country

Change Language

EN - English
FR - Français
DE - Deutsch
ES - Español
JA - 日本語
KO - 한국어

Country or Region:

United States

Product Name	Size / Unit Price	Qty

Total: USD 0.00 Checkout

Cat. No.: HY-B0793G

Copy Link Print Information

AZ-5104 (GMP)

AZ-5104 GMP is a GMP-grade form of AZ-5104 (HY-B0793). AZ-5104 is an orally active RORγ receptor-active compound, and also a circulating metabolite of AZD9291. AZ-5104 inhibits sensitizing EGFR mutants, EGFR^T790M drug-resistant EGFR mutants and wild-type EGFR, while showing no activity against the IGF-1R family. AZ-5104 can be used in the research of non-small cell lung cancer.

For research use only. We do not sell to patients.

CAS No.: 1421373-98-9
Formula: C₂₇H₃₁N₇O₂
Molecular Weight:485.58

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

AZ-5104 (GMP) Chemical Structure

CAS No.: 1421373-98-9

Price

Stock

Quantity

Amount: USD 0.00

* Please select Quantity before adding items.

Use of MCE Products

One-stop solution for XDC (ADC/PDC/RDC/ApDC/FDC/ISAC/VDC/SMDC)

Biological Activity
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

AZ-5104 GMP is a GMP-grade form of AZ-5104 (HY-B0793). AZ-5104 is an orally active RORγ receptor-active compound, and also a circulating metabolite of AZD9291. AZ-5104 inhibits sensitizing EGFR mutants, EGFR^T790M drug-resistant EGFR mutants and wild-type EGFR, while showing no activity against the IGF-1R family^[1]^[2]. AZ-5104 can be used in the research of non-small cell lung cancer^[2].

All ROR Isoforms :

All EGFR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
Calu-3	GI₅₀	58 nM Compound: 27	Cytotoxicity against human Calu3 cells assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay Cytotoxicity against human Calu3 cells assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay	[PMID: 25271963]
LoVo	IC₅₀	33 μM Compound: 27	Inhibition of wild type EGFR phosphorylation in human LoVo cells after 2 hrs by fluorescence assay Inhibition of wild type EGFR phosphorylation in human LoVo cells after 2 hrs by fluorescence assay	[PMID: 25271963]
LoVo	IC₅₀	33 nM Compound: AZ5104	Inhibition of wild type EGFR phosphorylation in human LoVo cells preincubated for 2 hrs followed by EGF stimulation measured after 30 mins by ELISA Inhibition of wild type EGFR phosphorylation in human LoVo cells preincubated for 2 hrs followed by EGF stimulation measured after 30 mins by ELISA	[PMID: 26968253]
LoVo	IC₅₀	33 nM Compound: 26	Antiproliferative activity against human LoVo cells harboring wild-type EGFR assessed as reduction in cell viability Antiproliferative activity against human LoVo cells harboring wild-type EGFR assessed as reduction in cell viability	[PMID: 38879996]
NCI-H1975	IC₅₀	2 μM Compound: 27	Inhibition of EGFR L858R/T790M double mutant phosphorylation in human NCI-H1975 cells after 2 hrs by fluorescence assay Inhibition of EGFR L858R/T790M double mutant phosphorylation in human NCI-H1975 cells after 2 hrs by fluorescence assay	[PMID: 25271963]
NCI-H1975	GI₅₀	16 nM Compound: 27	Cytotoxicity against human NCI-H1975 cells harboring EGFR L858R/T970M double mutant assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay Cytotoxicity against human NCI-H1975 cells harboring EGFR L858R/T970M double mutant assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay	[PMID: 25271963]
NCI-H1975	IC₅₀	2 nM Compound: 26	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as reduction in cell growth incubated for 72 hrs by CellTiter-Glo luminescent assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as reduction in cell growth incubated for 72 hrs by CellTiter-Glo luminescent assay	[PMID: 38879996]
PC-9	IC₅₀	2 μM Compound: 27	Inhibition of EGFR exon 19 deletion activating mutant phosphorylation in human PC9 cells after 2 hrs by fluorescence assay Inhibition of EGFR exon 19 deletion activating mutant phosphorylation in human PC9 cells after 2 hrs by fluorescence assay	[PMID: 25271963]
PC-9	GI₅₀	21 nM Compound: 27	Cytotoxicity against human PC9 cells harboring EGFR exon 19 deletion activating mutant assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay Cytotoxicity against human PC9 cells harboring EGFR exon 19 deletion activating mutant assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay	[PMID: 25271963]
PC-9	IC₅₀	2 nM Compound: AZ5104	Inhibition of EGFR Del ex19 mutant phosphorylation in human PC9 cells preincubated for 2 hrs by ELISA Inhibition of EGFR Del ex19 mutant phosphorylation in human PC9 cells preincubated for 2 hrs by ELISA	[PMID: 26968253]
PC-9	IC₅₀	2 nM Compound: 26	Antiproliferative activity against human PC-9 cells harboring EGFR del19 mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay Antiproliferative activity against human PC-9 cells harboring EGFR del19 mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay	[PMID: 38879996]

In Vitro

GMP-grade AZ-5104 potently inhibits the enzymatic activities of recombinant mutant and wild-type EGFR, and exhibits reduced selectivity for mutant EGFR compared with AZD9291^[2].
AZ-5104 GMP exhibits no significant activity against the IGF-1R receptor family in cellular assays^[2].
AZ-5104 GMP (incubated for 6 h) potently inhibits the phosphorylation of rare EGFR mutants (EGFR^G719S, EGFR^L861Q, exon 19 insertion mutation, EGFR^vIII) in transfected HEK293 cells, with activity superior to that of AZD9291, but exerts no inhibitory effect on EGFR exon 20 insertion mutation^[2].
AZ-5104 GMP exhibits stronger activity than AZD9291 in inhibiting HER2 phosphorylation in cellular assays^[2].
AZ-5104 GMP (2 nM-33 nM; 2 h) potently inhibits EGFR phosphorylation in PC-9, H1975 and LOVO human lung cancer cell lines, and exhibits reduced selectivity for mutant EGFR over wild-type EGFR compared with AZD9291^[2].
AZ-5104 GMP (administered for 3 days) exhibits stronger activity than AZD9291 in inhibiting the proliferation of EGFR-mutant and wild-type human lung cancer cell lines in vitro^[2].
AZ-5104 GMP exhibits greater potency than AZD9291 in inhibiting the growth and signal transduction of human lung cancer cells harboring HER2 exon 20 mutations^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

AZ-5104 GMP (5 mg/kg; p.o.; daily; 1 to 2 weeks) induces tumor shrinkage in EGFR^L858R-driven and EGFR^L858R+T790M-driven transgenic lung adenocarcinoma, with complete elimination of viable tumor tissue^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

bitransgenic CCSP-rtTA (C) mice with EGFRL858R (C/L858R) or EGFRL858R+T790M (C/L+T) genotypes (male and female, age ~3 weeks at induction start, tetracycline-inducible lung adenocarcinoma model induced by doxycycline-impregnated food pellets for ~3 months)^[2]
Dosage:

5 mg/kg
Administration:

p.o.; daily; 1 to 2 weeks
Result:

Induced tumor shrinkage, with no viable tumor detected on histological examination in C/L858R mice.
Induced significant tumor shrinkage, with no viable tumor detected on histological examination in C/L+T (EGFRL858R+T790M) mice, with more pronounced response after 2 weeks of treatment.

Chemical Information

CAS No. 1421373-98-9
Molecular Weight 485.58
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Nowak D, et al. Neural Networks in the Design of Molecules with Affinity to Selected Protein Domains. International journal of molecular sciences. 2023 Jan 16;24(2):1762. [Content Brief]

[2]. Cross DA, et al. AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer. Cancer discovery. 2014 Sep;4(9):1046-61. [Content Brief]

Calculators

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

Get Quote In-stock

Other size

Get Quote