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Anlotinib Dihydrochloride
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。
Anlotinib Dihydrochloride图片
CAS NO:1360460-82-7
规格:≥98%
包装与价格:
包装价格(元)
1mg电议
2mg电议
5mg电议
10mg电议
25mg电议
50mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW) 480.36
FormulaC23H24Cl2FN3O3
CAS No.1360460-82-7 (di-HCl); 1058156-90-3 (free base)
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: ≥ 60 mg/mL
Water:
Ethanol:
Chemical Name 1-(((4-((4-fluoro-2-methyl-1H-indol-5-yl)oxy)-6-methoxyquinolin-7-yl)oxy)methyl)cyclopropan-1-amine dihydrochloride
Synonyms AL3818 dihydrochloride; AL-3818 dihydrochloride; AL 3818 dihydrochloride; Anlotinib HCl;
SMILES CodeNC1(COC2=C(OC)C=C3C(OC4=C(F)C5=C(NC(C)=C5)C=C4)=CC=NC3=C2)CC1.[H]Cl.[H]Cl
实验参考方法
In Vitro

In vitro activity: Anlotinib (formerly known as AL3818) is a novel and potent multi-kinase inhibitor that inhibits VEGFR2/3, FGFR1-4, PDGFRα/β, c-Kit, and Ret. Anlotinib as a receptor tyrosine kinase (RTK) inhibitor has potential antineoplastic and anti-angiogenic activities. Anlotinib significantly reduces AN3CA cell number in vitro, characterized by high expression of a mutated FGFR2 protein. Daily oral administration of Anlotinib (5 mg/kg) resulted in a complete response in 55% of animals treated and in a reduced tumor volume, as well as decreased tumor weights of AN3CA tumors by 94% and 96%, respectively, following a 29-day treatment cycle. Whereas carboplatin and paclitaxel failed to alter tumor growth, the combination with Anlotinib did not seem to exhibit a superior effect when compared with Anlotinib treatment alone.


Kinase Assay: Anlotinib (formerly known as AL3818) is a novel and potent multi-kinase inhibitor that inhibits VEGFR2/3, FGFR1-4, PDGFRα/β, c-Kit, and Ret.


Cell Assay: AL3818 significantly reduces AN3CA cell number in vitro, characterized by high expression of a mutated FGFR2 protein. Daily oral administration of AL3818 (5 mg/kg) resulted in a complete response in 55% of animals treated and in a reduced tumor volume, as well as decreased tumor weights of AN3CA tumors by 94% and 96%, respectively, following a 29-day treatment cycle. Whereas carboplatin and paclitaxel failed to alter tumor growth, the combination with AL3818 did not seem to exhibit a superior effect when compared with AL3818 treatment alone.

In VivoDaily oral administration of Anlotinib (5 mg/kg) resulted in a complete response in 55% of animals treated and in a reduced tumor volume, as well as decreased tumor weights of AN3CA tumors by 94% and 96%, respectively, following a 29-day treatment cycle. Whereas carboplatin and paclitaxel failed to alter tumor growth, the combination with Anlotinib did not seem to exhibit a superior effect when compared with Anlotinib treatment alone.
Animal model
Formulation & Dosage
References J Hematol Oncol. 2016 Oct 4;9(1):105; Int J Gynecol Cancer. 2018 Jan;28(1):152-160.
生物活性


The lung metastasis changes in patients of alveolar soft tissue sarcoma with lung metastasis during treatment. J Hematol Oncol. 2016 Oct 4;9(1):105.



Duration of treatment and tumor size changes of 20 patients who received 12 mg QD at the 2/1 schedule.

J Hematol Oncol. 2016 Oct 4;9(1):105.



Plasma concentrations of anlotinib over time after a single oral dose of anlotinib capsules at 5 (green line), 10 (purple line), 12 (blue line), or 16 mg anlotinib/person (red line) in male (solid circles) and female cancer patients (open circles) (a). b Correlation of dose with plasma AUC0–120 h. c Correlation of dose with plasma Cmax. d Correlation of dose with t 1/2. e Plasma concentrations of anlotinib (24 h after daily dosing) over time during multiple oral doses of anlotinib capsules at 12 mg anlotinib/person/day in female cancer patients. f Plasma concentrations of anlotinib (24 h after daily dosing) over time during multiple oral doses of anlotinib capsules at 12 mg anlotinib/person/day in male cancer patients. J Hematol Oncol. 2016 Oct 4;9(1):105.