1. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Metabolic Enzyme/Protease
  2. EGFR IGF-1R Drug Metabolite
  3. AZ7550 hydrochloride

AZ7550 hydrochloride 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 hydrochloride Chemical Structure

AZ7550 hydrochloride Chemical Structure

CAS No. : 2309762-40-9

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

AZ7550 hydrochloride 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]

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

522.04

Formula

C27H32ClN7O2

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

C=CC(NC1=CC(NC2=NC=CC(C3=CN(C)C4=C3C=CC=C4)=N2)=C(OC)C=C1N(C)CCNC)=O.[H]Cl

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 : 1.88 mg/mL (3.60 mM; Need ultrasonic and warming; 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 1.9156 mL 9.5778 mL 19.1556 mL
5 mM --- --- ---
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 (sealed storage, away from moisture). 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)

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Purity & Documentation
References
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

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 (sealed storage, away from moisture). 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 1.9156 mL 9.5778 mL 19.1556 mL 47.8891 mL
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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.

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Product Name:
AZ7550 hydrochloride
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HY-B0794A
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