Taltobulin (Synonyms: HTI-286; SPA-110)
目录号: PL07269 纯度: ≥99%
CAS No. :228266-40-8
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中文名称
Taltobulin
中文别名
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;2-甘油磷酸二钠
英文名称
Taltobulin
英文别名
Taltobulin;N,beta,beta-Trimethyl-L-phenylalanyl-N-[(1S,2E)-3-carboxy-1-(1-methylethyl)-2-butenyl]-N,3-dimethyl-L-valinamide;(E,4S)-4-[[(2S)-3,3-dimethyl-2-[[(2S)-3-methyl-2-(methylamino)-3-phenylbutanoyl]amino]butanoyl]-methylamino]-2,5-dimethylhex-2-enoic acid;HTI-286;TANDUTINIB;HTI286;SPA110;SPA-110
Cas No.
228266-40-8
分子式
C27H43N3O4
分子量
473.65
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Taltobulin (HTI-286) 是一种合成的三肽半胱氨酸类似物,Taltobulin 是一种有效的抗微管剂 (antimicrotubule),可在体内外规避 P-糖蛋白介导的耐药性。Taltobulin 抑制纯化的微管蛋白聚合,破坏细胞中的微管组织,并诱导有丝分裂停滞以及凋亡 (apoptosis)。
生物活性
Taltobulin (HTI-286), a synthetic analogue of the tripeptide hemiasterlin, is a potent antimicrotubule agent that circumvents P-glycoprotein-mediated resistance in vitro and in vivo. Taltobulin inhibits the polymerization of purified tubulin, disrupts microtubule organization in cells, and induces mitotic arrest, as well as apoptosis.
性状
Solid
IC50 & Target[1][2]
Traditional Cytotoxic Agents
体外研究(In Vitro)
Taltobulin (HTI-286; 0.2-7.3 nM; 3 days) inhibits the growth of 18 tumor cell lines (leukemia, ovarian, NSCLC, breast, colon, and melanoma cell lines) with an average IC50 of 2.5±2.1 nM and a median value of 1.7 nM. has not independently confirmed the accuracy of these methods. They are for reference only.Cell Proliferation Assay-tbl">
体内研究(In Vivo)
Taltobulin (HTI-286; 1.6 mg/kg i.v.) inhibits the growth of human tumor xenografts (e.g., HCT-15, DLD-1, MX-1W, and KB-8-5) in athymic nu/nu female mice.
Taltobulin (HTI-286; 3 mg/kg; p.o. gavage) inhibits growth by 97.3 % and 82% in athymic nu/nu female mice with Lox melanoma xenografts and KB-3-1 epidermoid xenograft model, respectively. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Loganzo F, 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 vivo. Cancer Res. 2003 Apr 15;63(8):1838-45.
溶解度数据
In Vitro: DMSO : ≥ 100 mg/mL (211.13 mM)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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