AZ7550

Name: AZ7550
Brand: MedChemExpress
SKU: HY-B0794
Rating: 5.0 (3 reviews)

Cat. No.: HY-B0794: Data Sheet
SDS
Handling Instructions
FAQs
Technical Support

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.

AZ7550 Chemical Structure

CAS No. : 1421373-99-0

Size	Stock	Quantity
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of AZ7550:

AZ7550 Mesylate In-stock
AZ7550-d₅ Get quote
AZ7550 hydrochloride Get quote

3 Publications Citing Use of MCE AZ7550

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EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

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]

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]
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

Molecular Weight

485.58

Formula

C₂₇H₃₁N₇O₂

CAS No.

1421373-99-0

Appearance

Solid

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

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)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

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Concentration _(final)

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In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

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μL

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Data Sheet (279 KB) SDS (252 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]

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].

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

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]

Complete Stock Solution Preparation Table

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

AZ7550 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AZ75501421373-99-0AZ 7550AZ-7550EGFRIGF-1RDrug MetaboliteEpidermal growth factor receptorErbB-1HER1Insulin-like growth factor-1 receptorInhibitorinhibitorinhibit

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AZ7550

Customer Review

Other Forms of AZ7550:

AZ7550 Related Antibodies

3 Publications Citing Use of MCE AZ7550

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All EGFR Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

AZ7550 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

AZ7550 Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

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