1. Cell Cycle/DNA Damage Cytoskeleton Antibody-drug Conjugate/ADC Related Apoptosis
  2. Microtubule/Tubulin ADC Cytotoxin Apoptosis
  3. Taltobulin trifluoroacetate

Taltobulin trifluoroacetate  (Synonyms: HTI-286 trifluoroacetate; SPA-110 trifluoroacetate)

目录号: HY-15584A 纯度: 99.96%
COA 产品使用指南

Taltobulin trifluoroacetate (HTI-286 trifluoroacetate) 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 trifluoroacetate 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)。

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Taltobulin trifluoroacetate Chemical Structure

Taltobulin trifluoroacetate Chemical Structure

CAS No. : 228266-41-9

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥3555
In-stock
5 mg ¥2750
In-stock
10 mg ¥4100
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100 mg   询价  

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Other Forms of Taltobulin trifluoroacetate:

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Top Publications Citing Use of Products
  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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[1].

IC50 & Target

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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

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
(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[1].
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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Athymic nu/nu female mice with Lox melanoma model (5-6 weeks of age)[1]
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.
分子量

587.67

Formula

C29H44F3N3O6

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO 中的溶解度 : ≥ 39 mg/mL (66.36 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7016 mL 8.5082 mL 17.0164 mL
5 mM 0.3403 mL 1.7016 mL 3.4033 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7016 mL 8.5082 mL 17.0164 mL 42.5409 mL
5 mM 0.3403 mL 1.7016 mL 3.4033 mL 8.5082 mL
10 mM 0.1702 mL 0.8508 mL 1.7016 mL 4.2541 mL
15 mM 0.1134 mL 0.5672 mL 1.1344 mL 2.8361 mL
20 mM 0.0851 mL 0.4254 mL 0.8508 mL 2.1270 mL
25 mM 0.0681 mL 0.3403 mL 0.6807 mL 1.7016 mL
30 mM 0.0567 mL 0.2836 mL 0.5672 mL 1.4180 mL
40 mM 0.0425 mL 0.2127 mL 0.4254 mL 1.0635 mL
50 mM 0.0340 mL 0.1702 mL 0.3403 mL 0.8508 mL
60 mM 0.0284 mL 0.1418 mL 0.2836 mL 0.7090 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
Taltobulin trifluoroacetate
目录号:
HY-15584A
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