Name: Osimertinib mesylate
CAS#: 1421373-66-1 (mesylate)
Chemical Formula: C29H37N7O5S
Exact Mass:
Molecular Weight: 595.72
Elemental Analysis: C, 58.47; H, 6.26; N, 16.46; O, 13.43; S, 5.38
We produce Osimertinib mesylate,Osimertinib free base,AZD 9291,1421373-66-1,1421373-65-0 in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.
Osimertinib mesylate,Osimertinib free base,AZD 9291,1421373-66-1,1421373-65-0 Intermediates, we have 8; Osimertinib mesylate,Osimertinib free base,AZD 9291,1421373-66-1,1421373-65-0 Impurity we have 10, all from GMP, FDA plant.
Now Osimertinib mesylate,Osimertinib free base,AZD 9291,1421373-66-1,1421373-65-0 DMF document is preparing.
Until 2016, Aug, Osimertinib mesylate,Osimertinib free base,AZD 9291,1421373-66-1,1421373-65-0 more than produced 25kg API, 120kg Intermediates
Osimertinib Mesylate AZD-9291 (Mesylate);Tagrisso; 1421373-66-1
Osimertinib Mesylate Intermediates N-(2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxy-5-((4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl)amino)phenyl)acrylamide 1421373-65-0
Osimertinib Mesylate Intermediates N-(5-((4-(1H-indol-3-yl)pyrimidin-2-yl)amino)-2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxyphenyl)acrylamide 1421373-98-9
Osimertinib Mesylate Intermediates N-(4-fluoro-2-methoxy-5-nitrophenyl)-4-(1-methyl-1H-indol-3-yl)pyrimidin-2-amine 1421372-94-2
Osimertinib Mesylate Intermediates 3-(2-chloropyrimidin-4-yl)-1-methyl-1H-indole 1032452-86-0
GMP PRODUCE:
Alectinib;Veliparib;Acalabrutinib;Venetoclax;Sotagliflozin;Ledipasvir;LX1606;Anacetrapib;Abemaciclib
Description: Osimertinib, also known as mereletinib and AZD-9291, is a third-generation EGFR inhibitor, showed promise in preclinical studies and provides hope for patients with advanced lung cancers that have become resistant to existing EGFR inhibitors. AZD9291 is highly active in preclinical models and is well tolerated in animal models. It inhibits both activating and resistant EGFR mutations while sparing the normal form of EGFR that is present in normal skin and gut cells, thereby reducing the side effects encountered with currently available medicines. Osimertinib was approved on Nov. 2015.
Synonym: AZD-9291; AZD 9291; AZD9291; AZD-9291 mesylate; Mereletinib; Mereletinib mesylate; Osimertinib mesylate. Brand name: Tagrisso.
IUPAC/Chemical Name: N-(2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxy-5-((4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl)amino)phenyl)acrylamide mesylate
SMILES Code: CN(CCN(C)C)C1=CC(OC)=C(C=C1NC(C=C)=O)NC2=NC=CC(C3=CN(C)C4=C3C=CC=C4)=N2.OS(=O)(C)=O
1: Lung cancer: Diverse EGFR mutations explain AZD9291 resistance. Nat Rev Clin Oncol. 2015 May 19. doi: 10.1038/nrclinonc.2015.97. [Epub ahead of print] PubMed PMID: 25985937.
2: Thress KS, Paweletz CP, Felip E, Cho BC, Stetson D, Dougherty B, Lai Z, Markovets A, Vivancos A, Kuang Y, Ercan D, Matthews SE, Cantarini M, Barrett JC, Jänne PA, Oxnard GR. Acquired EGFR C797S mutation mediates resistance to AZD9291 in non-small cell lung cancer harboring EGFR T790M. Nat Med. 2015 Jun;21(6):560-2. doi: 10.1038/nm.3854. Epub 2015 May 4. PubMed PMID: 25939061.
3: Jänne PA, Yang JC, Kim DW, Planchard D, Ohe Y, Ramalingam SS, Ahn MJ, Kim SW, Su WC, Horn L, Haggstrom D, Felip E, Kim JH, Frewer P, Cantarini M, Brown KH, Dickinson PA, Ghiorghiu S, Ranson M. AZD9291 in EGFR inhibitor-resistant non-small-cell lung cancer. N Engl J Med. 2015 Apr 30;372(18):1689-99. doi: 10.1056/NEJMoa1411817. PubMed PMID: 25923549.
4: Eberlein CA, Stetson D, Markovets AA, Al-Kadhimi KJ, Lai Z, Fisher PR, Meador CB, Spitzler P, Ichihara E, Ross SJ, Ahdesmaki MJ, Ahmed A, Ratcliffe LE, O'Brien EL, Barnes CH, Brown H, Smith PD, Dry JR, Beran G, Thress KS, Dougherty B, Pao W, Cross DA. Acquired Resistance to the Mutant-Selective EGFR Inhibitor AZD9291 Is Associated with Increased Dependence on RAS Signaling in Preclinical Models. Cancer Res. 2015 Jun 15;75(12):2489-500. doi: 10.1158/0008-5472.CAN-14-3167. Epub 2015 Apr 13. PubMed PMID: 25870145.
5: Jiang T, Zhou C. Clinical activity of the mutant-selective EGFR inhibitor AZD9291 in patients with EGFR inhibitor-resistant non-small cell lung cancer. Transl Lung Cancer Res. 2014 Dec;3(6):370-2. doi: 10.3978/j.issn.2218-6751.2014.08.02. PubMed PMID: 25806323; PubMed Central PMCID: PMC4367669.
6: Finlay MR, Anderton M, Ashton S, Ballard P, Bethel PA, Box MR, Bradbury RH, Brown SJ, Butterworth S, Campbell A, Chorley C, Colclough N, Cross DA, Currie GS, Grist M, Hassall L, Hill GB, James D, James M, Kemmitt P, Klinowska T, Lamont G, Lamont SG, Martin N, McFarland HL, Mellor MJ, Orme JP, Perkins D, Perkins P, Richmond G, Smith P, Ward RA, Waring MJ, Whittaker D, Wells S, Wrigley GL. Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor. J Med Chem. 2014 Oct 23;57(20):8249-67. doi: 10.1021/jm500973a. Epub 2014 Oct 1. PubMed PMID: 25271963.
7: AZD9291 could be an option for NSCLC. Cancer Discov. 2014 Aug;4(8):OF10. doi: 10.1158/2159-8290.CD-NB2014-077. Epub 2014 May 22. PubMed PMID: 25092747.
8: Cross DA, Ashton SE, Ghiorghiu S, Eberlein C, Nebhan CA, Spitzler PJ, Orme JP, Finlay MR, Ward RA, Mellor MJ, Hughes G, Rahi A, Jacobs VN, Red Brewer M, Ichihara E, Sun J, Jin H, Ballard P, Al-Kadhimi K, Rowlinson R, Klinowska T, Richmond GH, Cantarini M, Kim DW, Ranson MR, Pao W. AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer. Cancer Discov. 2014 Sep;4(9):1046-61. doi: 10.1158/2159-8290.CD-14-0337. Epub 2014 Jun 3. PubMed PMID: 24893891; PubMed Central PMCID: PMC4315625.
CAS#: 1421373-66-1 (mesylate)
Chemical Formula: C29H37N7O5S
Exact Mass:
Molecular Weight: 595.72
Elemental Analysis: C, 58.47; H, 6.26; N, 16.46; O, 13.43; S, 5.38
We produce Osimertinib mesylate,Osimertinib free base,AZD 9291,1421373-66-1,1421373-65-0 in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.
Osimertinib mesylate,Osimertinib free base,AZD 9291,1421373-66-1,1421373-65-0 Intermediates, we have 8; Osimertinib mesylate,Osimertinib free base,AZD 9291,1421373-66-1,1421373-65-0 Impurity we have 10, all from GMP, FDA plant.
Now Osimertinib mesylate,Osimertinib free base,AZD 9291,1421373-66-1,1421373-65-0 DMF document is preparing.
Until 2016, Aug, Osimertinib mesylate,Osimertinib free base,AZD 9291,1421373-66-1,1421373-65-0 more than produced 25kg API, 120kg Intermediates
Osimertinib Mesylate AZD-9291 (Mesylate);Tagrisso; 1421373-66-1
Osimertinib Mesylate Intermediates N-(2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxy-5-((4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl)amino)phenyl)acrylamide 1421373-65-0
Osimertinib Mesylate Intermediates N-(5-((4-(1H-indol-3-yl)pyrimidin-2-yl)amino)-2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxyphenyl)acrylamide 1421373-98-9
Osimertinib Mesylate Intermediates N-(4-fluoro-2-methoxy-5-nitrophenyl)-4-(1-methyl-1H-indol-3-yl)pyrimidin-2-amine 1421372-94-2
Osimertinib Mesylate Intermediates 3-(2-chloropyrimidin-4-yl)-1-methyl-1H-indole 1032452-86-0
GMP PRODUCE:
Alectinib;Veliparib;Acalabrutinib;Venetoclax;Sotagliflozin;Ledipasvir;LX1606;Anacetrapib;Abemaciclib
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Synonym: AZD-9291; AZD 9291; AZD9291; AZD-9291 mesylate; Mereletinib; Mereletinib mesylate; Osimertinib mesylate. Brand name: Tagrisso.
IUPAC/Chemical Name: N-(2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxy-5-((4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl)amino)phenyl)acrylamide mesylate
SMILES Code: CN(CCN(C)C)C1=CC(OC)=C(C=C1NC(C=C)=O)NC2=NC=CC(C3=CN(C)C4=C3C=CC=C4)=N2.OS(=O)(C)=O
1: Lung cancer: Diverse EGFR mutations explain AZD9291 resistance. Nat Rev Clin Oncol. 2015 May 19. doi: 10.1038/nrclinonc.2015.97. [Epub ahead of print] PubMed PMID: 25985937.
2: Thress KS, Paweletz CP, Felip E, Cho BC, Stetson D, Dougherty B, Lai Z, Markovets A, Vivancos A, Kuang Y, Ercan D, Matthews SE, Cantarini M, Barrett JC, Jänne PA, Oxnard GR. Acquired EGFR C797S mutation mediates resistance to AZD9291 in non-small cell lung cancer harboring EGFR T790M. Nat Med. 2015 Jun;21(6):560-2. doi: 10.1038/nm.3854. Epub 2015 May 4. PubMed PMID: 25939061.
3: Jänne PA, Yang JC, Kim DW, Planchard D, Ohe Y, Ramalingam SS, Ahn MJ, Kim SW, Su WC, Horn L, Haggstrom D, Felip E, Kim JH, Frewer P, Cantarini M, Brown KH, Dickinson PA, Ghiorghiu S, Ranson M. AZD9291 in EGFR inhibitor-resistant non-small-cell lung cancer. N Engl J Med. 2015 Apr 30;372(18):1689-99. doi: 10.1056/NEJMoa1411817. PubMed PMID: 25923549.
4: Eberlein CA, Stetson D, Markovets AA, Al-Kadhimi KJ, Lai Z, Fisher PR, Meador CB, Spitzler P, Ichihara E, Ross SJ, Ahdesmaki MJ, Ahmed A, Ratcliffe LE, O'Brien EL, Barnes CH, Brown H, Smith PD, Dry JR, Beran G, Thress KS, Dougherty B, Pao W, Cross DA. Acquired Resistance to the Mutant-Selective EGFR Inhibitor AZD9291 Is Associated with Increased Dependence on RAS Signaling in Preclinical Models. Cancer Res. 2015 Jun 15;75(12):2489-500. doi: 10.1158/0008-5472.CAN-14-3167. Epub 2015 Apr 13. PubMed PMID: 25870145.
5: Jiang T, Zhou C. Clinical activity of the mutant-selective EGFR inhibitor AZD9291 in patients with EGFR inhibitor-resistant non-small cell lung cancer. Transl Lung Cancer Res. 2014 Dec;3(6):370-2. doi: 10.3978/j.issn.2218-6751.2014.08.02. PubMed PMID: 25806323; PubMed Central PMCID: PMC4367669.
6: Finlay MR, Anderton M, Ashton S, Ballard P, Bethel PA, Box MR, Bradbury RH, Brown SJ, Butterworth S, Campbell A, Chorley C, Colclough N, Cross DA, Currie GS, Grist M, Hassall L, Hill GB, James D, James M, Kemmitt P, Klinowska T, Lamont G, Lamont SG, Martin N, McFarland HL, Mellor MJ, Orme JP, Perkins D, Perkins P, Richmond G, Smith P, Ward RA, Waring MJ, Whittaker D, Wells S, Wrigley GL. Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor. J Med Chem. 2014 Oct 23;57(20):8249-67. doi: 10.1021/jm500973a. Epub 2014 Oct 1. PubMed PMID: 25271963.
7: AZD9291 could be an option for NSCLC. Cancer Discov. 2014 Aug;4(8):OF10. doi: 10.1158/2159-8290.CD-NB2014-077. Epub 2014 May 22. PubMed PMID: 25092747.
8: Cross DA, Ashton SE, Ghiorghiu S, Eberlein C, Nebhan CA, Spitzler PJ, Orme JP, Finlay MR, Ward RA, Mellor MJ, Hughes G, Rahi A, Jacobs VN, Red Brewer M, Ichihara E, Sun J, Jin H, Ballard P, Al-Kadhimi K, Rowlinson R, Klinowska T, Richmond GH, Cantarini M, Kim DW, Ranson MR, Pao W. AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer. Cancer Discov. 2014 Sep;4(9):1046-61. doi: 10.1158/2159-8290.CD-14-0337. Epub 2014 Jun 3. PubMed PMID: 24893891; PubMed Central PMCID: PMC4315625.
