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Purity: ≥98%
Osimertinib mesylate (formerly known as AZD9291; AZD-9291; AZD 9291; mereletinib; Tagrisso), the mesylate salt of osimertinib, is a novel, potent, oral bioavailable, irreversible, and mutant-selective, 3rd generation EGFR inhibitor approved by both FDA and the European Commission for cancer treatment. In LoVo cells, it inhibits WT EGFR, L858R/T790M EGFR, and Exon 19 deletion EGFR with IC50 values of 12.92, 11.44, and 493.8 nM, respectively.
| Targets |
EGFRL858R/T790M (IC50 = 1 nM); EGFRL858R (IC50 = 12 nM)
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| ln Vivo |
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| Enzyme Assay |
Osimertinib, formerly known as mereletinib and AZD-9291, is a third generation EGFR inhibitor that is available orally and is irreversible. It selectively targets specific mutants of EGFR, with IC50 values of 493.8 nM for wild-type EGFR in LoVo cells, L858R/T790M EGFR, and Exon 19 deletion EGFR, respectively. It reduces the side effects associated with currently available medications by inhibiting both activating and resistant EGFR mutations while protecting the normal form of EGFR found in normal skin and gut cells.
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| Cell Assay |
In 96-well plates, cells are plated at a density of 3,000 cells per well. Addition of osimertinib to the medium results in a 72-hour treatment. Cell Counting Kit-8 is used to perform assays for cell viability.
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| Additional Infomation |
Osimertinib mesylate is a methanesulfonate (mesylate) salt prepared from equimolar amounts of osimertinib and methanesulfonic acid. It is used for treatment of EGFR T790M mutation positive non-small cell lung cancer. It has a role as an antineoplastic agent and an epidermal growth factor receptor antagonist. It contains an osimertinib(1+).
Osimertinib Mesylate is the mesylate salt form of osimertinib, a third-generation, orally available, irreversible, mutant-selective, epidermal growth factor receptor (EGFR) inhibitor, with potential antineoplastic activity. Upon oral administration, osimertinib covalently binds to and inhibits the activity of numerous mutant forms of EGFR, including the secondarily-acquired resistance mutation T790M, L858R, and exon 19 deletions, thereby preventing EGFR-mediated signaling. This may both induce cell death and inhibit tumor growth in EGFR-overexpressing tumor cells. EGFR, a receptor tyrosine kinase mutated in many tumor cell types, plays a key role in tumor cell proliferation and tumor vascularization. As this agent is selective towards mutant forms of EGFR, its toxicity profile may be reduced when compared to non-selective EGFR inhibitors which also inhibit wild-type EGFR. See also: Osimertinib (has active moiety). |
| Molecular Formula |
C29H37N7O5S
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| Molecular Weight |
595.72
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| Exact Mass |
595.257
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| Elemental Analysis |
C, 58.47; H, 6.26; N, 16.46; O, 13.43; S, 5.38
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| CAS # |
1421373-66-1
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| Related CAS # |
Osimertinib;1421373-65-0;Osimertinib-d6;1638281-44-3;Osimertinib dimesylate;2070014-82-1
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| PubChem CID |
78357807
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| Appearance |
Light yellow solid powder
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| LogP |
5.817
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
42
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| Complexity |
845
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S(C([H])([H])[H])(=O)(=O)O[H].O(C([H])([H])[H])C1=C(C([H])=C(C(=C1[H])N(C([H])([H])[H])C([H])([H])C([H])([H])N(C([H])([H])[H])C([H])([H])[H])N([H])C(C([H])=C([H])[H])=O)N([H])C1=NC([H])=C([H])C(C2=C([H])N(C([H])([H])[H])C3=C([H])C([H])=C([H])C([H])=C32)=N1
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| InChi Key |
FUKSNUHSJBTCFJ-UHFFFAOYSA-N
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| 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)
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| Chemical Name |
N-[2-[2-(dimethylamino)ethyl-methylamino]-4-methoxy-5-[[4-(1-methylindol-3-yl)pyrimidin-2-yl]amino]phenyl]prop-2-enamide;methanesulfonic acid
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| Synonyms |
AZD-9291 mesylate; Mereletinib mesylate; AZD9291; AZD 9291; Trade name: Tagrisso
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.39 mg/mL (2.33 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 13.9 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.39 mg/mL (2.33 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 13.9 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1.39 mg/mL (2.33 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 1% DMSO+30% PEG 300+dd H2O: 30mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6786 mL | 8.3932 mL | 16.7864 mL | |
| 5 mM | 0.3357 mL | 1.6786 mL | 3.3573 mL | |
| 10 mM | 0.1679 mL | 0.8393 mL | 1.6786 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05880706 | Recruiting | Drug: Osimertinib Mesylate Tablets Drug: BL-B01D1 |
Non-small Cell Lung Cancer | Sichuan Baili Pharmaceutical Co., Ltd. |
July 19, 2023 | Phase 2 |
| NCT05020769 | Recruiting | Drug: SI-B001 Drug: Osimertinib |
Non-small Cell Lung Cancer | Sichuan Baili Pharmaceutical Co., Ltd. |
January 6, 2022 | Phase 2 Phase 3 |
| NCT05085054 | Not yet recruiting | Drug: Osimertinib Mesylate | Non Small Cell Lung Cancer | Wuhan Union Hospital, China | June 1, 2022 | Phase 2 |
| NCT05816252 | Recruiting | Drug: Osimertinib Drug: Carboplatin |
Non-small Cell Lung Cancer | Klus Pharma Inc. | April 19, 2023 | Phase 2 |
| NCT05085054 | Not yet recruiting | Drug: Osimertinib Mesylate | Non Small Cell Lung Cancer | Wuhan Union Hospital, China | June 1, 2022 | Phase 2 |
AZD9291 binding mode and structure.Cancer Discov.2014 Sep;4(9):1046-61. |
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Effect of AZD9291 on EGFR phosphorylationin vitro.Cancer Discov.2014 Sep;4(9):1046-61. |
In vivoanti-tumor efficacy of AZD9291 in subcutaneous xenograft models of EGFR-TKI sensitising and T790M resistant lung cancer.Cancer Discov.2014 Sep;4(9):1046-61. |
AZD9291 induces significant and sustained tumor regression in transgenic models of EGFR-TKI sensitising (C/L858R) and T790M resistant (C/L+T) lung cancer.Cancer Discov.2014 Sep;4(9):1046-61. |
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AZD9291 inhibits EGFR phosphorylation and downstream signallng in murine models of EGFR T790M resistant lung cancer.Cancer Discov.2014 Sep;4(9):1046-61. |
Proof of concept clinical studies validating AZD9291 as a mutant-selective EGFR kinase T790M inhibitor.Cancer Discov.2014 Sep;4(9):1046-61. |
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