Allitinib tosylate (AST-1306 (

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

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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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[1]

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 IC50 value 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.

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.

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 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 (sealed storage, away from moisture)。-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
 

参考文献	[1]. Xie H, Lin L, Tong L et al. AST1306, a novel irreversible inhibitor of the epidermal growth factor receptor 1 and 2, exhibits antitumor activity both in vitro and in vivo. PLoS One. 2011;6(7):e21487.  [Content Brief]