| CAS NO: | 1360460-82-7 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 1mg | 电议 |
| 2mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| Molecular Weight (MW) | 480.36 |
|---|---|
| Formula | C23H24Cl2FN3O3 |
| 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 Code | NC1(COC2=C(OC)C=C3C(OC4=C(F)C5=C(NC(C)=C5)C=C4)=CC=NC3=C2)CC1.[H]Cl.[H]Cl |
| 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 Vivo | 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. |
| Animal model | |
| Formulation & Dosage | |
| References | J Hematol Oncol. 2016 Oct 4;9(1):105; Int J Gynecol Cancer. 2018 Jan;28(1):152-160. |
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. |
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