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TP-5801 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 Chemical Structure

TP-5801 Chemical Structure

CAS No. : 2574474-81-8

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Customer Review

Other Forms of TP-5801:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TP-5801 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) treatment inhibits TNK1-driven, BCR-ABL-driven and IL-3-driven Ba/F3 cell growth[1].
TP-5801 (1 nM-10 μM; 10 d) inhibits TNK1-dependent L540 cell growth[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) treatment shows efficacy in the mouse survival model[1].
TP-5801 (oral gavage; 50 mg/kg; once daily; 7 d) treatment can inhibit localized tumor growth[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 luc 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 luc 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

527.46

Formula

C24H31BrN8O

CAS 号
性状

固体

颜色

Light yellow to green 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 : 16.67 mg/mL (31.60 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 1.8959 mL 9.4794 mL 18.9588 mL
5 mM 0.3792 mL 1.8959 mL 3.7918 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

纯度: 99.69%

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 1.8959 mL 9.4794 mL 18.9588 mL 47.3970 mL
5 mM 0.3792 mL 1.8959 mL 3.7918 mL 9.4794 mL
10 mM 0.1896 mL 0.9479 mL 1.8959 mL 4.7397 mL
15 mM 0.1264 mL 0.6320 mL 1.2639 mL 3.1598 mL
20 mM 0.0948 mL 0.4740 mL 0.9479 mL 2.3698 mL
25 mM 0.0758 mL 0.3792 mL 0.7584 mL 1.8959 mL
30 mM 0.0632 mL 0.3160 mL 0.6320 mL 1.5799 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
目录号:
HY-147316
需求量: