Anlotinib HCl

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 206058

CAS#: 1360460-82-7 (HCl)

Description: Anlotinib, also known as AL3818 and Catequentinib, is a receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic and anti-angiogenic activities. Upon administration, anlotininib targets multiple RTKs, including vascular endothelial growth factor receptor type 2 (VEGFR2) and type 3 (VEGFR3). This agent may both inhibit angiogenesis and halt tumor cell growth.

Chemical Structure

Anlotinib HCl
CAS# 1360460-82-7 (HCl)

Theoretical Analysis

MedKoo Cat#: 206058
Name: Anlotinib HCl
CAS#: 1360460-82-7 (HCl)
Chemical Formula: C23H24Cl2FN3O3
Exact Mass:
Molecular Weight: 480.3614
Elemental Analysis: C, 57.51; H, 5.04; Cl, 14.76; F, 3.96; N, 8.75; O, 9.99

Price and Availability

Size Price Availability Quantity
5.0mg USD 90.0 Ready to ship
10.0mg USD 150.0 Ready to ship
25.0mg USD 250.0 Ready to ship
50.0mg USD 450.0 Ready to ship
100.0mg USD 750.0 Ready to ship
200.0mg USD 1350.0 Ready to ship
Bulk inquiry

Related CAS #: 1058156-90-3 (free base)   1360460-82-7 (HCl)  

Synonym: AL3818; AL-3818; AL 3818; Anlotinib; Anlotinib HCl; Anlotinib dihydrochloride. Catequentinib,

IUPAC/Chemical Name: 1-(((4-((4-fluoro-2-methyl-1H-indol-5-yl)oxy)-6-methoxyquinolin-7-yl)oxy)methyl)cyclopropan-1-amine dihydrochloride


InChi Code: InChI=1S/C23H22FN3O3.2ClH/c1-13-9-15-16(27-13)3-4-19(22(15)24)30-18-5-8-26-17-11-21(20(28-2)10-14(17)18)29-12-23(25)6-7-23;;/h3-5,8-11,27H,6-7,12,25H2,1-2H3;2*1H

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

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >5 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Biological target: Anlotinib HCl is a receptor tyrosine kinase (RTK) inhibitor that primarily inhibits VEGFR2/3, FGFR1-4, PDGFRα/β, c-Kit, and Ret.
In vitro activity: Transforming growth factor-β1 (TGF-β1) is considered to be the most critical fibrogenic factor involved in the development of IPF (idiopathic pulmonary fibrosis) and its function depends on the signal transduction and regulation of Smad and non-Smad. Smad3 is the main activation protein of TGF-β/Smad signalling pathway, regulating a series of gene expression, and promotes fibroblast differentiation and proliferation. The constructed CAGA-NIH3T3 cell line stably transfected with the TGF-β1/Smad3 signalling pathway reporter plasmid was used to detect the effect of anlotinib hydrochloride on TGF-β1/Smad3 signalling pathway. As shown in Figure 5a, luciferases assay showed that anlotinib inhibited the TGFβ1/Smad3 signalling pathway in a dose-dependent manner. According to the results of Luciferases assay, 1 μM was selected as the best effective concentration for subsequent experiments. Further, it was observed that anlotinib hydrochloride significantly inhibited TGF-β1-induced phosphorylation of Smad3 protein, as shown in Figure 5b. Reference: J Pharm Pharmacol. 2020 Jan;72(1):44-55.
In vivo activity: The effect of anlotinib on bleomycin-induced pulmonary fibrosis in mice was evaluated. The histological changes at 14 days are shown in Figure 2a. In the saline group, there was no obvious inflammatory reaction and fibrosis in the lung tissue of mice, and the lung tissue structure was normal. After bleomycin was injected, not only the airway wall was significantly thickened, but also the alveolar structure was disordered. Meanwhile, the lung tissue of mice showed obvious alveolar inflammation, and some alveoli appeared realistic changes and fibrosis. In addition, the mice with bleomycin injection showed higher Ashcroft score than in control group. After anlotinib intervention, the above lesions were alleviated, and the Ashcroft score was significantly reduced (Figure 2b). It was also observed that the content of hydroxyproline in the left lung of mice in bleomycin group was significantly higher than that in saline group, as shown in Figure 2c. In anlotinib-treated group, the hydroxyproline content decreased, indicating that anlotinib inhibited ECM (extracellular matrix) deposition. The effect of anlotinib on the forced vital capacity in bleomycin-induced pulmonary fibrosis mice was also evaluated. The results showed that anlotinib increased the lung capacity of mice (Figure 2d). Reference: J Pharm Pharmacol. 2020 Jan;72(1):44-55.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 54.0 112.42
Water 96.0 199.85

Preparing Stock Solutions

The following data is based on the product molecular weight 480.3614 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Ruan H, Lv Z, Liu S, Zhang L, Huang K, Gao S, Gan W, Liu X, Zhang S, Helian K, Li X, Zhou H, Yang C. Anlotinib attenuated bleomycin-induced pulmonary fibrosis via the TGF-β1 signalling pathway. J Pharm Pharmacol. 2020 Jan;72(1):44-55. doi: 10.1111/jphp.13183. Epub 2019 Oct 28. PMID: 31659758.
In vitro protocol: 1. Ruan H, Lv Z, Liu S, Zhang L, Huang K, Gao S, Gan W, Liu X, Zhang S, Helian K, Li X, Zhou H, Yang C. Anlotinib attenuated bleomycin-induced pulmonary fibrosis via the TGF-β1 signalling pathway. J Pharm Pharmacol. 2020 Jan;72(1):44-55. doi: 10.1111/jphp.13183. Epub 2019 Oct 28. PMID: 31659758.
In vivo protocol: 1. Ruan H, Lv Z, Liu S, Zhang L, Huang K, Gao S, Gan W, Liu X, Zhang S, Helian K, Li X, Zhou H, Yang C. Anlotinib attenuated bleomycin-induced pulmonary fibrosis via the TGF-β1 signalling pathway. J Pharm Pharmacol. 2020 Jan;72(1):44-55. doi: 10.1111/jphp.13183. Epub 2019 Oct 28. PMID: 31659758.

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.


Dilution Calculator

Calculate the dilution required to prepare a stock solution.

  1: Zhong CC, Chen F, Yang JL, Jia WW, Li L, Cheng C, Du FF, Zhang SP, Xie CY, Zhang NT, Olaleye OE, Wang FQ, Xu F, Lou LG, Chen DY, Niu W, Li C. Pharmacokinetics and disposition of anlotinib, an oral tyrosine kinase inhibitor, in experimental animal species. Acta Pharmacol Sin. 2018 Apr 5. doi: 10.1038/aps.2017.199. [Epub ahead of print] PubMed PMID: 29620050.

2: Lin B, Song X, Yang D, Bai D, Yao Y, Lu N. Anlotinib inhibits angiogenesis via suppressing the activation of VEGFR2, PDGFRβ and FGFR1. Gene. 2018 May 15;654:77-86. doi: 10.1016/j.gene.2018.02.026. Epub 2018 Feb 14. PubMed PMID: 29454091.

3: Xie C, Wan X, Quan H, Zheng M, Fu L, Li Y, Lou L. Preclinical characterization of anlotinib, a highly potent and selective vascular endothelial growth factor receptor-2 inhibitor. Cancer Sci. 2018 Apr;109(4):1207-1219. doi: 10.1111/cas.13536. Epub 2018 Mar 25. PubMed PMID: 29446853.

4: Sun W, Wang Z, Chen R, Huang C, Sun R, Hu X, Li W, Chen R. Influences of Anlotinib on Cytochrome P450 Enzymes in Rats Using a Cocktail Method. Biomed Res Int. 2017;2017:3619723. doi: 10.1155/2017/3619723. Epub 2017 Dec 26. PubMed PMID: 29441353; PubMed Central PMCID: PMC5758843.

5: Han B, Li K, Zhao Y, Li B, Cheng Y, Zhou J, Lu Y, Shi Y, Wang Z, Jiang L, Luo Y, Zhang Y, Huang C, Li Q, Wu G. Anlotinib as a third-line therapy in patients with refractory advanced non-small-cell lung cancer: a multicentre, randomised phase II trial (ALTER0302). Br J Cancer. 2018 Mar 6;118(5):654-661. doi: 10.1038/bjc.2017.478. Epub 2018 Feb 13. PubMed PMID: 29438373; PubMed Central PMCID: PMC5846072.

6: Taurin S, Yang CH, Reyes M, Cho S, Coombs DM, Jarboe EA, Werner TL, Peterson CM, Janát-Amsbury MM. Endometrial Cancers Harboring Mutated Fibroblast Growth Factor Receptor 2 Protein Are Successfully Treated With a New Small Tyrosine Kinase Inhibitor in an Orthotopic Mouse Model. Int J Gynecol Cancer. 2018 Jan;28(1):152-160. doi: 10.1097/IGC.0000000000001129. PubMed PMID: 28953502; PubMed Central PMCID: PMC5735020.

7: Zhao J, Zhao H, Chi Y. The Safety and Efficacy of the S1/Temozolomide Regimen in Patients with Metastatic Neuroendocrine Tumors. Neuroendocrinology. 2017 Aug 17. doi: 10.1159/000480402. [Epub ahead of print] PubMed PMID: 28817826.

8: Sun Y, Niu W, Du F, Du C, Li S, Wang J, Li L, Wang F, Hao Y, Li C, Chi Y. Safety, pharmacokinetics, and antitumor properties of anlotinib, an oral multi-target tyrosine kinase inhibitor, in patients with advanced refractory solid tumors. J Hematol Oncol. 2016 Oct 4;9(1):105. PubMed PMID: 27716285; PubMed Central PMCID: PMC5051080.

Additional Information

Related CAS#
1058156-90-3 (Anlotinib)
1360460-82-7 (Anlotinib Dihydrochloride)