LP-261

Name: LP-261
CAS#: 915412-67-8
Chemical Formula: C22H19N3O4S
Exact Mass: 421.10963
Molecular Weight: 421.47
Elemental Analysis: C, 62.69; H, 4.54; N, 9.97; O, 15.18; S, 7.61

Description: LP-261 is a novel tubulin targeting anticancer agent that binds at the colchicine site on tubulin, inducing G2/M arrest. Screening in the NCI60 cancer cell lines resulted in a mean GI50 of approximately 100 nM. LP-261 is a very potent inhibitor of angiogenesis, preventing microvessel outgrowth in the rat aortic ring assay and HUVEC cell proliferation at nanomolar concentrations. Complete inhibition of tumor growth was achieved in the PC3 xenograft model and shown to be schedule dependent. Excellent inhibition of tumor growth in the SW620 model was observed, comparable with paclitaxel. Combining oral, low dose LP-261 with bevacizumab led to significantly improved tumor inhibition. Oral LP-261 is very effective at inhibiting tumor growth in multiple mouse xenograft models and is well tolerated. (source: Invest New Drugs. 2012 Feb;30(1):90-7. doi: 10.1007/s10637-010-9520-5. Epub 2010 Sep 7.)

IUPAC/Chemical Name: N-(3-(1H-indol-4-yl)-5-(2-methoxyisonicotinoyl)phenyl)methanesulfonamide

InChi Key: YUVDELGTFILMBB-UHFFFAOYSA-N

InChi Code: InChI=1S/C22H19N3O4S/c1-29-21-13-14(6-8-24-21)22(26)16-10-15(11-17(12-16)25-30(2,27)28)18-4-3-5-20-19(18)7-9-23-20/h3-13,23,25H,1-2H3

SMILES Code: CS(=O)(NC1=CC(C(C2=CC=NC(OC)=C2)=O)=CC(C3=CC=CC4=C3C=CN4)=C1)=O

Appearance: Solid powder