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AZ-5104

Catalog No. T2491   CAS 1421373-98-9

AZ5104 is a potent EGFR inhibitor.

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AZ-5104 Chemical Structure
AZ-5104, CAS 1421373-98-9
Pack Size Availability Price/USD Quantity
5 mg In stock $ 48.00
10 mg In stock $ 68.00
25 mg In stock $ 125.00
50 mg In stock $ 197.00
100 mg In stock $ 265.00
200 mg In stock $ 333.00
1 mL * 10 mM (in DMSO) In stock $ 53.00
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Purity: 99.9%
Purity: 99.59%
Purity: 98.45%
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Biological Description
Chemical Properties
Storage & Solubility Information
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

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 16 mg/mL(33 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 90 mg/mL (185.3 mM)

TargetMolReferences and Literature

1. Cross DA, et al. Cancer Discov. 2014, 4(9), 1046-1061.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Tyrosine Kinase Inhibitor Library Membrane Protein-targeted Compound Library Kinase Inhibitor Library Cysteine Covalent Library Bioactive Compounds Library Max Immunology/Inflammation Compound Library Anti-Colorectal Cancer Compound Library Anti-Liver Cancer Compound Library Anti-Breast Cancer Compound Library

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EAI045 Ligustroside EGFR/BRAFV600E-IN-3 Patritumab JCN037 Tyrphostin AG 112 EGFR mutant-IN-1 PD153035 hydrochloride

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Keywords

AZ-5104 1421373-98-9 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR AZ 5104 Epidermal growth factor receptor HER1 ErbB-1 inhibit AZ5104 Inhibitor inhibitor

 

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