CH5164840
WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#:406498
CAS#:1052645-73-4
Description:CH5164840 is a potent and selective HSP90 inhibitor. CH5164840 showed remarkable antitumor activity against NSCLC cell lines and xenograft models. CH5164840 has potent antitumor activity and is highly effective in combination with erlotinib against NSCLC tumors with EGFR overexpression and mutations.
Price and Availability
CH5164840, purity > 98%, is not in stock, may be available through custom synthesis. For cost-effective reason, minimum 1 gram order is requested. The product will be characterized by NMR, HPLC and MS analysis. Purity (HPLC) is usually >98%. CoA, QC data, MSDS will be provided when product is successfully made. The estimated lead time is 2-3 months. Please send email to sales@medkoo.com to inquire quote.
Chemical Structure
Theoretical Analysis
MedKoo Cat#: 406498Name: CH5164840CAS#: 1052645-73-4Chemical Formula: C19H23N5O2SExact Mass: 385.15725Molecular Weight: 385.48322Elemental Analysis: C, 59.20; H, 6.01; N, 18.17; O, 8.30; S, 8.32
Synonym:CH5164840; CH-5164840; CH 5164840.
IUPAC/Chemical Name:7 -Thia-3,5,11,15-tetraazatricyclo[15.3.1.12,6]docosa-1(21),2,4,6(22),17,19-hexaene-10,16-dione, 4-amino-18,20-dimethyl-.
InChi Key:OMFBVBRFVYLRQT-UHFFFAOYSA-N
InChi Code:InChI=1S/C19H23N5O2S/c1-11-8-12(2)14-9-13(11)15-10-17(24-19(20)23-15)27-7-4-16(25)21-5-3-6-22-18(14)26/h8-10H,3-7H2,1-2H3,(H,21,25)(H,22,26)(H2,20,23,24)
SMILES Code:NC1=NC(C(C=C2C(NCCCN3)=O)=C(C)C=C2C)=CC(SCCC3=O)=N1
Technical Data
Additional Information
Structure comparison between CH5015765 , CH5138303 and CH5164804
References
1: Kanamaru C, Yamada Y, Hayashi S, Matsushita T,Suda A, Nagayasu M, Kimura K, Chiba S. Retinal toxicity induced bysmall-molecule Hsp90 inhibitors in beagle dogs. J Toxicol Sci.2014;39(1):59-69. PubMed PMID: 24418710.
2: Saitoh R, Nagayasu M, Shibahara N, Ono N, Suda A, Kato M, Ishigai M.Assessing the Impact of HER2 Status on the Antitumor Activity of anHSP90 Inhibitor in Human Tumor Xenograft Mice using Pharmacokinetics-PharmacodynamicModeling. Drug Metab Pharmacokinet. 2013 Oct 15. [Epub ahead of print]PubMed PMID: 24126359.
3: Ono N, Yamazaki T, Tsukaguchi T, Fujii T, Sakata K, Suda A, TsukudaT, Mio T, Ishii N, Kondoh O, Aoki Y. Enhanced antitumor activity oferlotinib in combination with the Hsp90 inhibitor CH5164840 againstnon-small-cell lung cancer. Cancer Sci. 2013 Oct;104(10):1346-52. doi:10.1111/cas.12237. Epub 2013 Aug 20. PubMed PMID: 23863134.
4: Suda A, Koyano H, Hayase T, Hada K, Kawasaki K, Komiyama S, HasegawaK, Fukami TA, Sato S, Miura T, Ono N, Yamazaki T, Saitoh R, Shimma N,Shiratori Y, Tsukuda T. Design and synthesis of novel macrocyclic2-amino-6-arylpyrimidine Hsp90 inhibitors. Bioorg Med Chem Lett. 2012Jan 15;22(2):1136-41. doi: 10.1016/j.bmcl.2011.11.100. Epub 2011 Dec 1.PubMed PMID: 22192591.
5: Ono N, Yamazaki T, Nakanishi Y, Fujii T, Sakata K, Tachibana Y, SudaA, Hada K, Miura T, Sato S, Saitoh R, Nakano K, Tsukuda T, Mio T, IshiiN, Kondoh O, Aoki Y. Preclinical antitumor activity of the novel heatshock protein 90 inhibitor CH5164840 against human epidermal growthfactor receptor 2 (HER2)-overexpressing cancers. Cancer Sci. 2012Feb;103(2):342-9. doi: 10.1111/j.1349-7006.2011.02144.x. Epub 2011 Dec13. PubMed PMID: 22050138.
