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  4. PROTAC TTK degrader-1

PROTAC TTK degrader-1 

目录号: HY-143904 纯度: 98.01%
COA 产品使用指南

摩尔计算器

PROTAC TTK degrader-1 是一种有效的 TTK (苏氨酸酪氨酸激酶) PROTAC 降解剂，在 COLO-205 和 HCT-116 细胞中的 DC50 值分别为 1.7 和 5.8 nM。PROTAC TTK degrader-1 在 COLO-205 人结直肠癌细胞异种移植小鼠模型中显示出靶向降解和抗癌效果。

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PROTAC TTK degrader-1 Chemical Structure

PROTAC TTK degrader-1 Chemical Structure

CAS No. : 2953426-43-0

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥16873
In-stock
1 mg ￥3584
In-stock
5 mg ￥8960
In-stock
10 mg   询价  
50 mg   询价  

* Please select Quantity before adding items.

Customer Review

PROTAC TTK degrader-1 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC TTK degrader-1 is a potent TTK (threonine tyrosine kinase) PROTAC degrader, with DC50 values of 1.7 and 5.8 nM in COLO-205 and HCT-116 cell, respectively. PROTAC TTK degrader-1 exhibits target degradation and anticancer efficacy in a xenograft mouse model of COLO-205 human colorectal cancer cells[1].

IC50 & Target

DC50: 1.7 nM (TTK) in COLO-205, 5.8 nM (TTK) in HCT-116[1]
体外研究
(In Vitro)

PROTAC TTK degrader-1 (compound 8e) (0-10 μM, 96 h) inhibits cancer cell proliferation[1].
PROTAC TTK degrader-1 (5 and 50 nM, 6 h) induces degradation of TTK protein in a dose-dependent manner[1].

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

PROTAC TTK degrader-1 相关抗体:

Cell Proliferation Assay

Cell Line: COLO-205 and HCT-116 cells[1]
Concentration: 0-10 μM
Incubation Time: 96 h
Result: Inhibited the growth of COLO-205 cancer cells with an IC50 of 0.1 μM.

Western Blot Analysis

Cell Line: COLO-205, HCT-116 LOVO, HCT-8, and HCT-29 human colon cancer cell lines[1]
Concentration: 5, 50 nM
Incubation Time: 6 h
Result: Induced degradation of TTK protein in a dose-dependent manner.
体内研究
(In Vivo)

PROTAC TTK degrader-1 (10 mg/kg, IP, single) demonstrates reasonable pharmacokinetics profiles[1].
PROTAC TTK degrader-1 (10, 20 mg/kg, IP, once daily for 16 days) significantly reduces the TTK protein levels, and exhibits tumor-growth inhibition[1].
Pharmacokinetic Parameters of PROTAC TTK degrader-1 in male SD rats[1].

8e
AUC (ng/mL*h) 2235
T1/2 (h) 4.3

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

Animal Model: Male SD rats[1]
Dosage: 10 mg/kg, dissolved in mixed solvents (5% 20 mg/mL DMSO stock, 30% PG, 30% PEG400, and 35% Saline)
Administration: IP, single (Pharmacokinetic Analysis)
Result: Demonstrated reasonable pharmacokinetics profiles.
Animal Model: Male CB17-SCID mice (bearing COLO-205 tumor xenografts)[1]
Dosage: 10, 20 mg/kg
Administration: IP, once daily for 16 days
Result: Significantly reduced the TTK protein levels in animal tumor tissues, exhibited tumor-growth inhibition value of 46.0% upon 20 mg/kg dosing, did not cause a significant body weight loss of the animal.
分子量

855.98

Formula

C47H53N9O7
CAS 号
性状

固体

颜色

Light yellow to yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro: 

DMSO 中的溶解度 : 100 mg/mL (116.83 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.1683 mL 5.8413 mL 11.6825 mL
5 mM 0.2337 mL 1.1683 mL 2.3365 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 (protect from light)。-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

只
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

PROTAC TTK degrader-1 相关分类

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 (protect from light)。-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 1.1683 mL 5.8413 mL 11.6825 mL 29.2063 mL
5 mM 0.2337 mL 1.1683 mL 2.3365 mL 5.8413 mL
10 mM 0.1168 mL 0.5841 mL 1.1683 mL 2.9206 mL
15 mM 0.0779 mL 0.3894 mL 0.7788 mL 1.9471 mL
20 mM 0.0584 mL 0.2921 mL 0.5841 mL 1.4603 mL
25 mM 0.0467 mL 0.2337 mL 0.4673 mL 1.1683 mL
30 mM 0.0389 mL 0.1947 mL 0.3894 mL 0.9735 mL
40 mM 0.0292 mL 0.1460 mL 0.2921 mL 0.7302 mL
50 mM 0.0234 mL 0.1168 mL 0.2337 mL 0.5841 mL
60 mM 0.0195 mL 0.0974 mL 0.1947 mL 0.4868 mL
80 mM 0.0146 mL 0.0730 mL 0.1460 mL 0.3651 mL
100 mM 0.0117 mL 0.0584 mL 0.1168 mL 0.2921 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.

Keywords:

PROTAC TTK degrader-12953426-43-0PROTAC TTK degrader1PROTAC TTK degrader 1PROTACsCOLO-205 cancer cellsHuman colorectal cancerPharmacokinetics propertiesAnticancerInhibitorinhibitorinhibit

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