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Chemical Structure| 926037-48-1 Chemical Structure| 926037-48-1

Structure of Radotinib
CAS No.: 926037-48-1

Chemical Structure| 926037-48-1

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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.

Synonyms: IY-5511

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Product Details of Radotinib

CAS No. :926037-48-1
Formula : C27H21F3N8O
M.W : 530.50
SMILES Code : O=C(NC1=CC(C(F)(F)F)=CC(N2C=C(C)N=C2)=C1)C3=CC=C(C)C(NC4=NC=CC(C5=NC=CN=C5)=N4)=C3
Synonyms :
IY-5511
MDL No. :MFCD27956910
InChI Key :DUPWHXBITIZIKZ-UHFFFAOYSA-N
Pubchem ID :16063245

Safety of Radotinib

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of Radotinib

RTK

Isoform Comparison

Biological Activity

Target
  • Bcr-Abl

    BCR-ABL1, IC50:34 nM

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01602952 Leukemia|Leukemia, Myeloid|Leu... More >>kemia, Myelogenous, Chronic, BCR-ABL Positive|Philadelphia Chromosome|Hematologic Diseases Less << PHASE1|PHASE2 COMPLETED 2018-07-13 Local institution, Mumbai, Mah... More >>arashtra, 741-234, India|Local institution, Mumbai, Mazagaon, 512-364, India|Local institution, Daegu, Buk-gu, 511-230, Korea, Republic of|Local institution, Jeonju, Deokjin-gu, 212-789, Korea, Republic of|Local institution, Ulsan, Dong-gu, 411-978, Korea, Republic of|Local institution, Anyang-si, Dongan-gu, 751-231, Korea, Republic of|Local institution, Hwasun, Hwasun-eup, 322-511, Korea, Republic of|Local institution, Seoul, Jongro-ku, 231-855, Korea, Republic of|Local institution, Busan, Seo-gu, 400-321, Korea, Republic of|Seoul St. Mary's hospital, Seoul, Seocho-gu, Korea, Republic of|Local institution, Suwon, Yeongtong-gu, 781-512, Korea, Republic of|Local institution, Bangkok, Phyathai, 215-714, Thailand Less <<
NCT02422719 Chronic Myeloid Leukemia PHASE2 UNKNOWN 2025-03-19 Ulsan University Hospital, Uls... More >>an, 682714, Korea, Republic of Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.89mL

0.38mL

0.19mL

9.43mL

1.89mL

0.94mL

18.85mL

3.77mL

1.89mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

[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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