Home Metabolism Dehydrogenase inhibitor DS-1001b (DS 1001) For research use only.

DS-1001b (DS 1001)

Synonyms: DS-1001

DS-1001b is an oral selective inhibitor of mutant IDH1 R132X with potential antineoplastic activity and is designed to penetrate the blood-brain barrier.

DS-1001b (DS 1001) Chemical Structure

DS-1001b (DS 1001) Chemical Structure

CAS: 1898207-64-1

Purity & Quality Control

Batch: S888101 DMSO] 14 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.74%
99.74

DS-1001b (DS 1001) Related Products

Signaling Pathway

Dehydrogenase Signaling Pathways

Dehydrogenase Signaling Pathway

Choose Selective Dehydrogenase Inhibitors

Biological Activity

Description DS-1001b is an oral selective inhibitor of mutant IDH1 R132X with potential antineoplastic activity and is designed to penetrate the blood-brain barrier.
Targets
IDH1 R132X [1]
In vitro
In vitro

DS-1001b impairs the proliferation of IDH1 mutant chondrosarcoma cell lines and decreases 2-HG levels.[2]
Cell Research Cell lines JJ012,L835 cell lines
Concentrations 0-10µM
Incubation Time 72 h
Method

Cells are maintained in RPMI1640 supplemented with 10% fetal bovine serum and 1% penicillin/streptomycin (P/S). Cells are grown at 37 °C in a humidified incubator with 95% air and 5% CO2. Then cells are treated with DS-1001b for 72 hours.
In Vivo
In vivo

Continuous administration of DS-1001b impairs tumor growth in xenograft mice.[2]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04458272 Active not recruiting
WHO Grade II Glioma
Daiichi Sankyo Co. Ltd.|Daiichi Sankyo Inc.
 July 8 2020 Phase 2
NCT03030066 Active not recruiting
Glioma
Daiichi Sankyo Co. Ltd.|Daiichi Sankyo Inc.
 January 19 2017 Not Applicable

Chemical Information & Solubility

Molecular Weight 608.92 Formula

C29H29Cl3FN3O4
CAS No. 1898207-64-1 SDF --
Smiles CC1=CN(C2=CC=CC(=C12)C=CC(=O)O)C(=O)C3=C(ON=C3C4=C(C=C(C=C4Cl)Cl)Cl)C(C)(C)F.CC(C)(C)N
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 14 mg/mL ( (22.99 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
Batch:

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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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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.

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.

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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