Cat. No.: HY-B0794

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AZ7550

4 Cited Publications

Customer Review

Based on 4 publication(s) in Google Scholar

AZ7550 is an active metabolite of AZD9291 and inhibits the activity of IGF1R with an IC₅₀ of 1.6 μM.

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

Purity: 97.09%
CAS No.: 1421373-99-0
Formula: C₂₇H₃₁N₇O₂
Molecular Weight:485.58

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

AZ7550 Chemical Structure

CAS No.: 1421373-99-0

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Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Clinical Trial
Chemical Information
Publications (4)
Solvent & Solubility
- In Vitro
Protocol
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

AZ7550 is an active metabolite of AZD9291 and inhibits the activity of IGF1R with an IC₅₀ of 1.6 μM.

IC₅₀ & Target

IC50: 1.6 μM (IGF1R), 88 nM (MLK1), 156 nM (ACK1), 195 nM (ErbB4), 228 nM (MNK2), 302 nM (FLT3), 420 nM (ALK ), 449 nM (FES), 840 nM (IRR), 843 nM (BRK), 977 nM (BLK), 995 nM (FAK), 1256 nM (Ins R), 1317 nM (TEC), 1784 nM (FLT4), 2288 nM (PYK2), 2443 nM (Txk), 5104 nM (BTK)^[1]

All EGFR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
Calu-3	GI₅₀	537 nM Compound: 28	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	786 nM Compound: AZ7550	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	786 μM Compound: 28	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]
NCI-H1975	GI₅₀	19 nM Compound: 28	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	45 μM Compound: 28	Inhibition of EGFR L858R/T970M double mutant phosphorylation in human NCI-H1975 cells after 2 hrs by fluorescence assay Inhibition of EGFR L858R/T970M double mutant phosphorylation in human NCI-H1975 cells after 2 hrs by fluorescence assay	[PMID: 25271963]
NCI-H1975	IC₅₀	45 μM Compound: 28	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]
PC-9	GI₅₀	15 nM Compound: 28	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	26 nM Compound: AZ7550	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	26 μM Compound: 28	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]

In Vitro

AZ7550 (Compound 28) appeares to offer a broadly similar potency and selectivity profile to the parent compound AZD9291. AZ7550 inhibits double mutant (DM) cell line H1975, activating mutant (AM) cell line PC9, and wild type (WT) cell line LoVo with IC₅₀s of 45, 26, and 786 nM, respectively. AZ7550 inhibits DM antiproliferative cell line H1975, AM antiproliferative cell line PC9, and WT antiproliferative cell line Calu3 with GI₅₀s of 19, 15, and 537 nM, respectively^[1].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1421373-99-0
Appearance Solid
Molecular Weight 485.58
Formula C₂₇H₃₁N₇O₂
Color White to off-white
SMILES

C=CC(NC1=CC(NC2=NC=CC(C3=CN(C)C4=C3C=CC=C4)=N2)=C(OC)C=C1N(C)CCNC)=O
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (4)

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J Pharm Biomed Anal

Development and validation of an LC-MS/MS method for quantification of Osimertinib and its two metabolites AZ7550 and AZ5104 in human plasma including long-time storage. [Abstract]

2025 Jan 3:255:116662. PMID: 39787847
Biopharm Drug Dispos

Metabolism and pharmacokinetic study of deuterated osimertinib. [Abstract]

2023 Apr;44(2):165-174. PMID: 36649539
Patent

US20250275968A1.
bioRxiv

IGF-1 Peptide Mimetic-functionalized Hydrogels Enhance MSC Survival and Immunomodulatory Activity. [Abstract]

2024 Jul 2:2024.06.27.600680. PMID: 39005297

Solvent & Solubility

In Vitro:

DMSO : 83.33 mg/mL (171.61 mM; ultrasonic and adjust pH to 5 with 1 M HCl; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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Protocol

Kinase Assay^[1]

Biochemical enzyme profiling of AZD9291 and active metabolites across the kinome panel (single profiling experiment representative of two independent studies). % inhibition for kinases in the ~280 kinase panel that shows greater than 60% inhibition after 1 μM treatment with AZD9291, AZ5104 or AZ7550, and follow-up IC₅₀s where tested, are shown. Kinases with a conserved cysteine in the analogous position within their catalytic domain as Cys797 in EGFR are also shown, highlighted in bold^[1].

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Finlay MR, 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. 2014 Oct 23;57(20):8249-67. [Content Brief]

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.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0594 mL	10.2970 mL	20.5939 mL	51.4848 mL
	5 mM	0.4119 mL	2.0594 mL	4.1188 mL	10.2970 mL
	10 mM	0.2059 mL	1.0297 mL	2.0594 mL	5.1485 mL
	15 mM	0.1373 mL	0.6865 mL	1.3729 mL	3.4323 mL
	20 mM	0.1030 mL	0.5148 mL	1.0297 mL	2.5742 mL
	25 mM	0.0824 mL	0.4119 mL	0.8238 mL	2.0594 mL
	30 mM	0.0686 mL	0.3432 mL	0.6865 mL	1.7162 mL
	40 mM	0.0515 mL	0.2574 mL	0.5148 mL	1.2871 mL
	50 mM	0.0412 mL	0.2059 mL	0.4119 mL	1.0297 mL
	60 mM	0.0343 mL	0.1716 mL	0.3432 mL	0.8581 mL
	80 mM	0.0257 mL	0.1287 mL	0.2574 mL	0.6436 mL
	100 mM	0.0206 mL	0.1030 mL	0.2059 mL	0.5148 mL

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AZ7550

MCE Bioactive Compound Library

Clinical Compound Library Plus

Publications Citing Use of MedChemExpress (MCE) AZ7550

All EGFR Isoforms

Biological Activity

Chemical Information

Publications (4)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

AZ7550

MCE Bioactive Compound Library

Clinical Compound Library Plus

Publications Citing Use of MedChemExpress (MCE) AZ7550

All EGFR Isoforms

Biological Activity

Chemical Information

Publications (4)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

AZ7550 Related Classifications

Cat. No.: HY-B0794