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AZ5104 is a potent EGFR inhibitor.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $48 | In Stock | |
10 mg | $68 | In Stock | |
25 mg | $125 | In Stock | |
50 mg | $197 | In Stock | |
100 mg | $265 | In Stock | |
200 mg | $333 | In Stock | |
1 mL x 10 mM (in DMSO) | $53 | In Stock |
Description | AZ5104 is a potent EGFR inhibitor. |
Targets&IC50 | EGFR (L861Q):1 nM, EGFR (L858R):6 nM, ERB4:7 nM, EGFR (WT):25 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. | ||||||||||||||||||||||||||||||||||||||||
Solubility Information | Ethanol: 16 mg/mL (33 mM) H2O: < 1 mg/mL (insoluble or slightly soluble) DMSO: 90 mg/mL (185.3 mM) | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
DMSO
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