Osimertinib mesylate
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MedKoo CAT#: 206426

CAS#: 1421373-66-1 (mesylate)

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.


Chemical Structure

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Osimertinib mesylate
CAS# 1421373-66-1 (mesylate)

Theoretical Analysis

MedKoo Cat#: 206426
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

Size Price Shipping out time Quantity
1g USD 150 Same day
2g USD 250 Same day
5g USD 550 Same day
10g USD 950 Same day
20g USD 1650 Same day
50g USD 2650 2 Weeks
100g USD 4650 2 Weeks
1kg USD 12950 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2021-02-27. Prices are subject to change without notice.

Osimertinib mesylate, purity > 98%, is in stock. The same day shipping out after order is received.

Related CAS #: 1421373-65-0 (free base)   1421373-66-1 (mesylate)    

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

InChi Key: FUKSNUHSJBTCFJ-UHFFFAOYSA-N

InChi Code: InChI=1S/C28H33N7O2.CH4O3S/c1-7-27(36)30-22-16-23(26(37-6)17-25(22)34(4)15-14-33(2)3)32-28-29-13-12-21(31-28)20-18-35(5)24-11-9-8-10-19(20)24;1-5(2,3)4/h7-13,16-18H,1,14-15H2,2-6H3,(H,30,36)(H,29,31,32);1H3,(H,2,3,4)

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

Appearance:
Light yellow 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:
>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).

HS Tariff Code:
2934.99.9001

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
Soluble in DMSO, not in water 100.0

Preparing Stock Solutions

The following data is based on the product molecular weight 595.72 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.

Select a batch to recalculate based on the batch molecular weight:
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

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1: Zhang Z, Yang S, Wang Q. Impact of MET alterations on targeted therapy with EGFR-tyrosine kinase inhibitors for EGFR-mutant lung cancer. Biomark Res. 2019 Nov 21;7:27. doi: 10.1186/s40364-019-0179-6. eCollection 2019. Review. PubMed PMID: 31832192; PubMed Central PMCID: PMC6873421.

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6: Solassol I, Pinguet F, Quantin X. FDA- and EMA-Approved Tyrosine Kinase Inhibitors in Advanced EGFR-Mutated Non-Small Cell Lung Cancer: Safety, Tolerability, Plasma Concentration Monitoring, and Management. Biomolecules. 2019 Oct 30;9(11). pii: E668. doi: 10.3390/biom9110668. Review. PubMed PMID: 31671561.

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9: Leonetti A, Sharma S, Minari R, Perego P, Giovannetti E, Tiseo M. Resistance mechanisms to osimertinib in EGFR-mutated non-small cell lung cancer. Br J Cancer. 2019 Oct;121(9):725-737. doi: 10.1038/s41416-019-0573-8. Epub 2019 Sep 30. Review. PubMed PMID: 31564718; PubMed Central PMCID: PMC6889286.

10: Masood A, Kancha RK, Subramanian J. Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors in non-small cell lung cancer harboring uncommon EGFR mutations: Focus on afatinib. Semin Oncol. 2019 Jun;46(3):271-283. doi: 10.1053/j.seminoncol.2019.08.004. Epub 2019 Sep 11. Review. PubMed PMID: 31558282.

11: Wang S, Li J. Second-generation EGFR and ErbB tyrosine kinase inhibitors as first-line treatments for non-small cell lung cancer. Onco Targets Ther. 2019 Aug 15;12:6535-6548. doi: 10.2147/OTT.S198945. eCollection 2019. Review. PubMed PMID: 31496745; PubMed Central PMCID: PMC6700283.

12: Xu ZY, Li JL. Comparative review of drug-drug interactions with epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of non-small-cell lung cancer. Onco Targets Ther. 2019 Jul 9;12:5467-5484. doi: 10.2147/OTT.S194870. eCollection 2019. Review. PubMed PMID: 31371986; PubMed Central PMCID: PMC6636179.

13: Peters GJ. From 'Targeted Therapy' to Targeted Therapy. Anticancer Res. 2019 Jul;39(7):3341-3345. doi: 10.21873/anticanres.13476. Review. PubMed PMID: 31262854.

14: Wang Q, Yang S, Wang K, Sun SY. MET inhibitors for targeted therapy of EGFR TKI-resistant lung cancer. J Hematol Oncol. 2019 Jun 21;12(1):63. doi: 10.1186/s13045-019-0759-9. Review. PubMed PMID: 31227004; PubMed Central PMCID: PMC6588884.

15: Wang X, Zhong D. [Advanced Research on Non-small Cell Lung Cancer with De Novo T790M Mutation]. Zhongguo Fei Ai Za Zhi. 2019 May 20;22(5):324-328. doi: 10.3779/j.issn.1009-3419.2019.05.10. Review. Chinese. PubMed PMID: 31109443.

16: Singhi EK, Horn L, Sequist LV, Heymach J, Langer CJ. Advanced Non-Small Cell Lung Cancer: Sequencing Agents in the EGFR-Mutated/ALK-Rearranged Populations. Am Soc Clin Oncol Educ Book. 2019 Jan;39:e187-e197. doi: 10.1200/EDBK_237821. Epub 2019 May 17. Review. PubMed PMID: 31099642.

17: Rajappa S, Krishna MV, Narayanan P. Integrating Osimertinib in Clinical Practice for Non-Small Cell Lung Cancer Treatment. Adv Ther. 2019 Jun;36(6):1279-1290. doi: 10.1007/s12325-019-00917-6. Epub 2019 Apr 2. Review. PubMed PMID: 30941723.

18: Russo A, Franchina T, Ricciardi G, Battaglia A, Picciotto M, Adamo V. Heterogeneous Responses to Epidermal Growth Factor Receptor (EGFR) Tyrosine Kinase Inhibitors (TKIs) in Patients with Uncommon EGFR Mutations: New Insights and Future Perspectives in this Complex Clinical Scenario. Int J Mol Sci. 2019 Mar 21;20(6). pii: E1431. doi: 10.3390/ijms20061431. Review. PubMed PMID: 30901844; PubMed Central PMCID: PMC6470640.

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Additional Information

Related CAS#
CAS#1421373-65-0 (Osimertinib free base);
CAS#1421373-66-1 (Osimertinib mesylate salt)