research use only
Cat.No.S8764
| Related Targets | CXCR Nrf2 Mitophagy LRRK2 ULK FKBP Heme Oxygenase cGAS LC3 Cell wall |
|---|---|
| Other Autophagy Inhibitors | Resveratrol (trans-Resveratrol) Spautin-1 PIK-III DC661 Lys05 Autophinib Spermidine SMER28 EN6 Flubendazole |
|
In vitro |
DMSO
: 100 mg/mL
(207.24 mM)
Water : Insoluble Ethanol : Insoluble |
|
In vivo |
|||||
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.
| Molecular Weight | 482.51 | Formula | C26H23FN8O |
Storage (From the date of receipt) | 3 years -20°C powder |
|---|---|---|---|---|---|
| CAS No. | 1807988-47-1 | -- | Storage of Stock Solutions |
|
|
| Synonyms | N/A | Smiles | C1COCCN1C2=NC(=NC(=N2)NC3=CC=C(C=C3)F)NC4=CC=C(C=C4)C5=NC6=CC=CC=C6N5 | ||
| Targets/IC50/Ki |
Autophagy
|
|---|---|
| In vitro |
Treatment with IITZ-01 results in the vacuolated appearance of cells due to its specific accumulation in lysosomes. It deacidifies lysosomes and inhibits maturation of lysosomal enzymes leading to lysosomal dysfunction. This compound enhances autophagosome accumulation but inhibits autophagosomal degradation by impairing lysosomal function, finally resulting in the inhibition of autophagy. It also abolishes mitochondrial membrane potential and triggered apoptosis through the mitochondria-mediated pathway. In in-vitro screening assays, this chemical shows negligible inhibition toward PI3K γ (IC50: 2.62 μM) and no significant inhibition at 10 μM against mTORC1. Immunoblotting experiment has revealed no significant decrease in p-AKT levels in breast cancer cells when treated with this agent. It can trigger apoptosis via disrupting MMP and modulating Bcl-2 and IAP family proteins. |
| In vivo |
This compound displays potent antitumor action in vivo through autophagy inhibition and apoptosis induction in MDA-MB-231 breast cancer xenograft model. |
References |
Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.