Home Metabolism Dehydrogenase inhibitor Olutasidenib For research use only.

Olutasidenib

Synonyms: FT-2102

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.

Olutasidenib Chemical Structure

Olutasidenib Chemical Structure

CAS: 1887014-12-1

Purity & Quality Control

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

Olutasidenib Related Products

Signaling Pathway

Dehydrogenase Signaling Pathways

Dehydrogenase Signaling Pathway

Choose Selective Dehydrogenase Inhibitors

Biological Activity

Description 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.
Targets
IDH1 (R132H) [1]
(Cell-free assay)		 IDH1 (R132C) [1]
(Cell-free assay)
21.1 nM 114 nM
In vitro
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 olutasidenib could be efficacious against most IDH1-R132 mutant-expressing tumors. Olutasidenib is highly selective for IDH1 isoforms, showing no appreciable inhibition against wild-type IDH1 and IDH2 mutants.[1].
In Vivo
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, Olutasidenib 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. Olutasidenib 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].
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 15 2024 Phase 2

Chemical Information & Solubility

Molecular Weight 354.79 Formula

C18H15ClN4O2

 
CAS No. 1887014-12-1 SDF --
Smiles CC(C1=CC2=C(C=CC(=C2)Cl)NC1=O)NC3=CC=C(N(C3=O)C)C#N
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 71 mg/mL ( (200.11 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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