1. Metabolic Enzyme/Protease
  2. Isocitrate Dehydrogenase (IDH)

AGI-6780 

Cat. No.: HY-15734 Purity: 98.55%
Handling Instructions

AGI-6780 that potently and selectively inhibits the tumor-associated mutant IDH2R140Q with IC50 of 23±1.7 nM. AGI-6780 is less potent against IDH2WT with IC50 of 190±8.1 nM.

For research use only. We do not sell to patients.

AGI-6780 Chemical Structure

AGI-6780 Chemical Structure

CAS No. : 1432660-47-3

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 99 In-stock
Estimated Time of Arrival: December 31
5 mg USD 90 In-stock
Estimated Time of Arrival: December 31
10 mg USD 150 In-stock
Estimated Time of Arrival: December 31
50 mg USD 500 In-stock
Estimated Time of Arrival: December 31
100 mg USD 900 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

AGI-6780 that potently and selectively inhibits the tumor-associated mutant IDH2R140Q with IC50 of 23±1.7 nM. AGI-6780 is less potent against IDH2WT with IC50 of 190±8.1 nM.

IC50 & Target

IC50: 23±1.7 nM (IDH2R140Q), 190±8.1 nM (IDH2WT)[1]

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[1].

Solvent & Solubility
In Vitro: 

DMSO : ≥ 29 mg/mL (60.23 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0768 mL 10.3840 mL 20.7680 mL
5 mM 0.4154 mL 2.0768 mL 4.1536 mL
10 mM 0.2077 mL 1.0384 mL 2.0768 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[1]

AGI-6780 is prepared as 10 mM stock in DMSO and diluted to 50X final concentration in DMSO, for a 50 μL reaction mixture. IDH enzyme activity converting alpha-ketoglutarate to 2-hydroxyglutarate is measured using a NADPH depletion assay. In the assay the remaining cofactor is measured at the end of the reaction with the addition of a catalytic excess of diaphorase and resazurin, to generate a fluorescent signal in proportion to the amount of NADPH remaining. IDH enzyme activity in the direction of isocitrate to alpha-ketoglutarate conversion is measured by direct coupling of the NADPH production to conversion of resazurin to resorufin by diaphorase. In both cases, resorufin is measured fluorometrically at Ex544 Em590[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

Cells are sorted from fresh or frozen bone marrow aspirates and blood samples after labelling with PE-CD34, APC-CD38, PE-CD14, FITC-CD3 (clone HIT3a) and PECy7-CD19 (clone SJ25C1) antibodies using a MoFlow cell sorter. Unfractionated nucleated blood or bone marrow cells are plated in Methocult H4434 methylcellulose medium at 104 cells/dish, in duplicate dishes per condition. AGI-6780 (5 mM) is directly added to the medium. Dishes are incubated in a humidified incubator at 37°C and colonies containing at least 30 cells are counted after 13 days[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

481.51

Formula

C₂₁H₁₈F₃N₃O₃S₂

CAS No.

1432660-47-3

SMILES

O=S(C1=CC=C(C2=CSC=C2)C(NC(NC3=CC=CC(C(F)(F)F)=C3)=O)=C1)(NC4CC4)=O

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Purity: 98.55%

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Product Name:
AGI-6780
Cat. No.:
HY-15734
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AGI-6780

Cat. No.: HY-15734