AGI-6780 (Synonyms: AGI 6780;AGI6780) |
| カタログ番号GC14757 |
突然変異IDH2の強力で選択的な阻害剤
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1432660-47-3
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');)
;)
AGI-6780 is a potent and selective inhibitor of tumor-associated IDH2/R140Q mutation with IC50 value of 23 nM [1].
AGI-6780 could significantly reduce intracellular concentration of 2HG in the human glioblastoma TF1/R140Q cells, as well as reverse IDH2/R140Q-mediated differentiation block in TF1 cells in the presence of EPO. AGI-6780 could restore KLF1 and hemoglobin G1/2 expressions in the EPO-induced TF1/R140Q cells [1].
References:
[1] Wang F1, Travins J, DeLaBarre B, Penard-Lacronique V, Schalm S, Hansen E, Straley K, Kernytsky A, Liu W, Gliser C, Yang H, Gross S, Artin E, Saada V,Mylonas E, Quivoron C, Popovici-Muller J, Saunders JO, Salituro FG, Yan S, Murray S, Wei W, Gao Y, Dang L, Dorsch M, Agresta S, Schenkein DP, Biller SA, Su SM, de Botton S, Yen KE. Targeted inhibition of mutant IDH2 in leukemia cells induces cellular differentiation. Science. 2013 May 3;340(6132):622-6.
| Cell experiment [1]: | |
|
Cell lines |
Primary human AML cells |
|
Preparation method |
The solubility of this compound in DMSO is > 22.25 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
|
Reacting condition |
5 μM up to 10 days |
|
Applications |
IDH2 mutant samples treated with AGI-6780 showed a dose-dependent reduction in the amounts of extracellular and intracellular (R)-2-hydroxyglutarate. In the presence AGI-6780, a burst of cell proliferation was also observed only in the IDH2/R140Q mutant samples. Furthermore, AGI-6780 did not exert a cytotoxic effect as the number of viable, more mature CD45-positive cells increased in the presence of AGI-6780 only in the IDH2/R140Q mutant samples whereas the IDH2/WT samples remained unchanged. |
|
References: [1] Wang F1,Travins J,DeLaBarre B,Penard-Lacronique V,Schalm S,Hansen E,Straley K,Kernytsky A,Liu W,Gliser C,Yang H,Gross S,Artin E,Saada V,Mylonas E,Quivoron C,Popovici-Muller J,Saunders JO,Salituro FG,Yan S,Murray S,Wei W,Gao Y,Dang L,Dorsch M,Agresta S,Schenkein DP,Biller SA,Su SM,de Botton S,Yen KE. Targeted inhibition of mutant IDH2 in leukemia cells induces cellular differentiation. Science.2013 May 3;340(6132):622-6. |
|
| Cas No. | 1432660-47-3 | SDF | |
| 同義語 | AGI 6780;AGI6780 | ||
| Chemical Name | 1-[5-(cyclopropylsulfamoyl)-2-thiophen-3-ylphenyl]-3-[3-(trifluoromethyl)phenyl]urea | ||
| Canonical SMILES | C1CC1NS(=O)(=O)C2=CC(=C(C=C2)C3=CSC=C3)NC(=O)NC4=CC=CC(=C4)C(F)(F)F | ||
| Formula | C21H18F3N3O3S2 | M.Wt | 481.51 |
| 溶解度 | ≥ 22.25 mg/mL in DMSO, ≥ 100.8 mg/mL in EtOH | Storage | Store at -20°C |
| 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 | 2.0768 mL | 10.384 mL | 20.768 mL |
| 5 mM | 0.4154 mL | 2.0768 mL | 4.1536 mL |
| 10 mM | 0.2077 mL | 1.0384 mL | 2.0768 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: >98.00%
- 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 *