Avanbulin

Research use only, not for human use.

Avanbulin (BAL27862, BAL-27862) is a novel microtubule-destabilizing agent that potently inhibits tubulin assembly at 37°C with IC50 of 1.4 uM in tubulin-binding assays.

Avanbulin (BAL27862, BAL-27862) is a novel microtubule-destabilizing agent that potently inhibits tubulin assembly at 37°C with IC50 of 1.4 uM in tubulin-binding assays; potentli bindis to unassembled tubulin with a stoichiometry of 1 mol/mol tubulin and a dissociation constant of 244±30 nM, BAL27862 bound to tubulin independently of vinblastine, without the formation of tubulin oligomers; inhibits tumor cell proliferation through activation of the spindle assembly checkpoint, inhibits EB1-dependent migration and invasion and promotes differentiation of glioblastoma stem-like cells both in vitro and in vivo.

Avanbulin (0-4 μM) binds to tubulin in the site as Colchicine with an apparent Kd value of 244 nM..Avanbulin (50 μM; 0, 10, 20, 30, 60 min) induces the proteolysis of tubulin.Avanbulin (33 nM; 0, 10, 20, 30, 60 min; HeLa-tubGFP cells) collapses the mitotic spindle and forms the tiny tubulin aggregates.Avanbulin does not induce the formation of tubulin oligomers.Avanbulin induces growth inhibition of 23 tumor cell lines with a median relative IC50 of 13.8 nM (96 hours) .Avanbulin (6 nM and 20 nM) inhibits the migration of GBM6 and GBM9 cells.Avanbulin (6 nM and 20 nM; GBM6-shEB1 and GBM6-sh0 cells) triggers astrocytic differentiation of GBM6 in an EB1-dependent manner.Avanbulin (12? nM; 4? h) reduces kinetochore-microtubule (KT–MT) occupancy of MG132(10 μM; 2h) treated hTert-RPE1 eGFP-α-tubulin cells.Avanbulin (12 ?nM; 4 ?h) reduces average inter-KT distances of cells, shows intact spindle morphology, and lacks obvious chromosome alignment defects. Cell Cytotoxicity Assay Cell Line:23 cell lines, including RD, TC-71, SJ-GBM2, NB-1643.Concentration:0.1 nM-1.0 μM Incubation Time:96 hours Result:Induced growth inhibition of cells with a median relative IC50 of 13.8 nM.

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BAL27862 | BAL-27862

Cytoskeleton/Cell Adhesion Molecules

Microtubule/Tubulin

Microtubule/Tubulin

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798577-91-0

387.403

C20H17N7O2

>98% (HPLC)

In Vitro:?DMSO : 250 mg/mL (645.34 mM)

N#CCCNC1=NON=C1C2=NC3=CC=CC=C3N2CC(C4=CC=C(N)C=C4)=O

3-[(4-{1-[2-(4-aminophenyl)-2-oxoethyl]-1H-benzimidazol-2-yl}-1,2,5-oxadiazol-3-yl)amino]propanenitrile

(-20℃)

With Ice Pack

≥ 2 years