[CAS NO. 3038480-88-2] LWG-301
PRODUCTS SPECIFICATIONS [3038480-88-2]
DESCRIPTION [3038480-88-2]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 566.72 |
| Molecular Formula | C28H38N8O3S |
| SMILES | CCCCOC1=CC=CC(CC(NC2=NN=C(C=C2)N3CCC(CC3)NC4=NN=C(S4)NC(CCCC)=O)=O)=C1 |
Summary
LWG-301 is an allosteric inhibitor of Glutaminase 1 ( GLS1 ) with an IC 50 value of 7 nM. LWG-301 significantly block glutamine metabolism, increases intracellular ROS , thus induces apoptosis . LWG-301 exhibits moderate antitumor effects in HCT116 xenograft model [1] .
In Vitro
LWG-301 (compound 41a) inhibits HCT116 cancer cells growth with an IC
50
value of 61 nM
[1]
.
LWG-301 has great metabolic stability in human liver microsomes with T
1/2
=108 min, CL=32 μL/min/mg
[1]
.
LWG-301 (10 μM; 6 h) interacts with GLS1 protein in a dose- and time-dependent manner
[1]
.
LWG-301 (0.03-3 μM; 14 d) inhibits the colony formation of HCT116 cells in a concentration-dependent manner
[1]
.
LWG-301 (0.2 μM, 1 μM, 5 μM; 24 h) blocks the metabolism of glutamine thus results a decrease of glutamate, glutathione, and fumaric acid
[1]
.
LWG-301 (1-10 μM; 24 h) induces ROS production and (0.1-10 μM; 24 h) induces apoptosis in HCT116 cells
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Western Blot Analysis [1]
| Cell Line: | HCT116 cells |
| Concentration: | 0.001, 0.01, 0.1, 1, and 10 μM |
| Incubation Time: | 10, 30, 60, 180, 240 min |
| Result: | Showed the interaction with GLS1 in a dose- and time-dependent manner. |
Immunofluorescence [1]
| Cell Line: | HCT116 cells |
| Concentration: | 1, 5, and 10 μM |
| Incubation Time: | 6 hours |
| Result: | Induced ROS production in HCT116 cells. |
Apoptosis Analysis [1]
| Cell Line: | HCT116 cells |
| Concentration: | 0.1, 0.3, 1, 3, and 10 μM |
| Incubation Time: | 24 hours |
| Result: | Induced apoptosis in HCT116 cells |
In Vivo
LWG-301 (compound 41a) (100 mg/kg; i.p.; once daily for 20 d) shows anti-tumor activity without in HCT116 xenograft tumor model in mice
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | HCT116 tumor-bearing nude mice [1] |
| Dosage: | 100 mg/kg; |
| Administration: | Intraperitoneal injection; once a day for 20 days; |
| Result: |
Reduced tumor growth, resulting in 38.9% tumor growth inhibition.
Showed little toxicity on main organ. |
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.