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AZ-5104

🥰Excellent
Catalog No. T2491Cas No. 1421373-98-9

AZ5104 is a potent EGFR inhibitor.

AZ-5104

AZ-5104

🥰Excellent
Purity: 99.9%
Catalog No. T2491Cas No. 1421373-98-9
AZ5104 is a potent EGFR inhibitor.
Pack SizePriceAvailabilityQuantity
5 mg$48In Stock
10 mg$68In Stock
25 mg$125In Stock
50 mg$197In Stock
100 mg$265In Stock
200 mg$333In Stock
1 mL x 10 mM (in DMSO)$53In Stock
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Purity:99.9%
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Product Introduction

Bioactivity
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.
Chemical Properties
Molecular Weight485.58
FormulaC27H31N7O2
Cas No.1421373-98-9
SmilesCOc1cc(N(C)CCN(C)C)c(NC(=O)C=C)cc1Nc1nccc(n1)-c1c[nH]c2ccccc12
Relative Density.1.267 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -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
1mg5mg10mg50mg
1 mM2.0594 mL10.2970 mL20.5939 mL102.9696 mL
5 mM0.4119 mL2.0594 mL4.1188 mL20.5939 mL
10 mM0.2059 mL1.0297 mL2.0594 mL10.2970 mL
20 mM0.1030 mL0.5148 mL1.0297 mL5.1485 mL
DMSO
1mg5mg10mg50mg
50 mM0.0412 mL0.2059 mL0.4119 mL2.0594 mL
100 mM0.0206 mL0.1030 mL0.2059 mL1.0297 mL

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