Home Neuronal Signaling Notch inhibitor Limantrafin (CB-103) For research use only.

Limantrafin (CB-103)

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

Limantrafin (CB-103) Chemical Structure

Limantrafin (CB-103) Chemical Structure

CAS: 218457-67-1

Selleck's Limantrafin (CB-103) has been cited by 3 publications

Purity & Quality Control

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

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Biological Activity

Description

Limantrafin (CB-103) is an orally active inhibitor of the Notch transcription activation complex. CB-103 produces Notch loss-of-function phenotypes in flies and mice and inhibits the growth of human breast cancer and leukemia xenografts.
Targets
Notch [1]
In vitro
In vitro

CB-103 inhibits growth of Notch-addicted human T cell acute lymphoblastic leukemia cell lines through modulation of the Notch transcription complex.[1]
Cell Research Cell lines marrow mesenchymal stroma cells (MSCs), RPMI-8402 cells
Concentrations 10 nM to 25 μM, 1 μM
Incubation Time 3 days, 1 h, 4 h, 24 h
Method

MSCs are seeded in 384-well plates at a concentration of 2,500 cells per well in 30 μL AIMV medium. After 24 hours, ALL cells are added at a concentration of 25,000 to 30,000 cells per well in 27.5 μL AIMV. CB-103 or DMSO as control is added after an additional 24 hours at five different concentrations (from 10 nM to 25 μM). Three days later, ALL cells are collected from cocultures by scraping and stained with 7-AAD. Cell viability is measured by flow cytometry using counting beads for cell count normalization.
In Vivo
In vivo

CB-103 function in vivo recapitulates genetic notch loss-of-function phenotypes without causing gut toxicity. CB-103 blocks tumor growth of GSI-resistant cancers.[1]
Animal Research Animal Models NOD/SCIDγc-/- mice, C57Bl/6 wt mice
Dosages 20 mg/kg, 25 mg/kg
Administration Oral gavage
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05464836 Recruiting
Leukemia Lymphoblastic|Leukemia
M.D. Anderson Cancer Center
 April 6 2023 Phase 2
NCT04714619 Terminated
Advanced Breast Cancer
MedSIR|Cellestia Biotech AG
 May 6 2021 Phase 2

Chemical Information & Solubility

Molecular Weight 242.32 Formula

C15H18N2O
CAS No. 218457-67-1 SDF --
Smiles CC(C)(C)C1=CC=C(OC2=CC=C(N)C=N2)C=C1
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 48 mg/mL ( (198.08 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 48 mg/mL

Water : Insoluble


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In vivo
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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.

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