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AGI-6780
CAS No. 1432660-47-3
AGI-6780( AGI6780 | AGI 6780 | AGI-6780 )
Catalog No. M11841 CAS No. 1432660-47-3
AGI-6780 is a potent and selective inhibitor of IDH2 R140Q mutant with IC50 of 23 nM.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 2MG | 40 | In Stock |
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| 5MG | 65 | In Stock |
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| 10MG | 110 | In Stock |
|
| 25MG | 209 | In Stock |
|
| 50MG | 372 | In Stock |
|
| 100MG | 556 | In Stock |
|
| 500MG | 1197 | In Stock |
|
| 1G | Get Quote | In Stock |
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Biological Information
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Product NameAGI-6780
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NoteResearch use only, not for human use.
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Brief DescriptionAGI-6780 is a potent and selective inhibitor of IDH2 R140Q mutant with IC50 of 23 nM.
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DescriptionAGI-6780 is a potent and selective inhibitor of IDH2 R140Q mutant with IC50 of 23 nM.(In Vitro):AGI-6780 is tested in both human glioblastoma U87 and TF-1 cells expressing IDH2R140Q, as well as against IDH1R132H for 48 h incubation, with IC50 of 11±2.6 nM, 18±0.51 nM, and >1 mM, respectivly.Treatment of TF-1R140Q cells with AGI-6780, at concentrations that lower 2HG to near-normal physiologic levels, restore expression of both HBG and KLF1 genes and the color change associated with differentiation. AGI-6780 can reverse the IDH2R140Q-induced differentiation block in TF-1 cells. Pretreatment with AGI-6780 (0.2 μM and 1 μM) markedly decreased the intracellular concentration of (R)-2-hydroxyglutarate in the TF1R140Q cells and restored their ability to undergo EPO-induced differentiation.
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In VitroAGI-6780 is tested in both human glioblastoma U87 and TF-1 cells expressing IDH2R140Q, as well as against IDH1R132H for 48 h incubation, with IC50 of 11±2.6 nM, 18±0.51 nM, and >1 mM, respectivly.Treatment of TF-1R140Q cells with AGI-6780, at concentrations that lower 2HG to near-normal physiologic levels, restore expression of both HBG and KLF1 genes and the color change associated with differentiation. AGI-6780 can reverse the IDH2R140Q-induced differentiation block in TF-1 cells. Pretreatment with AGI-6780 (0.2 μM and 1 μM) markedly decreased the intracellular concentration of (R)-2-hydroxyglutarate in the TF1R140Q cells and restored their ability to undergo EPO-induced differentiation.
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In Vivo——
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SynonymsAGI6780 | AGI 6780 | AGI-6780
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PathwayMetabolic Enzyme/Protease
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TargetDehydrogenase
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RecptorIDH2 R140Q mutant
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Research AreaCancer
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Indication——
Chemical Information
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CAS Number1432660-47-3
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Formula Weight481.51
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Molecular FormulaC21H18F3N3O3S2
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Purity>98% (HPLC)
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SolubilityEthanol: 96 mg/mL (199.37 mM); DMSO: 96 mg/mL (199.37 mM)
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SMILESO=S(C1=CC=C(C2=CSC=C2)C(NC(NC3=CC=CC(C(F)(F)F)=C3)=O)=C1)(NC4CC4)=O
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Chemical NameN-cyclopropyl-4-(thiophen-3-yl)-3-(3-(3-(trifluoromethyl)phenyl)ureido)benzenesulfonamide
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1.Wang F, et al. Science. 2013 May 3;340(6132):622-6.
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