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。
| 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) |
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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. |
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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. |
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| 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 | 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℃, 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。 *以上所有助溶剂都可在本网站选购。
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