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Olutasidenib Dehydrogenase inhibitor

Name: Olutasidenib
Brand: Selleck Chemicals
SKU: S8949
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S8949

Olutasidenib is a potent, orally bioavailable, brain penetrant and selective mutant IDH1 (mIDH1) inhibitor with IC50 of 21.1 nM, 114 nM for IDH1-R132H, IDH1-R132C, respectively.

Chemical Structure

Molecular Weight: 354.79

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S894901 DMSO]71 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.97%

99.97

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Chemical Information, Storage & Stability

Molecular Weight	354.79	Formula	C₁₈H₁₅ClN₄O₂	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1887014-12-1	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	FT-2102			Smiles	CC(C1=CC2=C(C=CC(=C2)Cl)NC1=O)NC3=CC=C(N(C3=O)C)C#N

Solubility

In vitro
Batch:

DMSO : 71 mg/mL (200.11 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.550mg/ml (10.01mM)	Taking the 1 mL working solution as an example, add 50 μL of 71 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.590mg/ml (1.66mM)	Taking the 1 mL working solution as an example, add 50 μL of 11.8 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	IDH1 (R132H) ^[1] (Cell-free assay) 21.1 nM IDH1 (R132C) ^[1] (Cell-free assay) 114 nM
In vitro	Profiling in various mIDH1 over-expressing U87 cells and HCT116 cells reveals that olutasidenib potently inhibits 2-HG production by multiple IDH1-R132 mutants (R132H, R132C, R132G, R132L), suggesting this compound could be efficacious against most IDH1-R132 mutant-expressing tumors. It is highly selective for IDH1 isoforms, showing no appreciable inhibition against wild-type IDH1 and IDH2 mutants.^[1].
In vivo	In IDH1-R132H/ xenograft models, the free concentration of Olutasidenib is comparable in plasma and xenograft tumors, and exposures are dose-dependent. In comparison to the vehicle treated group, this compound shows a time and dose-dependent inhibition of 2-HG levels in tumor. Calculations based upon the percentage of suppression of 2-HG concentration in tumor versus the free drug concentration in tumor give in vivo IC50 values of 26 nM and 36 nM in the HCT116-IDH1-R132H or HCT116-IDH1-R132C models, respectively. This chemical has good cell permeability and low efflux ratio in the male CD-1 mouse, which indicate a low probability of p-glycoprotein driven efflux.^[1].
References	[1] https://pubmed.ncbi.nlm.nih.gov/31971798/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT06161974	Not yet recruiting	High Grade Glioma\|Astrocytoma\|Astrocytoma Grade III\|Astrocytoma Grade IV\|Diffuse Intrinsic Pontine Glioma\|WHO Grade III Glioma\|WHO Grade IV Glioma\|Metastatic Brain Tumor\|Diffuse Midline Glioma H3 K27M-Mutant\|Thalamus Tumor\|Spinal Tumor\|IDH1 Mutation\|IDH1 R132\|IDH1 R132C\|IDH1 R132H\|IDH1 R132S\|IDH1 R132G\|IDH1 R132L\|Oligodendroglioma	Rigel Pharmaceuticals\|Nationwide Children''s Hospital	June 2024	Phase 2

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