| Identification | Back Directory | [Name]
Suprafenacine | [CAS]
1477482-50-0 | [Synonyms]
Suprafenacine
Suprafenacine >=98% (HPLC)
N'-[(E)-(4-methylphenyl)methylidene]-4
7-tetrahydro-1H-indazole-3-carbohydrazide
N'-[(E)-(4-methylphenyl)methylidene]-4,5,6,7-tetrahydro-1H-indazole-3-carbohydrazide
N-[(E)-(4-methylphenyl)methylideneamino]-4,5,6,7-tetrahydro-1~{H}-indazole-3-carboxamide
1H-Indazole-3-carboxylic acid, 4,5,6,7-tetrahydro-, (2E)-2-[(4-methylphenyl)methylene]hydrazide | [Molecular Formula]
C16H18N4O | [MDL Number]
MFCD01913314 | [MOL File]
1477482-50-0.mol | [Molecular Weight]
282.34 |
| Hazard Information | Back Directory | [Uses]
Suprafenacine is a cell permeable, tubulin-destabilizing molecule which bind microtubules at the colchicine-binding site and inhibit polymerization. Suprafenacine can induce G2/M cell cycle arrest and apoptosis, and can be used for cancer research[1]. | [Biological Activity]
Suprafenacine is an inhibitor of tubulin polymerization (IC50 = 0.38 μM) with anticancer activity.1 It inhibits the proliferation of HeLa, Jurkat, SNU-16, MDA-MB-231, A549, SH-SY5Y, HCT15, and KB-3-1 cells (IC50s = 83-381.2 nM) and P-glycoprotein-enriched KB-VI cells (IC50 = 215.7 nM). Suprafenacine (10 μM) increases phosphorylation of JNK and Bcl-2 and induces apoptosis and cell cycle arrest at the G2/M phase in HeLa cells. Suprafenacine (20 mg/kg) reduces tumor growth in an HCT15 colon adenocarcinoma mouse xenograft model. | [in vivo]
Suprafenacine (20 mg/kg, i.p., every 3 days for 9 days) suppresses 40% of tumor mass in HCT15 tumor bearing SCID mice compared with control mice[1].
| [References]
1.Choi, B.-H., Chattopadhaya, S., Thanh, L.N., et al.Suprafenacine, an indazole-hydrazide agent, targets cancer cells through microtubule destabilizationPLoS One9(10)e110955(2014)
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