[CAS NO. 2319837-99-3] AZ7550 Mesylate

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Catalog:	HY-B0794B
Brand:	MCE
CAS:	2319837-99-3

Overview

MDL	-
Molecular Weight	773.90
Molecular Formula	C30H43N7O11S3
SMILES	CN1C=C(C2=NC(NC3=CC(NC(C=C)=O)=C(N(CCNC)C)C=C3OC)=NC=C2)C4=CC=CC=C41.O=S(O)(C)=O.O=S(O)(C)=O.O=S(O)(C)=O

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

1 Publications Citing Use of MCE

[1]Biopharm Drug Dispos. 2023 Jan 17.

Summary

AZ7550 Mesylate is an active metabolite of AZD9291 and inhibits the activity of IGF1R with an IC ₅₀ 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]

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 IC ₅₀ s 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 GI ₅₀ s of 19, 15, and 537 nM, respectively ^[1] .

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT02197234	AstraZeneca	Non Small Cell Lung Cancer	December 22, 2014	Phase 1
NCT02317016	AstraZeneca	Non Small Cell Lung Cancer	March 10, 2015	Phase 1
NCT02224053	AstraZeneca	Healthy Volunteer	September 2014	Phase 1
NCT02161770	AstraZeneca	Solid Tumours	December 22, 2014	Phase 1
NCT02163733	AstraZeneca	Advanced Non Small Cell Lung Cancer\|Advanced (Inoperable) Non Small Cell Lung Cancer	November 14, 2014	Phase 1
NCT02197247	AstraZeneca	Non Small Cell Lung Cancer	December 4, 2014	Phase 1

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 25 mg/mL ( 32.30 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.2922 mL	6.4608 mL	12.9216 mL
5 mM	0.2584 mL	1.2922 mL	2.5843 mL
10 mM	0.1292 mL	0.6461 mL	1.2922 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (3.23 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (3.23 mM); Clear solution

* All of the co-solvents are available by MCE.

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.

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