Chemical Structure : Lexibulin dihydrochloride
CAS No.:
917111-49-0
Lexibulin dihydrochloride
(CYT-997 dihydrochloride)
Catalog No. : PC-42620Not For Human Use, Lab Use Only.
An orally active tubulin polymerization inhibitor with potent cytotoxic and vascular disrupting activity in vitro and in vivo.
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Purity & Documentation Purity:
>98% (HPLC) Select Batch: PC-4262001
Biological Activity
An orally active tubulin polymerization inhibitor with potent cytotoxic and vascular disrupting activity in vitro and in vivo; inhibits a broad selection of cancer cell lines with IC50 of <100 nM; blocks the cell cycle at the G2-M boundary and increases phosphorylated Bcl-2, expression of cyclin B1; orally bioavailable, and efficacious in a range of in vivo cancer models.
Blood Cancer
Phase 2 Discontinued
Physicochemical Properties
M.Wt
507.4559
Formula
C24H32Cl2N6O2
Appearance
Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility
10 mM in DMSO
Chemical Name/SMILES
Urea, N-ethyl-N'-[2-methoxy-4-[5-methyl-4-[[(1S)-1-(3-pyridinyl)butyl]amino]-2-pyrimidinyl]phenyl]-, hydrochloride (1:2)
References
1. Burns CJ, et al. Mol Cancer Ther. 2009 Nov;8(11):3036-45.
2. Burns CJ, et al. Bioorg Med Chem Lett. 2009 Aug 15;19(16):4639-42.
3. Burns CJ, et al. J Pharmacol Exp Ther. 2011 Dec;339(3):799-806.
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