TP-5801|cas:2574474-81-8|西域试剂

TP-5801,98.36%

产品编号：Bellancom-147316| CAS NO：2574474-81-8| 分子式：C₂₄H₃₁BrN₈O| 分子量：527.46

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-147316		￥5000.00	杭州北京（现货）
Bellancom-147316		￥8500.00	杭州北京（现货）

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TP-5801

产品介绍

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。

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.

体外研究

TP-5801 (10 pM-10 μM; 72 h) treatment inhibits TNK1-driven, BCR-ABL-driven and IL-3-driven Ba/F3 cell growth.
TP-5801 (1 nM-10 μM; 10 d) inhibits TNK1-dependent L540 cell growth.

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

Cell Viability Assay

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

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.
TP-5801 (oral gavage; 50 mg/kg; once daily; 7 d) treatment can inhibit localized tumor growth.

西域 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
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
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.

体内研究

TP-5801 (oral gavage; 10 mg/kg; once) treatment shows efficacy in the mouse survival model.
TP-5801 (oral gavage; 50 mg/kg; once daily; 7 d) treatment can inhibit localized tumor growth.

西域 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
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
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.

体内研究

TP-5801 (oral gavage; 10 mg/kg; once) treatment shows efficacy in the mouse survival model.
TP-5801 (oral gavage; 50 mg/kg; once daily; 7 d) treatment can inhibit localized tumor growth.

西域 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
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
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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 16.67 mg/mL (31.60 mM; Need ultrasonic)

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
10 mM	0.1896 mL	0.9479 mL	1.8959 mL

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。

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)

参考文献