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Taltobulin (trifluoroacetate)

    
≥98%

Taltobulin (trifluoroacetate)

源叶(MedMol)
S84544 一键复制产品信息
228266-41-9
C29H44F3N3O6
587.6714
Taltobulin trifluoroacetate
货号 规格 价格 上海 北京 珠海 重庆 武汉 购买数量
S84544-5mg
≥98%

¥2300.00

货期:3-5天 - - - -
S84544-10mg
≥98%

¥4100.00

货期:3-5天 - - - -
产品介绍 参考文献 质检证书(COA) 摩尔浓度计算器 相关产品
产品描述: Taltobulin trifluoroacetate (HTI-286 trifluoroacetate), a synthetic analogue of the tripeptide hemiasterlin, is a potent antimicrotubule agent that circumvents P-glycoprotein-mediated resistance in vitro and in vivo. Taltobulin trifluoroacetate inhibits the polymerization of purified tubulin, disrupts microtubule organization in cells, and induces mitotic arrest, as well as apoptosis
靶点: Traditional Cytotoxic Agents
体外研究: 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. Cell Proliferation Assay Cell Line: Leukemia CCRF-CEM cell line; ovarian 1A9 cell line; NSCLC A549 and NCI-H1299 cell lines; breast MX-1W and MCF-7 cell lines; colon HCT-116, DLD-1, Colo205, KM20, SW620, S1, HCT-15 and Moser cell lines; melanoma A375, Lox and SK-Mel-2 cell lines Concentration: 0.2-7.3 nM Incubation Time: 3 days Result: Inhibited the growth of tumor cell lines with IC50s of 0.2±0.03 nM (for leukemia CCRF-CEM cell line), 0.6±0.1 nM (for ovarian 1A9 cell line), 1.1±0.5 and 6.8±6.1 nM ( for NSCLC A549 and NCI-H1299 cell lines), 1.8±0.6, 7.3±2.3 nM (for breast MX-1W, MCF-7 cell lines), 0.7±0.2, 1.1±0.4, 1.5±0.6, 1.8±0.6, 3.6±0.8, 3.7±2.0, 4.2±2.5, and 5.3±4.1 nM ( for colon HCT-116, DLD-1, Colo205, KM20, SW620, S1, HCT-15, and Moser cell lines), 1.1±0.8, 1.4±0.6 and 1.7±0.5 nM (for melanoma A375, Lox and SK-Mel-2 cell lines).
体内研究: 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. Animal Model: Athymic nu/nu female mice with Lox melanoma model (5-6 weeks of age) Dosage: 1.6 mg/kg Administration: Administered i.v.;for 35 days Result: Growth of Lox tumors was inhibited by 96-98% on day 12 compared with vehicle-treated controls.Growth of KB-8-5 tumors was inhibited by 84% on day 14 compared with vehicle-treated controls.Growth of MX-1W tumors was inhibited by 97% compared with vehicle-treated controls.Growth of DLD-1 and HCT-15 tumors was inhibited by 80 and 66%, respectively.
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.
溶解性: Soluble  in  DMSO
保存条件: -20℃
配置溶液浓度参考:
1mg 5mg 10mg
1 mM 1.702 ml 8.508 ml 17.016 ml
5 mM 0.34 ml 1.702 ml 3.403 ml
10 mM 0.17 ml 0.851 ml 1.702 ml
50 mM 0.034 ml 0.17 ml 0.34 ml
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参考文献

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摩尔浓度计算器

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