research use only
Cat.No.S9711
| Related Targets | VEGFR PDGFR FGFR c-Met Src MEK CSF-1R FLT3 HER2 c-Kit |
|---|---|
| Other EGFR Inhibitors | Lazertinib (YH25448) Icotinib Hydrochloride Sunvozertinib AG-490 AG-1478 Canertinib (CI-1033) WZ4002 Rociletinib (CO-1686) Poziotinib (NOV120101, HM781-36B) Genistein |
| Molecular Weight | 669.72 | Formula | C31H34F3N9O3S |
Storage (From the date of receipt) | 3 years -20°C powder |
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| CAS No. | unknown | -- | Storage of Stock Solutions |
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In vitro |
DMSO
: 100 mg/mL
(149.31 mM)
Water : Insoluble Ethanol : Insoluble |
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In vivo |
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Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
| Targets/IC50/Ki |
EGFR
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|---|---|
| In vitro |
CH7233163 shows potent antitumor activities against tumour with EGFR-Del19/T790M/C797S in vitro. This compound potently inhibits the proliferation of Del19/T790M/C797S_NIH3T3 cells with IC50 of 20 nmol/L. It potently and dose-dependently blocks the EGFR phosphorylation in the Del19/T790M/C797S_NIH3T3 cells. This chemical can inhibit Del19/T790M/C797S signalling. |
| In vivo |
Pharmacodynamic study is performed using Del19/T790M/C797S_NIH3T3 xenografted tumours in mice. CH7233163 clearly inhibits EGFR phosphorylation after oral administration and potent tumour regression is observed. This compound has potent therapeutic efficacy against tumours with EGFR-Del19/T790M/C797S in vivo. |
References |
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