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AZ5104 is a potent EGFR inhibitor.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 5 mg | $48 | In Stock | In Stock | |
| 10 mg | $68 | In Stock | In Stock | |
| 25 mg | $125 | In Stock | In Stock | |
| 50 mg | $197 | In Stock | In Stock | |
| 100 mg | $265 | In Stock | In Stock | |
| 200 mg | $333 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $53 | In Stock | In Stock |
| Description | AZ5104 is a potent EGFR inhibitor. |
| Targets&IC50 | EGFR (L858R):6 nM, ERB4:7 nM, EGFR (WT):25 nM, EGFR (L861Q):1 nM, EGFR (L858R/T790M):<1 nM |
| In vitro | AZ5104 shows great potency against ex19del (2 nM in PC-9), T790M (2 nM in H1975), and wild-type EGFR (33 nM in LOVO) cell lines. AZ5104 causes inhibition of cell viability with IC50 of 3.3 nM, 2.6 nM, 80 nM, and 53 nM for H1975 (T790M/L858R), PC-9 (ex19del), Calu 3 (WT), and NCI-H2073 (WT), respectively. [1] |
| In vivo | In both C/L858R and C/L+T mice, AZ5104 (5 mg/kg/d, p.o.) induces significant and sustained tumor regression. [1] |
| Kinase Assay | Recombinant Kinase assays: Kinase assays are performed using peptide or protein substrates in a filter-binding radioactive ATP transferase assay for protein kinases, or lipid substrates and HTRF assay for lipid kinase. |
| Molecular Weight | 485.58 |
| Formula | C27H31N7O2 |
| Cas No. | 1421373-98-9 |
| Smiles | COc1cc(N(C)CCN(C)C)c(NC(=O)C=C)cc1Nc1nccc(n1)-c1c[nH]c2ccccc12 |
| Relative Density. | 1.267 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||||||||||||
| Solubility Information | Ethanol: 16 mg/mL (32.95 mM), Sonication is recommended. H2O: < 1 mg/mL (insoluble or slightly soluble) DMSO: 90 mg/mL (185.35 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (6.8 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
DMSO
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