC=CC(C3=CN=CC=N3)=N2)C=C(/C(O)=N/C4=CC(N(C=N5)C=C5C)=CC(C(F)(F)F)=C4)C=C1 |
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。 |
细胞实验[1]: | |
细胞系 |
急性髓细胞白血病病人的骨髓细胞(BMCs) |
溶解方法 |
在DMSO中的溶解度大于26.6 mg/mL。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。 |
反应条件 |
1,10和100 μM,72 h,37 ℃ |
应用 |
Radotinib是BCR-ABL1酪氨酸激酶的抑制剂,已经被批准用作慢性骨髓白血病的二期治疗。在急性髓细胞白血病病人的骨髓细胞(BMCs)中,Radotinib增加酶切 caspase-3、caspase-7和caspase-9的水平,导致凋亡增加。Radotinib也会诱导G0/G1期阻滞,抑制AML病人骨髓细胞的增殖。 |
临床实验[2]: | |
临床样本 |
大于18周岁的对伊马替尼耐药或不耐受的费城染色体阳性慢性粒细胞白血病慢性期患者 |
剂量 |
400 mg,每天两次 |
应用 |
病人对Radotinib的响应与对其他二代酪氨酸激酶抑制剂的响应相当。在对伊马替尼耐药或不耐受的慢性粒细胞白血病慢性期患者中,Radotinib是有效的并且能够很好地被病人耐受。 |
注意事项 |
请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。 |
References: [1]. Heo S K, Noh E K, Gwon G D, et al. Radotinib inhibits acute myeloid leukemia cell proliferation via induction of mitochondrial-dependent apoptosis and CDK inhibitors[J]. European journal of pharmacology, 2016, 789: 280-290. [2]. Kim S H, Menon H, Jootar S, et al. Efficacy and safety of radotinib in chronic phase chronic myeloid leukemia patients with resistance or intolerance to BCR-ABL1 tyrosine kinase inhibitors[J]. Haematologica, 2014: haematol. 2013.096776. |
质量控制和MSDS
- 批次:
化学结构
![Radotinib(IY-5511)](http://www.apexbt.com//media/diy/images/struct/B5846.png)