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Lumacaftor VX 809
Product NO.: P175941
Aliases  
CAS NO. 936727-05-8
Formula C24H18N2O5F2 
Weight 452.40692 
EINECS NO.  
MDL NO.  
Lumacaftor VX 809
EOS Med Chem produce Lumacaftor VX-809 936727-05-8 in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.
Lumacaftor VX-809 936727-05-8 Intermediates, EOS Med Chem have 8; Lumacaftor VX-809 936727-05-8 Impurity we have 10, all from GMP, FDA plant.
Now Lumacaftor VX-809 936727-05-8 DMF document is preparing.
Until 2016, Aug, Lumacaftor VX-809 936727-05-8 more than produced 25kg API, 120kg Intermediates
 
Lumacaftor VX-809 936727-05-8 VX 809 936727-05-8
Lumacaftor VX-809 936727-05-9 Intermediate 1- (2,2-Difluoro-benzo [1,3] dioxol-5-yl) -cyclopropanecarboxylicacid 862574-88-7
Lumacaftor VX-809 936727-05-10 Intermediate 6-Chloro-5-Methyl-pyridin-2-ylaMine 442129-37-5
Lumacaftor VX-809 936727-05-11 Intermediate 3- (6-Amino-3-methyl-pyridin-2-yl) -benzoicacidtert-butylester 1083057-14-0
Lumacaftor VX-809 936727-05-12 Intermediate 3-Carboxyphenylboronic acid pinacol ester 269409-73-6
Lumacaftor VX-809 936727-05-13 Intermediate 1- (2,2-difluorobenzo [d] [1,3] dioxol-5-yl) cyclopropanecarbonitrile 862574-87-6
Lumacaftor VX-809 936727-05-14 Intermediate 2- (2,2-difluorobenzo [d] [1,3] dioxol-5-yl) acetonitrile 68119-31-3
Lumacaftor VX-809 936727-05-15 Intermediate 3-tert-Butoxycarbonylphenylboronic acid 220210-56-0
 
 
Name: Lumacaftor
CAS#: 936727-05-8
Chemical Formula: C24H18F2N2O5
Exact Mass: 452.11838
Molecular Weight: 452.41
Elemental Analysis: C, 63.72; H, 4.01; F, 8.40; N, 6.19; O, 17.68
 
Description: Lumacaftor, also known as VX-809, is a potent CFTR corrector, many be useful for treatment of patients with cystic fibrosis who have a phe508del CFTR mutation. Cystic fibrosis (CF) is a genetic disorder that causes multiorgan morbidity and premature death, most commonly from pulmonary dysfunction.
 
Synonym: VX-809; VX809; VX 809; Lumacaftor
IUPAC/Chemical Name: 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid
SMILES Code: O=C(O)C1=CC=CC(C2=NC(NC(C3(C4=CC=C(OC(F)(F)O5)C5=C4)CC3)=O)=CC=C2C)=C1
 
1: Arora K, Naren AP. Pharmacological Correction of Cystic Fibrosis: Molecular Mechanisms at the Plasma Membrane to Augment Mutant CFTR Function. Curr Drug Targets. 2015 Dec 8. [Epub ahead of print] PubMed PMID: 26648081.
2: Brewington JJ, McPhail GL, Clancy JP. Lumacaftor alone and combined with ivacaftor: preclinical and clinical trial experience of F508del CFTR correction. Expert Rev Respir Med. 2015 Dec 9:1-13. [Epub ahead of print] PubMed PMID: 26581802.
3: Bosch B, De Boeck K. Searching for a cure for cystic fibrosis. A 25-year quest in a nutshell. Eur J Pediatr. 2015 Nov 14. [Epub ahead of print] PubMed PMID: 26567541.
4: Dong ZW, Chen J, Ruan YC, Zhou T, Chen Y, Chen Y, Tsang LL, Chan HC, Peng YZ. CFTR-regulated MAPK/NF-κB signaling in pulmonary inflammation in thermal inhalation injury. Sci Rep. 2015 Oct 30;5:15946. doi: 10.1038/srep15946. PubMed PMID: 26515683; PubMed Central PMCID: PMC4626762.
5: Rehman A, Baloch NU, Janahi IA. Lumacaftor-Ivacaftor in Patients with Cystic Fibrosis Homozygous for Phe508del CFTR. N Engl J Med. 2015 Oct 29;373(18):1783. doi: 10.1056/NEJMc1510466#SA1. PubMed PMID: 26510035.
6: Wainwright CE, Elborn JS, Ramsey BW. Lumacaftor-Ivacaftor in Patients with Cystic Fibrosis Homozygous for Phe508del CFTR. N Engl J Med. 2015 Oct 29;373(18):1783-4. doi: 10.1056/NEJMc1510466. PubMed PMID: 26510034.
7: Elborn JS, Ramsey B, Wainwright C, Boyle M. Response to: 'Lumacaftor/ivacaftor for patients homozygous for Phe508del-CFTR: should we curb our enthusiasm?' by Jones and Barry. Thorax. 2015 Oct 27. pii: thoraxjnl-2015-207611. doi: 10.1136/thoraxjnl-2015-207611. [Epub ahead of print] PubMed PMID: 26506855.
8: Matthes E, Goepp J, Carlile GW, Luo Y, Dejgaard K, Billet A, Robert R, Thomas DY, Hanrahan JW. Low free drug concentration prevents inhibition of F508del CFTR functional expression by the potentiator VX-770 (ivacaftor). Br J Pharmacol. 2015 Oct 22. doi: 10.1111/bph.13365. [Epub ahead of print] PubMed PMID: 26492939.
9: Gohil K. Pharmaceutical Approval Update. P T. 2015 Sep;40(9):567-8. PubMed PMID: 26417173; PubMed Central PMCID: PMC4571842.
10: Kuk K, Taylor-Cousar JL. Lumacaftor and ivacaftor in the management of patients with cystic fibrosis: current evidence and future prospects. Ther Adv Respir Dis. 2015 Dec;9(6):313-26. doi: 10.1177/1753465815601934. Epub 2015 Sep 28. Review. PubMed PMID: 26416827.
11: Silverman E. Orkambi's Slick Unveiling Puts Insurers in a Bind. Manag Care. 2015 Aug;24(8):16-7. PubMed PMID: 26399136.
12: Ong T, Ramsey BW. Update in Cystic Fibrosis 2014. Am J Respir Crit Care Med. 2015 Sep 15;192(6):669-75. doi: 10.1164/rccm.201504-0656UP. Review. PubMed PMID: 26371812.
13: Bali V, Lazrak A, Guroji P, Fu L, Matalon S, Bebok Z. A synonymous codon change alters the drug sensitivity of ΔF508 cystic fibrosis transmembrane conductance regulator. FASEB J. 2015 Sep 3. pii: fj.15-273714. [Epub ahead of print] PubMed PMID: 26336913.
14: Goralski JL, Davis SD. Improving complex medical care while awaiting next-generation CFTR potentiators and correctors: The current pipeline of therapeutics. Pediatr Pulmonol. 2015 Oct;50 Suppl 40:S66-73. doi: 10.1002/ppul.23253. PubMed PMID: 26335956.
15: Phuan PW, Veit G, Tan JA, Finkbeiner WE, Lukacs GL, Verkman AS. Potentiators of Defective ΔF508-CFTR Gating that Do Not Interfere with Corrector Action. Mol Pharmacol. 2015 Oct;88(4):791-9. doi: 10.1124/mol.115.099689. Epub 2015 Aug 5. PubMed PMID: 26245207; PubMed Central PMCID: PMC4576684.
16: Sinha C, Zhang W, Moon CS, Actis M, Yarlagadda S, Arora K, Woodroofe K, Clancy JP, Lin S, Ziady AG, Frizzell R, Fujii N, Naren AP. Capturing the Direct Binding of CFTR Correctors to CFTR by Using Click Chemistry. Chembiochem. 2015 Sep 21;16(14):2017-22. doi: 10.1002/cbic.201500123. Epub 2015 Aug 11. PubMed PMID: 26227551; PubMed Central PMCID: PMC4672727.
17: Ferkol T, Quinton P. Precision Medicine: At What Price? Am J Respir Crit Care Med. 2015 Sep 15;192(6):658-9. doi: 10.1164/rccm.201507-1428ED. PubMed PMID: 26207804.
18: Tomati V, Sondo E, Armirotti A, Caci E, Pesce E, Marini M, Gianotti A, Jeon YJ, Cilli M, Pistorio A, Mastracci L, Ravazzolo R, Scholte B, Ronai Z, Galietta LJ, Pedemonte N. Genetic Inhibition Of The Ubiquitin Ligase Rnf5 Attenuates Phenotypes Associated To F508del Cystic Fibrosis Mutation. Sci Rep. 2015 Jul 17;5:12138. doi: 10.1038/srep12138. PubMed PMID: 26183966; PubMed Central PMCID: PMC4505316.
19: Nau JY. [Cystic Fibrosis: toward a genetic treatment; Clostridium difficile versus Clostridium difficile]. Rev Med Suisse. 2015 May 27;11(476):1210-1. French. PubMed PMID: 26182641.
20: Farinha CM, Sousa M, Canato S, Schmidt A, Uliyakina I, Amaral MD. Increased efficacy of VX-809 in different cellular systems results from an early stabilization effect of F508del-CFTR. Pharmacol Res Perspect. 2015 Aug;3(4):e00152. doi: 10.1002/prp2.152. Epub 2015 Jun 11. PubMed PMID: 26171232; PubMed Central PMCID: PMC4492728.
 
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