拉多替尼 /Radotinib
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货号：A231107
同义名：
雷度替尼
/ IY-5511
Radotinib is a selective BCR-ABL1 inhibitor with IC50 of 34 nM, also inhibits platelet-derived growth factor receptor (PDGFR), is used to treat cancers and Chronic Myeloid Leukemia.
Radotinib 化学结构
Radotinib 3D分子结构
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会员价
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Radotinib 纯度/质量文件 产品仅供科研
货号：A231107
标准纯度：
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产品说明书
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Radotinib 质控信息
转化生长因子-β 亚型比较
Bcr-Abl 亚型比较
NVP-BHG 712
+
99%+
KW-2449
+++
Abl, IC50: 14 nM
Abl (T315I), IC50: 4 nM
FLT3
99%+
Ponatinib
++++
98%
AT9283
99%+
Imatinib Mesylate
+
c-Kit,PDGFR
99%
Danusertib
++
RET
99%+
Rebastinib
++++
p-Abl1 (native), IC50: 0.75 nM
u-Abl1 (T315I), IC50: 5 nM
FLT3,Tie-2
99%+
PP121
++
PDGFR,VEGFR
99%+
GNF-7
+++
M351T, IC50: 133 nM
E255V, IC50: 122 nM
99%+
Olverembatinib dimesylate
++++
Abl, IC50: 0.34 nM
Abl (G250E), IC50: 0.35 nM
99%
Dasatinib monohydrate
++++
Src
98%
Dasatinib
++++
Src
98%
Bafetinib
+++
98+%
GNF-2
+
Bcr-Abl (SUP-B15 cell line), IC50: 268 nM
Bcr-Abl (K562 cell line), IC50: 273 nM
98%+
Degrasyn
+
DUB
98+%
GNF-5
++
98%
Radotinib
++
98+%
PD173955
Src
99%+
Nilotinib
++
98%
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1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。
Radotinib 生物活性
靶点
Bcr-Abl
BCR-ABL1, IC50:34 nM
描述
The BCR-ABL1 oncogene is a fusion protein that results from transposition of a segment of the c-ABL1 gene from chromosome 9q34 onto the BCR gene on chromosome 22q11. It encodes a cytoplasmic protein tyrosine kinase with elevated and dysregulated enzymatic activity that plays a vital role in the pathogenesis and progression of chronic myeloid leukemia (CML)[5] 50 of 34 nM, is used for the treatment of CML[6] [7]
Radotinib 动物研究
Dose
Mice: 10 mg/kg, 20 mg/kg[3] [4]
Administration
i.p., p.o.
Pharmacokinetics
Animal
Mice[4]
Dose
30 mg/kg
Administration
p.o.
Cmax
10082.9 ng/ml
AUCt
87081.4 ng·h/ml
Radotinib 参考文献
[1] Heo SK, Noh EK, et al. Radotinib Induces Apoptosis of CD11b+ Cells Differentiated from Acute Myeloid Leukemia Cells. PLoS One. 2015 Jun 12;10(6):e0129853.
[2] Kim SH, Menon H, 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.
[3] Heo SK, Noh EK, et al. Radotinib inhibits mitosis entry in acute myeloid leukemia cells via suppression of Aurora kinase A expression. Tumour Biol. 2019 May;41(5):1010428319848612.
[4] Lee S, Kim S, et al. The c-Abl inhibitor, Radotinib HCl, is neuroprotective in a preclinical Parkinson's disease mouse model. Hum Mol Genet. 2018 Jul 1;27(13):2344-2356.
[5] Tsubaki M, Takeda T, Kino T, Sakai K, Itoh T, Imano M, Nakayama T, Nishio K, Satou T, Nishida S. Contributions of MET activation to BCR-ABL1 tyrosine kinase inhibitor resistance in chronic myeloid leukemia cells. Oncotarget. 2017 Jun 13;8(24):38717-38730. doi: 10.18632/oncotarget.16314. PMID: 28418880; PMCID: PMC5503566.
[6] Kim SH, Menon H, Jootar S, Saikia T, Kwak JY, Sohn SK, Park JS, Jeong SH, Kim HJ, Kim YK, Oh SJ, Kim H, Zang DY, Chung JS, Shin HJ, Do YR, Kim JA, Kim DY, Choi CW, Park S, Park HL, Lee GY, Cho DJ, Shin JS, Kim DW. 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. doi: 10.3324/haematol.2013.096776. Epub 2014 Apr 4. PMID: 24705186; PMCID: PMC4077080.
[7] Kim KE, Park S, Cheon S, Kim DY, Cho DJ, Park JM, Hur DY, Park HJ, Cho D. Novel Application of Radotinib for the Treatment of Solid Tumors via Natural Killer Cell Activation. J Immunol Res. 2018 Dec 31;2018:9580561. doi: 10.1155/2018/9580561. PMID: 30687767; PMCID: PMC6330826.
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Radotinib 实验方案
计算器
摩尔计算器
总药量计算器
工作液计算器
存储液制备
1mg
5mg
10mg
1 mM
5 mM
10 mM
1.88mL
0.38mL
0.19mL
9.42mL
1.88mL
0.94mL
18.85mL
3.77mL
1.88mL
Radotinib 技术信息
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