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Radotinib

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Chemical Structure| 926037-48-1 同义名 : 雷度替尼 ;IY-5511
CAS号 : 926037-48-1
货号 : A231107
分子式 : C27H21F3N8O
纯度 : 98+%
分子量 : 530.504
MDL号 : MFCD27956910
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 5 mg/mL(9.43 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
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]. Radotinib, a novel and selective BCR-ABL1 tyrosine kinase inhibitor with IC50 of 34 nM, is used for the treatment of CML[6]. Cell viability of K562 (a representative CML cell line) cells was significantly reduced even at the lowest concentration of radotinib (12.5 μM), indicating that radotinib kills K562 cells directly. The purified NK cells were incubated with various doses (0, 12.5, 25, 50, 100, and 200 μM) of radotinib. NK cell cytotoxicity was markedly upregulated upon radotinib treatment indicating radotinib could be used as an effective and strong therapeutic to treat solid tumors via upregulation of NK cell cytotoxicity[7].
实验方案
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
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.