Sunvozertinib

Storage temp: -20°C

Form: Solid

Color: Off-white to Light Brown

1. Cell Experiment​​

​​DMSO:​​ 50 mg/mL (85.60 mM; ultrasonic and warming to 80°C)

Preparing Stock Solutions：

​​

Please prepare the stock solution in the appropriate solvent based on the product's solubility in different solvents. Once dissolved, aliquot the solution to avoid product inactivation caused by repeated freeze-thaw cycles.

​​Storage method and shelf life of the stock solution:​​ -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use within 6 months; when stored at -20°C, please use within 1 month.

​​2. Animal Experiment​​

Please select the appropriate dissolution protocol based on your experimental animals and administration method. For the following protocols, first prepare a clear stock solution in vitro, then add co-solvents in sequence:

To ensure reliable experimental results, the clear stock solution can be stored appropriately according to the storage conditions. For in vivo experiments, it is recommended to prepare the working solution fresh and use it on the same day.

The percentages shown before the solvents refer to the volume percentage of each solvent in the final solution. If precipitation occurs during preparation, heating and/or sonication can be used to aid dissolution.

Protocol 1​​

Add each solvent in the following order: 10% DMSO, 40% PEG300, 5% Tween-80, 45% Saline.

​​Solubility:​​ ≥ 2.5 mg/mL (4.28 mM); Clear solution

This protocol yields a clear solution with a concentration of ≥ 2.5 mg/mL (saturation unknown).

​​Preparation example for a 1 mL working solution:​​

Take 100 μL of the 25.0 mg/mL clear DMSO stock solution and add it to 400 μL of PEG300, mix well. Then add 50 μL of Tween-80 to the mixture and mix thoroughly. Finally, add 450 μL of normal saline to bring the volume to 1 mL.

​​Protocol 2​​

Add each solvent in the following order: 10% DMSO, 90% (20% SBE-β-CD in Saline)

​​Solubility:​​ 2.5 mg/mL (4.28 mM); Suspended solution; Ultrasonic required

This protocol yields a homogeneous suspension at 2.5 mg/mL (4.28 mM), suitable for oral and intraperitoneal administration.

​​Preparation example for a 1 mL working solution:​​

Take 100 μL of the 25.0 mg/mL clear DMSO stock solution and add it to 900 μL of a 20% SBE-β-CD solution in saline, mix well.

​​Protocol 3​​

Add each solvent in the following order: 10% DMSO, 90% Corn Oil

​​Solubility:​​ ≥ 2.5 mg/mL (4.28 mM); Clear solution

This protocol yields a clear solution with a concentration of ≥ 2.5 mg/mL (saturation unknown). ​​This protocol is not suitable for experiments lasting longer than half a month.​​

​​Preparation example for a 1 mL working solution:​​

Take 100 μL of the 25.0 mg/mL clear DMSO stock solution and add it to 900 μL of corn oil, mix well.

Sunvozertinib exhibited anti-tumour activity against xenograft models of NSCLC with EGFR exon 20 insertion mutations.In EGFRexon20ins patient-derived xenograft models, sunvozertinib induced tumour regression.

Epidermal growth factor receptor (EGFR) is a transmembrane protein that is involved in growth factor signalling and is commonly expressed in non-small cell lung cancer (NSCLC) cells. EGFR exon 20 insertion mutations are found in about 2% of patients with NSCLC. Sunvozertinib is an irreversible and selective EGFR tyrosine kinase inhibitor with potent inhibition of EGFR exon 20 insertion mutants. Sunvozertinib is active against other EGFR mutations, including T790M mutations. It displays weak inhibitory activity against wild-type EGFR.