An inhibitor of mutant EGFRs and an active metabolite of AZD 9291
Related Products
Isomer(s)
40753AZ 7550 (hydrochloride)
Parent Compound(s)
16237AZD 9291
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AZ 5104

Item No. 17994

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[2-[[2-(dimethylamino)ethyl]methylamino]-5-[[4-(1H-indol-3-yl)-2-pyrimidinyl]amino]-4-methoxyphenyl]-2-propenamide
CAS Number
1421373-98-9
Molecular Formula
C27H31N7O2
Formula Weight
485.6
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 30 mg/mlEthanol:PBS(pH 7.2) (1:1): 0.5 mg/ml
λmax
277, 313 nm
SMILES
CN(CCN(C)C)C1=C(NC(C=C)=O)C=C(NC2=NC=CC(C3=CNC4=C3C=CC=C4)=N2)C(OC)=C1
InChi Code
InChI=1S/C27H31N7O2/c1-6-26(35)30-22-15-23(25(36-5)16-24(22)34(4)14-13-33(2)3)32-27-28-12-11-21(31-27)19-17-29-20-10-8-7-9-18(19)20/h6-12,15-17,29H,1,13-14H2,2-5H3,(H,30,35)(H,28,31,32)
InChi Key
IQNVEOMHJHBNHC-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    5 mg

    $69

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    10 mg

    $127

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    25 mg

    $297

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    50 mg

    $525

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    Product Description

    AZ 5104 is an inhibitor of mutant EGFRs (IC50 = 2 nM for EGFRL858R/T790M and EGFRT790M for both) and an active metabolite of AZD 9291 (Item No. 16237).1 It is selective for these mutant EGFRs over wild-type EGFR (IC50 = 33 nM). AZ 5104 is formed from AZD 9291 by the cytochrome P450 (CYP) isoform CYP3A.2 It decreases proliferation of H1975 non-small cell lung cancer (NSCLC) cells containing the L858R activating and T790M resistance mutations (GI50 = 24 nM). AZ 5104 (2.5-10 mg/kg per day) reduces tumor growth in an H1975 mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Finlay, M.R., Anderton, M., Ashton, S., et al. Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor. J. Med. Chem. 57(20), 8249-8267 (2014).

    2. Dickinson, P.A., Vantarini, M.V., Collier, J., et al. Metabolic disposition of osimertinib in rats, dogs, and humans: Insights into a drug designed to bind covalently to a cysteine residue of epidermal growth factor receptor. Drug Metab. Dispos. 44(8), 1201-1212 (2016).