Size | Price | Stock | Qty |
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25mg |
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50mg |
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100mg |
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500mg |
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Other Sizes |
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Purity: ≥98%
Osimertinib (formerly AZD-9291 and mereletinib; trade name Tagrisso) is an oral bioavailable, irreversible/covalent, and mutant-selective EGFR inhibitor with potential antineoplastic activity. In LoVo cells, it inhibits WT EGFR, L858R/T790M EGFR, and Exon 19 deletion EGFR with IC50 values of 493.8 nM, 11.44, and 12.92 nM, respectively. Both the FDA and the European Commission approved it in 2017 for the treatment of cancer.
Targets |
EGFRL858R (IC50 = 12 nM); EGFRL858R/T790M (IC50 = 1 nM)
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ln Vitro |
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ln Vivo |
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Enzyme Assay |
In Corning black, clear-bottomed 384-well plates, 10,000 cells are seeded per well in growth medium, and the plates are then incubated for an entire night at 37°C with 5% CO2. Compounds are serially diluted in 100% DMSO and used to acoustically dose cells using an Echo 555. After aspirating the medium and incubating the plates for an additional two hours, 40μL of lysis buffer is added to each well. Greiner black high bind 384-well plates are blocked with 3% BSA after being coated with capture antibody. After the block is removed, 15μL of lysate is added to the Greiner black high bind 384-well plates, and the plates are incubated for two hours. Detection antibody (20μL) was added and the plates were incubated for two hours after aspiration and PBS washing. Aspiration and PBS washing are followed by the addition of 20μL of QuantaBlu fluorogenic peroxidase substrate and an hour of incubation. Add 20μL of QuantaBlu stop solution to each plate, and use an Envision plate reader to read the fluorescence at 352 nm for excitation and 460 nm for emission. A suitable software program is used to export the data obtained with each compound and perform curve fitting analysis. By calculating the compound concentration necessary to produce a 50% effect, an IC50 value is obtained from this data.
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Cell Assay |
In vitro, AZD9291 shows significant suppression of EGFR phosphorylation in EGFRm+ (e.g., PC9; < 25 nM) and EGFR m+/T790M (e.g., H1975; < 25 nM) cell lines, but much less activity against wild-type EGFR lines (e.g., LoVo; > 500 nM). In vitro, AZD9291 continuously demonstrated a much more powerful suppression of proliferation in mutant EGFR cell lines when compared to wild-type.
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Animal Protocol |
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References |
Molecular Formula |
C28H33N7O2
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Molecular Weight |
499.61
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Exact Mass |
499.27
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Elemental Analysis |
C, 67.31; H, 6.66; N, 19.62; O, 6.40
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CAS # |
1421373-65-0
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Related CAS # |
Osimertinib mesylate;1421373-66-1;Osimertinib-d6;1638281-44-3;Osimertinib dimesylate;2070014-82-1;Osimertinib-13C,d3;2254100-49-5
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Appearance |
Brown to yellow solid powder
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SMILES |
CN1C=C(C2=CC=CC=C21)C3=NC(=NC=C3)NC4=C(C=C(C(=C4)NC(=O)C=C)N(C)CCN(C)C)OC
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InChi Key |
DUYJMQONPNNFPI-UHFFFAOYSA-N
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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)
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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
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Synonyms |
AZD-9291; AZD9291; AZD 9291; Osimertinib free base; Mereletinib; 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 |
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) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.0016 mL | 10.0078 mL | 20.0156 mL | |
5 mM | 0.4003 mL | 2.0016 mL | 4.0031 mL | |
10 mM | 0.2002 mL | 1.0008 mL | 2.0016 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 |
NCT04413201 | Active Recruiting |
Drug: Afatinib Drug: Osimertinib |
Non-squamous NSCLC | Michael Hopp | September 11, 2020 | Phase 4 |
NCT04908956 | Active Recruiting |
Drug: Osimertinib Radiation: SBRT |
EGFR Gene Mutation NSCLC Stage IV |
ETOP IBCSG Partners Foundation | August 4, 2022 | Phase 2 |
NCT03535363 | Active Recruiting |
Drug: Osimertinib | NSCLC Non-small Cell Lung Cancer |
Case Comprehensive Cancer Center | October 26, 2018 | Phase 1 |
NCT03667820 | Active Recruiting |
Drug: Osimertinib Radiation: SABR |
Non-small Cell Lung Cancer (NSCLC) |
University of Texas Southwestern Medical Center |
September 26, 2018 | Phase 2 |
NCT04563871 | Active Recruiting |
Drug: 80mg Osimertinib | Non-small Cell Lung Cancer (NSCLC) |
Samsung Medical Center | November 17, 2020 | Phase 2 |
AZD9291 binding mode and structure.Cancer Discov.2014 Sep;4(9):1046-61. td> |
Effect of AZD9291 on EGFR phosphorylationin vitro.Cancer Discov.2014 Sep;4(9):1046-61. td> |
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. td> |
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. td> |
AZD9291 inhibits EGFR phosphorylation and downstream signallng in murine models of EGFR T790M resistant lung cancer.Cancer Discov.2014 Sep;4(9):1046-61. td> |
Proof of concept clinical studies validating AZD9291 as a mutant-selective EGFR kinase T790M inhibitor.Cancer Discov.2014 Sep;4(9):1046-61. td> |