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

Olutasidenib (Synonyms: FT-2102)

Cat. No.: HY-114226 Purity: 98.35%
Handling Instructions

Olutasidenib (FT-2102) is a highly potent, orally active, brain penetrant and selective inhibitor of mutant Isocitrate dehydrogenase 1 (IDH1), with IC50 values of 21.2 nM and 114 nM for IDH1- R132H and IDH1- R132C, respectively . Olutasidenib (FT-2102) is under the study in the treatment of acute myeloid leukemia (AML) or myelodysplastic syndrome (MDS) .

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

Olutasidenib Chemical Structure

Olutasidenib Chemical Structure

CAS No. : 1887014-12-1

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10 mM * 1 mL in DMSO USD 275 In-stock
Estimated Time of Arrival: December 31
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10 mg USD 350 In-stock
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25 mg USD 700 In-stock
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50 mg USD 1100 In-stock
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100 mg USD 1800 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

Olutasidenib (FT-2102) is a highly potent, orally active, brain penetrant and selective inhibitor of mutant Isocitrate dehydrogenase 1 (IDH1), with IC50 values of 21.2 nM and 114 nM for IDH1- R132H and IDH1- R132C, respectively . Olutasidenib (FT-2102) is under the study in the treatment of acute myeloid leukemia (AML) or myelodysplastic syndrome (MDS) [1][2].

IC50 & Target

IC50: 21.2 nM (IDH1- R132H), 114 nM (IDH1- R132C)[2].

In Vitro

Olutasidenib (FT-2102) potently inhibits 2-HG production by multiple IDH1-R132 mutants (R132H, R132C, R132G, R132L), suggesting Olutasidenib (FT-2102) could be efficacious against most IDH1-R132 mutant-expressing tumors. Olutasidenib (FT-2102) is highly selective for IDH1 isoforms, showing no appreciable inhibition against wild-type IDH1 (> 20 µM) and IDH2 mutants (R172K and R140Q: both > 20 µM)[2].

In Vivo

Olutasidenib (FT-2102, three oral doses (12.5, 25, and 50 mg/kg) in 12-hour intervals) exhibits potent anti-tumor activity in HCT116-IDH1-R132H/+ xenograft bearing female BALB/c Nude mice[2].

Animal Model: HCT116-IDH1-R132H/+ xenograft bearing female BALB/c Nude mice[2].
Dosage: 12.5, 25, and 50 mg/kg.
Administration: Three oral doses (12.5, 25, and 50 mg/kg) in 12-hour intervals.
Result: Showed a time and dose-dependent inhibition of 2-HG levels in in tumor.
At the highest dose tested in these studies (50 mg/kg), treatment with FT-2102 inhibited 2-HG levels in the tumor by >90% for up to 24 hours after the last dose in the HCT116-IDH1-R132H/+ xenograft model.
Clinical Trial
Molecular Weight

354.79

Formula

C₁₈H₁₅ClN₄O₂

CAS No.

1887014-12-1

SMILES

N#CC1=CC=C(N[[email protected]](C2=CC3=C(NC2=O)C=CC(Cl)=C3)C)C(N1C)=O

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 : 125 mg/mL (352.32 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8186 mL 14.0928 mL 28.1857 mL
5 mM 0.5637 mL 2.8186 mL 5.6371 mL
10 mM 0.2819 mL 1.4093 mL 2.8186 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 (5.86 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (5.86 mM); Clear solution

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

OlutasidenibFT-2102FT2102FT 2102Isocitrate Dehydrogenase (IDH)2-HGmutantInhibitorinhibitorinhibit

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Olutasidenib
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HY-114226
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