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

Vorasidenib (Synonyms: AG-881)

Cat. No.: HY-104042 Purity: 99.87%
Handling Instructions

Vorasidenib (AG-881) is an orally available, brain penetrant second-generation dual mutant isocitrate dehydrogenases 1 and 2 (mIDH1/2) inhibitor. Vorasidenib (AG-881) exhibits nanomolar inhibition of (D)-2-hydroxyglutarate (D-2-HG), and the IC50 ranges of 0.04~22 nM against IDH1 R132C, IDH1 R132G, IDH1 R132H and IDH1 R132S and 7~14 nM against IDH2 R140Q and 130 nM against IDH2 R172K.

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

Vorasidenib Chemical Structure

Vorasidenib Chemical Structure

CAS No. : 1644545-52-7

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 137 In-stock
Estimated Time of Arrival: December 31
2 mg USD 90 In-stock
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5 mg USD 150 In-stock
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10 mg USD 250 In-stock
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50 mg USD 750 In-stock
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100 mg USD 1100 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Vorasidenib (AG-881) is an orally available, brain penetrant second-generation dual mutant isocitrate dehydrogenases 1 and 2 (mIDH1/2) inhibitor. Vorasidenib (AG-881) exhibits nanomolar inhibition of (D)-2-hydroxyglutarate (D-2-HG), and the IC50 ranges of 0.04~22 nM against IDH1 R132C, IDH1 R132G, IDH1 R132H and IDH1 R132S and 7~14 nM against IDH2 R140Q and 130 nM against IDH2 R172K[1][2].

IC50 & Target

IC50: 0.04~22 nM (IDH1 R132C, IDH1 R132G, IDH1 R132H, IDH1 R132S), 7~14 nM (IDH2 R140Q), 130 nM (IDH2 R172K)[2]

In Vitro

Vorasidenib has strong antiproliferative activity against human glioblastoma U-87 MG pLVX-IDH2 R140Q-neo, fibrosarcoma HT-1080 and neurosphere TS603 cells, all with IC50s of less than 50 nM[2].

Clinical Trial
Molecular Weight

414.74

Formula

C₁₄H₁₃ClF₆N₆

CAS No.

1644545-52-7

SMILES

C[[email protected]@H](NC1=NC(C2=NC(Cl)=CC=C2)=NC(N[[email protected]](C)C(F)(F)F)=N1)C(F)(F)F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (241.11 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4111 mL 12.0557 mL 24.1115 mL
5 mM 0.4822 mL 2.4111 mL 4.8223 mL
10 mM 0.2411 mL 1.2056 mL 2.4111 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 2.08 mg/mL (5.02 mM); Suspended solution; Need ultrasonic

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.08 mg/mL (5.02 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: 2.08 mg/mL (5.02 mM); Clear solution; Need warming

*All of the co-solvents are provided by MCE.
References

Purity: 99.87%

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Keywords:

VorasidenibAG-881AG881AG 881Isocitrate Dehydrogenase (IDH)Inhibitorinhibitorinhibit

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Vorasidenib
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