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  3. TP-5801 TFA

TP-5801 TFA 是一种具有口服活性的非受体酪氨酸激酶 (TNK1) 抑制剂 (IC50=1.40 nM),并表现出抗肿瘤活性。

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TP-5801 TFA Chemical Structure

TP-5801 TFA Chemical Structure

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5 mg ¥5000
In-stock
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Customer Review

Other Forms of TP-5801 TFA:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TP-5801 TFA is an orally active TNK1 (non-receptor tyrosine kinase) inhibitor (IC50=1.40 nM), and shows anti-tumor activity[1].

IC50 & Target

IC50: 1.40 nM (TNK1)[1]

体外研究
(In Vitro)

TP-5801 (10 pM-10 μM; 72 h) TFA 处理抑制 TNK1 驱动、BCR-ABL 驱动和 IL-3 驱动的 Ba/F3 细胞生长[1]
TP-5801 (1 nM-10 μM; 10 d) TFA 抑制 TNK1 依赖性 L540 细胞生长[1]

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

Cell Viability Assay[1]

Cell Line: Ba/F3 cells
Concentration: 10 pM-10 μM
Incubation Time: 72 hours
Result: Inhibited TNK1-driven cell growth with IC50s of 76.78 and 36.95 nM against WT TNK1 and AAA mutant cells, respectively. Inhibited BCR-ABL-driven and IL-3-driven Ba/F3 cell growth with IC50s of 8.5 and 1.2 μM, respectively.

Cell Viability Assay[1]

Cell Line: L540 cells
Concentration: 1, 10, 100, and 1000 nM
Incubation Time: 10 days
Result: Inhibited TNK1-dependent L540 cell growth at low nM level.
体内研究
(In Vivo)

TP-5801 (oral gavage; 10 mg/kg; once) TFA 在小鼠肿瘤存活模型中有效果[1]
TP-5801 (oral gavage; 50 mg/kg; once daily; 7 d) TFA 可抑制局部肿瘤生长[1]

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

Animal Model: Female NOD/SCID mice injected with Ba/F3 luciferase cells expressing TNK1 AAA[1]
Dosage: 10 mg/kg
Administration: Oral gavage; 10 mg/kg; once
Result: Showed no signs of toxicity and significantly prolonged lifespan.
Animal Model: NOD/SCID mice implanted subcutaneously with Ba/F3 luciferase cells expressing TNK1 AAA or BCR-ABL[1]
Dosage: 50 mg/kg
Administration: Oral gavage; 50 mg/kg; once daily; 7 days
Result: Reduced phospho-STAT3 in TNK1-driven xenografts at 2 hours post-treatment, and tumor burden in mice xenografted.
分子量

641.48

Formula

C26H32BrF3N8O3

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, sealed storage, away from moisture and light

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

溶解性数据
细胞实验: 

DMSO 中的溶解度 : 100 mg/mL (155.89 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 1.5589 mL 7.7945 mL 15.5890 mL
5 mM 0.3118 mL 1.5589 mL 3.1178 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 and 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

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 and 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 1.5589 mL 7.7945 mL 15.5890 mL 38.9724 mL
5 mM 0.3118 mL 1.5589 mL 3.1178 mL 7.7945 mL
10 mM 0.1559 mL 0.7794 mL 1.5589 mL 3.8972 mL
15 mM 0.1039 mL 0.5196 mL 1.0393 mL 2.5982 mL
20 mM 0.0779 mL 0.3897 mL 0.7794 mL 1.9486 mL
25 mM 0.0624 mL 0.3118 mL 0.6236 mL 1.5589 mL
30 mM 0.0520 mL 0.2598 mL 0.5196 mL 1.2991 mL
40 mM 0.0390 mL 0.1949 mL 0.3897 mL 0.9743 mL
50 mM 0.0312 mL 0.1559 mL 0.3118 mL 0.7794 mL
60 mM 0.0260 mL 0.1299 mL 0.2598 mL 0.6495 mL
80 mM 0.0195 mL 0.0974 mL 0.1949 mL 0.4872 mL
100 mM 0.0156 mL 0.0779 mL 0.1559 mL 0.3897 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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Inquiry Information

产品名称:
TP-5801 TFA
目录号:
HY-147316A
需求量: