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Allitinib tosylate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Allitinib tosylate图片
CAS NO:1050500-29-2
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
艾力替尼
AST-1306 (TsOH)
产品介绍
Allitinib tosylate (AST-1306 (TsOH)) 是一种具有口服活性且不可逆的EGFRErbB2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。
生物活性

Allitinib tosylate (AST-1306 (TsOH)) is an orally active and irreversibleEGFRandErbB2inhibitor withIC50s of 0.5 and 3 nM, respectively. Allitinib tosylate also inhibitsErbB4with an IC50of 0.8 nM. Allitinib tosylate is an anilino-quinazoline compound and has anti-cancer activity[1]

IC50& Target

EGFR

0.5 nM (IC50)

ErbB2

3 nM (IC50)

EGFRL858R/T790M

12 nM (IC50)

ErbB4

0.8 nM (IC50)

体外研究
(In Vitro)

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[1].
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[1].
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[1].
AST1306 tosylate (0.001-1.0 μM; 4 hours) is more than 3000-fold selective for ErbB family kinases over other kinase families[1].
AST1306 tosylate potently inhibits the EGFR T790M/L858R double mutant, exhibiting an IC50value of 12±2 nmol/L[1].

Cell Proliferation Assay[1]

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[1]

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
(In Vivo)

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[1].

Animal Model:Nude mice with SK-OV-3 and Calu-3 tumors[1]
Dosage:25, 50, 100 mg/kg
Administration:p.o.; twice daily; for 28 days
Result:Caused a dramatic suppression of tumor growth.
Clinical Trial
分子量

621.08

性状

Solid

Formula

C31H26ClFN4O5S

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

4°C, sealed storage, away from moisture

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

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 mg5 mg10 mg
1 mM1.6101 mL8.0505 mL16.1010 mL
5 mM0.3220 mL1.6101 mL3.2202 mL
10 mM0.1610 mL0.8050 mL1.6101 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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 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。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
*以上所有助溶剂都可在本网站选购。