Osimertinib free base
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 206042

CAS#: 1421373-65-0 (free base)

Description: Osimertinib, also known as AZD-9291 and Mereletinib, 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 in Nov. 2015 by FDA.


Price and Availability

Size
Price

1g
USD 150
10g
USD 950
Size
Price

2g
USD 250
50g
USD 2650
Size
Price

5g
USD 550
1kg
USD 9950

Osimertinib free base, purity > 98%, is in stock. The same day shipping out after order is received. Note: the estimated shipping out time for order > 4g may be 2 weeks.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 206042
Name: Osimertinib free base
CAS#: 1421373-65-0 (free base)
Chemical Formula: C28H33N7O2
Exact Mass: 499.26957
Molecular Weight: 499.60732
Elemental Analysis: C, 67.31; H, 6.66; N, 19.62; O, 6.40


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

Synonym: AZD9291; AZD 9291; AZD-9291; AZD-9291 freebase; Mereletinib; Osimertinib free base; trade 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

InChi Key: DUYJMQONPNNFPI-UHFFFAOYSA-N

InChi Code: InChI=1S/C28H33N7O2/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/h7-13,16-18H,1,14-15H2,2-6H3,(H,30,36)(H,29,31,32)

SMILES Code: C=CC(NC1=CC(NC2=NC=CC(C3=CN(C)C4=C3C=CC=C4)=N2)=C(OC)C=C1N(CCN(C)C)C)=O


Technical Data

Appearance:
Brown to yellow solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Certificate of Analysis:

Safety Data Sheet (MSDS):

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).

Harmonized System Code:
2934.99.90.01


Additional Information

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


References

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2: Shetty V, Babu S. Management of CNS metastases in patients with EGFR mutation-positive NSCLC. Indian J Cancer. 2019 Nov;56(Supplement):S31-S37. doi: 10.4103/ijc.IJC_455_19. Review. PubMed PMID: 31793440.

3: Doval DC, Desai CJ, Sahoo TP. Molecularly targeted therapies in non-small cell lung cancer: The evolving role of tyrosine kinase inhibitors. Indian J Cancer. 2019 Nov;56(Supplement):S23-S30. doi: 10.4103/ijc.IJC_449_19. Review. PubMed PMID: 31793439.

4: Rebuzzi SE, Alfieri R, La Monica S, Minari R, Petronini PG, Tiseo M. Combination of EGFR-TKIs and chemotherapy in advanced EGFR mutated NSCLC: Review of the literature and future perspectives. Crit Rev Oncol Hematol. 2019 Oct 31:102820. doi: 10.1016/j.critrevonc.2019.102820. [Epub ahead of print] Review. PubMed PMID: 31785991.

5: Zhu VW, Klempner SJ, Ou SI. Receptor Tyrosine Kinase Fusions as an Actionable Resistance Mechanism to EGFR TKIs in EGFR-Mutant Non-Small-Cell Lung Cancer. Trends Cancer. 2019 Nov;5(11):677-692. doi: 10.1016/j.trecan.2019.09.008. Epub 2019 Oct 29. Review. PubMed PMID: 31735287.

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.

7: LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012-. Available from http://www.ncbi.nlm.nih.gov/books/NBK548495/ PubMed PMID: 31643814.

8: Gelatti ACZ, Drilon A, Santini FC. Optimizing the sequencing of tyrosine kinase inhibitors (TKIs) in epidermal growth factor receptor (EGFR) mutation-positive non-small cell lung cancer (NSCLC). Lung Cancer. 2019 Nov;137:113-122. doi: 10.1016/j.lungcan.2019.09.017. Epub 2019 Sep 23. Review. PubMed PMID: 31568888.

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.

19: Le T, Gerber DE. Newer-Generation EGFR Inhibitors in Lung Cancer: How Are They Best Used? Cancers (Basel). 2019 Mar 15;11(3). pii: E366. doi: 10.3390/cancers11030366. Review. PubMed PMID: 30875928; PubMed Central PMCID: PMC6468595.

20: Holleman MS, van Tinteren H, Groen HJ, Al MJ, Uyl-de Groot CA. First-line tyrosine kinase inhibitors in EGFR mutation-positive non-small-cell lung cancer: a network meta-analysis. Onco Targets Ther. 2019 Feb 20;12:1413-1421. doi: 10.2147/OTT.S189438. eCollection 2019. Review. PubMed PMID: 30863108; PubMed Central PMCID: PMC6388947.