Taltobulin (HTI-286)

An inhibitor of microtubule polymerization

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5mg

￥2475.00

1980.00

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10mg

￥3850.00

3080.00

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50mg

￥11762.00

9410.00

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货号: ajce49748
CAS: 228266-40-8
别名: N,BETA,BETA-三甲基-L-苯基丙氨酰基-N-[(1S,2E)-3-羧基-1-(1-甲基乙基)-2-丁烯基]-N,3-二甲基-L-缬氨酰胺,HTI-286; SPA-110
分子式: C27H43N3O4
分子量: 473.65
纯度: >98%
溶解度: DMSO : ≥ 100 mg/mL (211.13 mM)
储存: Store at -20°C
库存: 现货

Background

HTI 286 is an inhibitor of microtubule polymerization.^1,2 It binds to (K_d = 260 nM) and inhibits the polymerization of tubulin in a cell-free assay when used at concentrations of 0.1 and 1 ?M. HTI 286 (30 nM) induces cell cycle arrest at the G₂/M phase and apoptosis in KB-3-1 epidermoid carcinoma cells.² It inhibits cell growth in a panel of 18 tumor cell lines, including HCT-15 and DLD-1 colon cancer cells, which overexpress P-glycoprotein (mean IC₅₀ = 2.5 nM). HTI 286 (1.6 mg/kg) reduces tumor volume in LOX, KB-3-1, KB-8-5, MX-1, DLD-1, and HCT-15 mouse xenograft models.

1.Krishnamurthy, G., Cheng, W., Lo, M.-C., et al.Biophysical characterization of the interactions of HTI-286 with tubulin heterodimer and microtubulesBiochemistry42(46)13484-13495(2003) 2.Loganzo, F., Discafani, C.M., Annable, T., et al.HTI-286, a synthetic analogue of the tripeptide hemiasterlin, is a potent antimicrotubule agent that circumvents P-glycoprotein-mediated resistance in vitro and in vivoCancer Res.63(8)1838-1845(2003)