Home Metabolism Dehydrogenase inhibitor IDH-305 For research use only.

IDH-305

IDH-305 (Compound 13) is an orally available, mutant-selective and brain-penetrant inhibitor of isocitrate dehydrogenase 1 (IDH1) that targets IDH1(R132) mutation with IC50 of 27 nM, 28 nM and 6.14 μM for IDH1R132H, IDH1R132C and IDH1WT, respectively.

IDH-305 Chemical Structure

IDH-305 Chemical Structure

CAS: 1628805-46-8

Purity & Quality Control

Batch: S357401 DMSO] 98 mg/mL] false] Ethanol] 98 mg/mL] false] Water] Insoluble] false Purity: 99.20%
99.20

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Biological Activity

Description IDH-305 (Compound 13) is an orally available, mutant-selective and brain-penetrant inhibitor of isocitrate dehydrogenase 1 (IDH1) that targets IDH1(R132) mutation with IC50 of 27 nM, 28 nM and 6.14 μM for IDH1R132H, IDH1R132C and IDH1WT, respectively.
Targets
IDH1R132H [1]
(Cell-free assay)		 IDH1R132C [1]
(Cell-free assay)		 IDH1WT [1]
(Cell-free assay)
27 nM 28 nM 6.14 μM
In vitro
In vitro

IDH-305 inhibits HCT116-IDH1R132H/+ cells with an IC50 of 24 nM.[1]
Cell Research Cell lines MCF10A-IDH1R132H/+
Concentrations 0.001-10 μM
Incubation Time --
Method

--
In Vivo
In vivo

IDH-305 exhibits in vivo correlation of 2-HG reduction and efficacy in a patient-derived IDH1 mutant xenograft tumor model.[1]
Animal Research Animal Models Nu/nu mice of HMEX2838-IDH1R132C+/- PDX model
Dosages 30, 100, 300 mg/kg
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02987010 Withdrawn
Glioma
University of Texas Southwestern Medical Center
 January 2017 Phase 2

Chemical Information & Solubility

Molecular Weight 490.45 Formula

C23H22F4N6O2
CAS No. 1628805-46-8 SDF --
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 98 mg/mL ( (199.81 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 98 mg/mL

Water : 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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