| Size | Price | Stock | Qty |
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| 5mg |
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| 25mg |
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Purity: ≥98%
AZ7550 Mesylate (AZ-7550), the mesylate salt of AZ 7550, is an active metabolite of AZD-9291 (Osimertinib) by removing one of the methyl groups from the ethyl diamine side chain. AZD 9291 (Osimertinib) was approved in 2015 for the treatment of non-small-cell lung cancer (NSCLC) in patients harboring sensitizing (or activating) mutations for a number of years.
| ln Vitro |
In terms of potency and selectivity, AZ7550 (compound 28) seems to offer properties that are largely comparable to those of the parent molecule AZD9291. The DM cell line H1975, the AM cell line PC9, and the WT cell line LoVo are all inhibited by AZ7550, with IC50 values of 45, 26, and 786 nM, respectively. The anti-proliferative cell lines H1975 from DM, PC9 from AM, and Calu3 from WT are all inhibited by AZ7550, with GI50 values of 19, 15, and 537 nM, respectively[1].
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| 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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| Molecular Formula |
C28H35N7O5S
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| Molecular Weight |
581.686404466629
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| CAS # |
2319837-99-3
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| Related CAS # |
AZ7550;1421373-99-0;AZ7550 hydrochloride;2309762-40-9
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| 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
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| Synonyms |
AZ7550 Mesylate; AZ 7550; AZ-7550
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~25 mg/mL (~32.30 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.23 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (3.23 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7191 mL | 8.5956 mL | 17.1913 mL | |
| 5 mM | 0.3438 mL | 1.7191 mL | 3.4383 mL | |
| 10 mM | 0.1719 mL | 0.8596 mL | 1.7191 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
AZD9291 binding mode and structure.Cancer Discov.2014 Sep;4(9):1046-61. |
Effect of AZD9291 on EGFR phosphorylationin vitro.Cancer Discov.2014 Sep;4(9):1046-61. |
In vivoanti-tumor efficacy of AZD9291 in subcutaneous xenograft models of EGFR-TKI sensitising and T790M resistant lung cancer.Cancer Discov.2014 Sep;4(9):1046-61. |
AZD9291 induces significant and sustained tumor regression in transgenic models of EGFR-TKI sensitising (C/L858R) and T790M resistant (C/L+T) lung cancer.Cancer Discov.2014 Sep;4(9):1046-61. |
AZD9291 inhibits EGFR phosphorylation and downstream signallng in murine models of EGFR T790M resistant lung cancer.Cancer Discov.2014 Sep;4(9):1046-61. |
Proof of concept clinical studies validating AZD9291 as a mutant-selective EGFR kinase T790M inhibitor.Cancer Discov.2014 Sep;4(9):1046-61. |
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