917111-49-0
Chemical Structure
Lexibulin dihydrochloride
Synonym(s): CYT-997 dihydrochloride
- CAS No.: 917111-49-0
- Formula:C24H32Cl2N6O2
- Molecular Weight:507.46
IUPAC Name: (S)-1-ethyl-3-(2-methoxy-4-(5-methyl-4-((1-(pyridin-3-yl)butyl)amino)pyrimidin-2-yl)phenyl)urea dihydrochloride
InChIKey: HGDCRTLMRFHNOZ-TXEPZDRESA-N
SMILES: CCC[C@H](NC1=C(C)C=NC(C2=CC=C(NC(NCC)=O)C(OC)=C2)=N1)C3=CN=CC=C3.[H]Cl.[H]Cl
Biological Activity: Lexibulin dihydrochloride (CYT-997 dihydrochloride) is a potent and orally active tubulin polymerisation inhibitor with IC50s of 10-100 nM in cancer cell lines; with potent cytotoxic and vascular disrupting activity in vitro and in vivo[1][2]. Lexibulin dihydrochloride induces cell apoptosis and induces mitochondrial ROS generation in GC cells[3].
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Lexibulin dihydrochloride | Lexibulin dihydrochloride (CYT-997 dihydrochloride) is a potent and orally active tubulin polymerisation inhibitor with IC50s of 10-100 nM in cancer cell lines; with potent cytotoxic and vascular disrupting activity in vitro and in vivo. Lexibulin dihydrochloride induces cell apoptosis and induces mitochondrial ROS generation in GC cells. | |||||||||||||||||||||
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References
- [1]. Burns CJ, et al. CYT997: a novel orally active tubulin polymerization inhibitor with potent cytotoxic and vascular disrupting activity in vitro and in vivo. Mol Cancer Ther. 2009 Nov;8(11):3036-45. [Content Brief]
- [2]. Monaghan K, et al. CYT997 causes apoptosis in human multiple myeloma. Invest New Drugs. 2011 Apr;29(2):232-8. [Content Brief]
- [3]. Ya Cao, wt al. Mitochondrial ROS Accumulation Inhibiting JAK2/STAT3 Pathway Is a Critical Modulator of CYT997-induced Autophagy and Apoptosis in Gastric Cancer. J Exp Clin Cancer Res. 2020 Jun 23;39(1):119. [Content Brief]
