Allitinib tosylate - CAS:1050500-29-2

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Allitinib tosylate (Synonyms:艾力替尼; AST-1306 (TsOH))

目录号 : KM7655 CAS No. : 1050500-29-2 纯度 : 98%

Data Sheet 产品使用指南

Allitinib tosylate (AST-1306 (TsOH)) 是一种具有口服活性且不可逆的 EGFR 和 ErbB2 抑制剂IC₅₀ 分别为 0.5 和 3 nM。Allitinib tosylate 抑制 ErbB4，IC₅₀ 为 0.8 nM。Allitinib tosylate 是一种苯胺基喹唑啉化合物，具有抗癌活性。

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5mg		In-stock
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50mg		In-stock
100mg	询价	In-stock
200mg	询价	In-stock

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生物活性

Allitinib tosylate (AST-1306 (TsOH)) is an orally active and irreversible EGFR and ErbB2 inhibitor with IC₅₀s of 0.5 and 3 nM, respectively. Allitinib tosylate also inhibits ErbB4 with an IC₅₀ of 0.8 nM. Allitinib tosylate is an anilino-quinazoline compound and has anti-cancer activity

体外研究

AST1306 tosylate (AST-1306 (TsOH); 0.19-6.25 μM; 72 hours) induces a significant, concentration-dependent inhibition of the growth of HIH3T3-EGFR T790M/L858R cells.
AST1306 tosylate inhibits the activation of tyrosine kinases and downstream signaling pathways in A549 cells, Calu-3 cells and SK-OV-3 cells. AST1306 tosylate dose-dependently and markedly inhibits EGF-induced EGFR phosphorylation in A549 cells.
AST1306 tosylate (0.1, 0.5, 1.0, 5.0 μM) can dramatically inhibit the growth of both tumor cells on soft agar, and SK-OV-3 cells exhibited much more sensitivity than that of A549 cells.
AST1306 tosylate (0.001-1.0 μM; 4 hours) is more than 3000-fold selective for ErbB family kinases over other kinase families.
AST1306 tosylate potently inhibits the EGFR T790M/L858R double mutant, exhibiting an IC₅₀ value of 12±2 nmol/L.

Cell Proliferation Assay

Cell Line:	NIH3T3 parental cells and NIH3T3 cells
Concentration:	0.19, 0.39, 0.78, 1.56, 3.13, 6.25 μM
Incubation Time:	72 hours
Result:	Induced a significant, concentration-dependent inhibition of the growth of HIH3T3-EGFR T790M/L858R cells.

Western Blot Analysis

Cell Line:	A549 cells , Calu-3 cells and SK-OV-3 cells
Concentration:	0.001, 0.01, 0.1, 1.0 μM
Incubation Time:	4 hours
Result:	Inhibits the activation of tyrosine kinases and downstream signaling pathways.

体内研究

AST1306 tosylate (AST-1306 (TsOH); p.o.; 25-100 mg/kg; twice daily; for 28 days) causes a dramatic suppression of tumor growth in SK-OV-3 and Calu-3 xenograft models.

Animal Model:	Nude mice with SK-OV-3 and Calu-3 tumors
Dosage:	25, 50, 100 mg/kg
Administration:	p.o.; twice daily; for 28 days
Result:	Caused a dramatic suppression of tumor growth.

分子式

C₂₄H₁₈N₄O₂FCl^.C₉H₁₂Os

分子量

621.08

CAS号

1050500-29-2

中文名称

艾力替尼

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 50 mg/mL (80.50 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.6101 mL	8.0505 mL	16.1010 mL
5 mM	0.3220 mL	1.6101 mL	3.2202 mL
10 mM	0.1610 mL	0.8050 mL	1.6101 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。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (4.03 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.03 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

临床试验

纯度： 98%

Data Sheet

产品使用指南

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

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

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