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

Olutasidenib  (Synonyms: FT-2102)

Cat. No.: HY-114226 Purity: 99.30%
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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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Solid + Solvent
10 mM * 1 mL in DMSO
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 USD 231 In-stock
Solution
10 mM * 1 mL in DMSO USD 231 In-stock
Solid
5 mg USD 210 In-stock
10 mg USD 340 In-stock
25 mg USD 620 In-stock
50 mg USD 950 In-stock
100 mg USD 1500 In-stock
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Based on 1 publication(s) in Google Scholar

Olutasidenib Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Olutasidenib

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IDH1 IDH2

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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

IDH1

 

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].

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

Olutasidenib Related Antibodies
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].

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

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.
Appearance

Solid

Color

Light yellow to yellow

SMILES

N#CC1=CC=C(N[C@H](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 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (352.32 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8186 mL 14.0928 mL 28.1857 mL 70.4642 mL
5 mM 0.5637 mL 2.8186 mL 5.6371 mL 14.0928 mL
10 mM 0.2819 mL 1.4093 mL 2.8186 mL 7.0464 mL
15 mM 0.1879 mL 0.9395 mL 1.8790 mL 4.6976 mL
20 mM 0.1409 mL 0.7046 mL 1.4093 mL 3.5232 mL
25 mM 0.1127 mL 0.5637 mL 1.1274 mL 2.8186 mL
30 mM 0.0940 mL 0.4698 mL 0.9395 mL 2.3488 mL
40 mM 0.0705 mL 0.3523 mL 0.7046 mL 1.7616 mL
50 mM 0.0564 mL 0.2819 mL 0.5637 mL 1.4093 mL
60 mM 0.0470 mL 0.2349 mL 0.4698 mL 1.1744 mL
80 mM 0.0352 mL 0.1762 mL 0.3523 mL 0.8808 mL
100 mM 0.0282 mL 0.1409 mL 0.2819 mL 0.7046 mL
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Olutasidenib Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Olutasidenib1887014-12-1FT-2102FT2102FT 2102Isocitrate Dehydrogenase (IDH)2-HGmutantInhibitorinhibitorinhibit

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