Home Metabolism Dehydrogenase inhibitor DS-1001b (DS 1001)

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DS-1001b (DS 1001) Dehydrogenase inhibitor

Cat.No.S8881

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) Dehydrogenase inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 608.92

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Quality Control

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

Solubility

In vitro
Batch:

DMSO : 14 mg/mL (22.99 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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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.
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Chemical Information, Storage & Stability

Molecular Weight 608.92 Formula

C29H29Cl3FN3O4

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1898207-64-1 -- Storage of Stock Solutions

Synonyms DS-1001 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

Mechanism of Action

Targets/IC50/Ki
IDH1 R132X
In vitro

DS-1001b impairs the proliferation of IDH1 mutant chondrosarcoma cell lines and decreases 2-HG levels.
In vivo

Continuous administration of DS-1001b impairs tumor growth in xenograft mice.
References

Clinical Trial Information

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

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04458272 Active not recruiting
WHO Grade II Glioma
Daiichi Sankyo Co. Ltd.|Daiichi Sankyo
 July 8 2020 Phase 2
NCT03030066 Active not recruiting
Glioma
Daiichi Sankyo
 January 19 2017 Not Applicable

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