592543-24-3
Chemical Structure
ON012380
- CAS No.: 592543-24-3
- Formula:C22H27NO8S
- Molecular Weight:465.52
IUPAC Name: (E)-(2-methoxy-5-(((2,4,6-trimethoxystyryl)sulfonyl)methyl)phenyl)-L-alanine
InChIKey: KLFKGEAXNPYTKB-VFNNOXKTSA-N
SMILES: C(=C/S(CC1=CC(N[C@H](C(O)=O)C)=C(OC)C=C1)(=O)=O)\C2=C(OC)C=C(OC)C=C2OC
Biological Activity: ON012380 is a kinase inhibitor with an IC50 of 9 nM against BCR-ABL. As a substrate-competitive BCR-ABL inhibitor, ON012380 binds to a non-ATP site, and inhibits the kinase activities of PDGFR, Fyn and LynB at higher concentrations. ON012380 induces apoptosis, inhibits STAT-5 phosphorylation, reduces cell viability and suppresses cell growth in leukemia cells. ON012380 can be used in the research of chronic myeloid leukemia and Imatinib (HY-15463)-resistant chronic myeloid leukemia[1][2][3][4].
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ON012380 | ON012380 is a kinase inhibitor with an IC50 of 9 nM against BCR-ABL. As a substrate-competitive BCR-ABL inhibitor, ON012380 binds to a non-ATP site, and inhibits the kinase activities of PDGFR, Fyn and LynB at higher concentrations. ON012380 induces apoptosis, inhibits STAT-5 phosphorylation, reduces cell viability and suppresses cell growth in leukemia cells. ON012380 can be used in the research of chronic myeloid leukemia and Imatinib (HY-15463)-resistant chronic myeloid leukemia. | |||||||||||||||||||||
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References
- [1]. Gumireddy K, et al. A non-ATP-competitive inhibitor of BCR-ABL overrides imatinib resistance. Proceedings of the National Academy of Sciences of the United States of America. 2005 Feb 08;102(6):1992-7. [Content Brief]
- [2]. Maekawa T, et al. The Bcr-Abl tyrosine kinase inhibitor imatinib and promising new agents against Philadelphia chromosome-positive leukemias. Int J Clin Oncol. 2007 Oct;12(5):327-40.
- [3]. Kirkland LO, et al. Non-ATP competitive protein kinase inhibitors as anti-tumor therapeutics. Biochemical pharmacology. 2009 May 15;77(10):1561-71.
- [4]. Wu J, et al. ON012380, a putative BCR-ABL kinase inhibitor with a unique mechanism of action in imatinib-resistant cells. Leukemia. 2010 Apr;24(4):869-72.
