ASCT2-IN-2 |
| Catalog No.GC74030 |
ASCT2-IN-2 (composé 25e) est un inhibiteur d’asct2 avec une ci50 de 5,14 μM.
Products are for research use only. Not for human use. We do not sell to patients.
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
ASCT2-IN-2 (compound 25e) is an ASCT2 inhibitor with IC50 of 5.14 μM. ASCT2-IN-2 regulates amino acid metabolism as well as mTOR signaling and thereby induces cell apoptosis. ASCT2-IN-2 inhibits tumor growth.
ASCT2-IN-2 (50 μM, 15 min) inhibits Glutamine (Gln) uptake in cells A549 and HEK293 (Gln inhibition ratio 55.62% and 98.31%) by targeting hASCT2, with IC50 values of 5.6 μM and 3.5 μM, respectively[1]. ASCT2-IN-2 (0-50 μM, 15 min) improves metabolic stability in murine liver microsome, with a half-time of 166.51 min and a clearance of 8.27 μL/min•mg[1].ASCT2-IN-2 (0-50 μM, 15 min) improves activity of LAT1 and thereby promotes leucine uptake in A549 cells[1].ASCT2-IN-2 (5-10 μM, 24 h) inhibits Gln metabolism, upregulates the ROS production and thereby induces apoptosis in cell A549[1].ASCT2-IN-2 (5-10 μM, 24 h) inhibits AKT phosphorylation and mTORC1 activity under starvation, promotes cell autophagy[1].ASCT2-IN-2 (5-10 μM, 24 h) dose-dependently inhibits proliferation in A549[1].ASCT2-IN-2 (0-10 nM, 96 h) inhibits organoid proliferation of drug resistant NSCLCs in cells H1975 OR and HCC827 OR [1].
ASCT2-IN-2 (i.p.;25 or 50 mg/kg, once every two days for 3 weeks) inhibits tumor growth with a TGI of 70% in A549 Xenograft Model in BALB/c mice[1].Pharmacokinetic Analysis of ASCT2-IN-2 in Sprague-Dawley rats[1]
References:
[1]. Qin L et al., Discovery of Novel Aminobutanoic Acid-Based ASCT2 Inhibitors for the Treatment of Non-Small-Cell Lung Cancer. J Med Chem. 2024 Jan 13. doi: 10.1021/acs.jmedchem.3c01093
| Cas No. | SDF | ||
| Formula | C44H50N2O4 | M.Wt | 670.88 |
| Solubility | DMSO : ≥ 150 mg/mL (223.59 mM) | Storage | -20°C, protect from light, stored under nitrogen |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.4906 mL | 7.4529 mL | 14.9058 mL |
| 5 mM | 0.2981 mL | 1.4906 mL | 2.9812 mL |
| 10 mM | 0.1491 mL | 0.7453 mL | 1.4906 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *