1. Protein Tyrosine Kinase/RTK
  2. IGF-1R
  3. AZ7550 Mesylate

AZ7550 Mesylate (Synonyms: AZ7550 trimesylate salt)

Cat. No.: HY-B0794B Purity: 98.85%
Handling Instructions

AZ7550 Mesylate 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 Mesylate Chemical Structure

AZ7550 Mesylate Chemical Structure

Size Price Stock Quantity
5 mg USD 280 In-stock
Estimated Time of Arrival: December 31
10 mg USD 440 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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Other Forms of AZ7550 Mesylate:

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Description

AZ7550 Mesylate 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].

Clinical Trial
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 : 4.18 mg/mL (5.40 mM; Need ultrasonic and warming)

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.
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
Molecular Weight

773.90

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

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
AZ7550 Mesylate
Cat. No.:
HY-B0794B
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AZ7550 Mesylate

Cat. No.: HY-B0794B