Original:Anlotinib free base 1058156-90-3, stock more than 100g

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Description: Anlotinib, also known as AL3818, 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.

Name: Anlotinib free base 

CAS#: 1058156-90-3 (free base) 

Chemical Formula: C23H22FN3O3 

Exact Mass: 407.1645 

Molecular Weight: 407.4454 

Elemental Analysis: C, 67.80; H, 5.44; F, 4.66; N, 10.31; O, 11.78

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

Synonym: AL3818; AL-3818; AL 3818; Anlotinib; Anlotinib free base;

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

InChi Key: KSMZEXLVHXZPEF-UHFFFAOYSA-N

InChi Code: InChI=1S/C23H22FN3O3/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

SMILES Code: NC1(COC2=C(OC)C=C3C(OC4=C(F)C5=C(NC(C)=C5)C=C4)=CC=NC3=C2)CC1

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

Shelf Life: >2 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).

Harmonized System Code: 293490

REFERENCES

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.