AZ5104 |
| Catalog No.GC12955 |
EGFR inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1421373-98-9
Sample solution is provided at 25 µL, 10mM.
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AZ5104, is the demethylated metabolite of AZD-9291,is a potent EGFR inhibitor. IC50 <1 nM, 6 nM, 1 nM, 25 nM, for EGFR (L858R/T790M), EGFR (L858R), EGFR (L861Q), and EGFR (wildtype), respectively.
EGFR (epidermal growth factor receptor) is a receptor tyrosine kinase on the cell surface. The receptor activation leads to dimerization and tyrosine autophosphorylation. It induces downstream cellular responses such as modification in gene expression, cell proliferation and cytoskeletal rearrangement etc.
Compare to AZD9291, AZ5104 has somewhat more potency in mutant EGFR cell lines ex19del (2 nmol/L in PC-9), T790M (2 nmol/L in H1975), and wild-type EGFR (33 nmol/L in LOVO) cell lines. In a phenotypic assay, AZ5104 showed a greater potency across cell lines in a phenotypic assay.
3 hours after oral dosing in the mouse, the circulating active metabolites in plasma is 33% for AZ5104. In both C/L858R and C/L+T mice, 5 mg/kg/day dose of AZ5104, also show efficacy in shrinking tumors.
Reference:
1. Cross DA, Ashton SE, Ghiorghiu S et al. AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer. Cancer Discov. 2014 Sep;4(9):1046-61.
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Cell experiment: |
Cells were treated for 2 h with a dose-response of each drug (AZ-5104). Wild-type cells were stimulated for 10 minutes with 25 ng/mL of EGF before lysis. Level of EGFR phosphorylation was quantified in cell extracts using ELISA[1]. |
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References: [1]. Cross DA, et al. AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer. Cancer Discov. 2014 Sep;4(9):1046-61. |
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| Cas No. | 1421373-98-9 | SDF | |
| Chemical Name | (Z)-N-(5-((4-(1H-indol-3-yl)pyrimidin-2-yl)amino)-2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxyphenyl)acrylimidic acid | ||
| Canonical SMILES | C=C/C(O)=N/C1=CC(NC2=NC=CC(C3=CNC4=CC=CC=C34)=N2)=C(OC)C=C1N(CCN(C)C)C | ||
| Formula | C27H31N7O2 | M.Wt | 485.58 |
| Solubility | ≥ 16.95mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.0594 mL | 10.297 mL | 20.5939 mL |
| 5 mM | 0.4119 mL | 2.0594 mL | 4.1188 mL |
| 10 mM | 0.2059 mL | 1.0297 mL | 2.0594 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 15 reference(s) in Google Scholar.)
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