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Lexibulin dihydrochloride

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:

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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