Allitinib(Synonyms: AST-1306; ALS 1306)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Allitinib (Synonyms: AST-1306; ALS 1306)

Allitinib (AST-1306) 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 抑制 ErbB4,IC50 为 0.8 nM。Allitinib 是一种苯胺基喹唑啉化合物,具有抗癌活性。

Allitinib(Synonyms: AST-1306;  ALS 1306)

Allitinib Chemical Structure

CAS No. : 897383-62-9

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Allitinib 的其他形式现货产品:

Allitinib tosylate

生物活性

Allitinib (AST-1306) is an orally active and irreversible EGFR and ErbB2 inhibitor with IC50s of 0.5 and 3 nM, respectively. Allitinib also inhibits ErbB4 with an IC50 of 0.8 nM. Allitinib is an anilino-quinazoline compound and has anti-cancer activity[1].

IC50 & Target[1]

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 (AST-1306; 0.19-6.25 μM; 72 hours) induces a significant, concentration-dependent inhibition of the growth of HIH3T3-EGFR T790M/L858R cells[1].
AST1306 inhibits the activation of tyrosine kinases and downstream signaling pathways in A549 cells, Calu-3 cells and SK-OV-3 cells. AST1306 dose-dependently and markedly inhibits EGF-induced EGFR phosphorylation in A549 cells[1].
AST1306 (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 (0.001-1.0 μM; 4 hours) is more than 3000-fold selective for ErbB family kinases over other kinase families[1].
AST1306 potently inhibits the EGFR T790M/L858R double mutant, exhibiting an IC50 value of 12 nM[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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 (AST-1306; 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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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

448.88

Formula

C24H18ClFN4O2

CAS 号

897383-62-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

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.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务