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

200mg
USD 150
2g
USD 650
20g
USD 2950
Size
Price

500mg
USD 250
5g
USD 950
50g
USD 3850
Size
Price

1g
USD 450
10g
USD 1850
100g
USD 5250

Osimertinib free base, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


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:
293490


Additional Information

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


References

1: Galbraith S. The changing world of oncology drug development-A global pharmaceutical company's perspective. Chin Clin Oncol. 2014 Jun;3(2):20. doi: 10.3978/j.issn.2304-3865.2014.05.11. PubMed PMID: 25841416.

2: 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.

3: Planchard D. O10.4AZD9291 a novel EGFR-TKI that overcomes T790M-mediated resistance in NSCLC. Ann Oncol. 2015 Mar;26 Suppl 2:ii14. doi: 10.1093/annonc/mdv088.4. PubMed PMID: 25795815.

4: Liao BC, Lin CC, Yang JC. Second and third-generation epidermal growth factor receptor tyrosine kinase inhibitors in advanced nonsmall cell lung cancer. Curr Opin Oncol. 2015 Mar;27(2):94-101. doi: 10.1097/CCO.0000000000000164. PubMed PMID: 25611025.

5: Stinchcombe TE. Recent advances in the treatment of non-small cell and small cell lung cancer. F1000Prime Rep. 2014 Dec 1;6:117. doi: 10.12703/P6-117. eCollection 2014. Review. PubMed PMID: 25580271; PubMed Central PMCID: PMC4251418.

6: Steuer CE, Khuri FR, Ramalingam SS. The next generation of epidermal growth factor receptor tyrosine kinase inhibitors in the treatment of lung cancer. Cancer. 2014 Dec 17. doi: 10.1002/cncr.29139. [Epub ahead of print] PubMed PMID: 25521095.

7: Meador CB, Jin H, de Stanchina E, Nebhan CA, Pirazzoli V, Wang L, Lu P, Vuong H, Hutchinson KE, Jia P, Chen X, Eisenberg R, Ladanyi M, Politi K, Zhao Z, Lovly CM, Cross DA, Pao W. Optimizing the sequence of anti-EGFR-targeted therapy in EGFR-mutant lung cancer. Mol Cancer Ther. 2015 Feb;14(2):542-52. doi: 10.1158/1535-7163.MCT-14-0723. Epub 2014 Dec 4. PubMed PMID: 25477325; PubMed Central PMCID: PMC4338015.

8: Nguyen KS, Neal JW, Wakelee H. Review of the current targeted therapies for non-small-cell lung cancer. World J Clin Oncol. 2014 Oct 10;5(4):576-87. doi: 10.5306/wjco.v5.i4.576. Review. PubMed PMID: 25302162; PubMed Central PMCID: PMC4129523.

9: Jorge SE, Kobayashi SS, Costa DB. Epidermal growth factor receptor (EGFR) mutations in lung cancer: preclinical and clinical data. Braz J Med Biol Res. 2014 Nov;47(11):929-39. Epub 2014 Sep 5. PubMed PMID: 25296354; PubMed Central PMCID: PMC4230282.

10: 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.