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Limantrafin (CB-103) Notch inhibitor

Cat.No.S9719

An orally active inhibitor of the Notch transcription activation complex, Limantrafin (CB-103) produces Notch loss-of-function phenotypes in flies and mice and inhibits the growth of human breast cancer and leukemia xenografts.

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Quality Control

Batch: S971901 DMSO]48 mg/mL]false]Ethanol]48 mg/mL]false]Water]Insoluble]false Purity: 99.77%
99.77

Solubility

In vitro
Batch:

DMSO : 48 mg/mL (198.08 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 48 mg/mL

Water : Insoluble

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In vivo
Batch:

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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 242.32 Formula

C15H18N2O

Storage (From the date of receipt) 3 years -20°C powder
CAS No. 218457-67-1 -- Storage of Stock Solutions

Synonyms N/A SMILES CC(C)(C)C1=CC=C(OC2=CC=C(N)C=N2)C=C1

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC50/Ki
Notch
In vitro

Limantrafin (CB-103) inhibits growth of Notch-addicted human T cell acute lymphoblastic leukemia cell lines through modulation of the Notch transcription complex.

In vivo

Limantrafin (CB-103) functions in vivo to recapitulate genetic notch loss-of-function phenotypes without causing gut toxicity, and it blocks tumor growth of GSI-resistant cancers.

References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-06-29)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05774899 RECRUITING
Adenoid Cystic Carcinoma; Metastatic Adenoid Cystic Carcinoma; Recurrent Adenoid Cystic Carcinoma
Glenn J. Hanna
2023-06-01 PHASE1; PHASE2
NCT05464836 TERMINATED
Leukemia, Lymphoblastic; Leukemia
M.D. Anderson Cancer Center
2023-04-06 PHASE2
NCT05464836 Recruiting
Leukemia Lymphoblastic|Leukemia
M.D. Anderson Cancer Center
2023-04-06 Phase 2
NCT03422679 TERMINATED
Breast Cancer; Colorectal Cancer; Adenoid Cystic Carcinoma; Non-hodgkin Lymphoma; Glomus Tumor, Malignant; Hepatocellular Carcinoma; Osteosarcoma; T-ALL
Cellestia Biotech AG
2017-12-05 PHASE1; PHASE2
NCT04714619 TERMINATED
Advanced Breast Cancer
MedSIR
2021-05-06 PHASE2
NCT04714619 Terminated
Advanced Breast Cancer
MedSIR|Cellestia Biotech AG
2021-05-06 Phase 2

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