Home Protein Tyrosine Kinase CSF-1R inhibitor Chiauranib

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Chiauranib CSF-1R inhibitor

Cat.No.E0616

Chiauranib (CS2164) selectively inhibits multiple kinase targets aurora B kinase (AURKB), colony-stimulating factor 1 receptor (CSF1R), and vascular endothelial growth factor receptor (VEGFR)/platelet-derived growth factor receptor (PDGFR)/c-Kit , thereby inhibiting the rapid proliferation of tumor cells, enhancing the antitumor immunity, and inhibiting tumor angiogenesis, to achieve the anti-tumor efficacy.
Chiauranib CSF-1R inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 435.5

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Quality Control

Batch: E061601 DMSO]87 mg/mL]false]Ethanol]10 mg/mL]false]Water]Insoluble]false Purity: 99.49%
99.49

Solubility

In vitro
Batch:

DMSO : 87 mg/mL (199.77 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 10 mg/mL

Water : 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 435.5 Formula

C27H21N3O3

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1256349-48-0 -- Storage of Stock Solutions

Synonyms CS2164 Smiles COC1=CC2=C(C=C1)C(=CC=N2)OC3=CC4=C(C=C3)C(=CC=C4)C(=O)NC5=C(N)C=CC=C5

Mechanism of Action

Targets/IC50/Ki
c-Kit
(Kinase inhibition assay)
4 nM
VEGFR2
(Kinase inhibition assay)
7 nM
CSF-1R
(Kinase inhibition assay)
7 nM
Aurora B
(Kinase inhibition assay)
9 nM
References

Clinical Trial Information

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

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05346601 Completed
Healthy Volunteers
Chipscreen Biosciences Ltd.|H & J CRO International Inc.
 June 2 2022 Phase 1
NCT02122809 Completed
Solid Tumors
Chipscreen Biosciences Ltd.
 February 2014 Phase 1

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