[CAS NO. 1421373-98-9] AZ5104
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PRODUCTS SPECIFICATIONS [1421373-98-9]
Store
Catalog
SLK-S7298
Brand
Selleck
CAS
1421373-98-9
DESCRIPTION [1421373-98-9]
Overview
| MDL | MFCD28899992 |
|---|---|
| Molecular Weight | 485.58 |
| Molecular Formula | C27H31N7O2 |
| SMILES | C=CC(NC1=CC(NC2=NC=CC(C3=CNC4=C3C=CC=C4)=N2)=C(OC)C=C1N(CCN(C)C)C)=O |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0594 mL | 10.2970 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 |
| 50 mM | 0.0412 mL | 0.2059 mL | 0.4119 mL |
Description
AZ5104, the demethylated metabolite of AZD-9291, is a potent inhibitor with of <1 nM, 6 nM, 1 nM, and 25 nM for EGFR (L858R/T790M), EGFR (L858R), EGFR (L861Q), and EGFR (wildtype), respectively. Phase 1.
Targets
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.
In vivo
In both C/L858R and C/L+T mice, AZ5104 (5 mg/kg/d, p.o.) induces significant and sustained tumor regression.
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