CB-103

Catalog No.S9719

For research use only.

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.

CB-103 Chemical Structure

CAS No. 218457-67-1

Selleck's CB-103 has been cited by 1 Publication

Purity & Quality Control

Choose Selective Notch Inhibitors

Biological Activity

Description

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

CB-103 inhibits growth of Notch-addicted human T cell acute lymphoblastic leukemia cell lines through modulation of the Notch transcription complex.[1]

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]

Protocol (from reference)

Cell Research:

[1]

  • 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.

Animal Research:

[1]

  • Animal Models: NOD/SCIDγc-/- mice, C57Bl/6 wt mice
  • Dosages: 20 mg/kg, 25 mg/kg
  • Administration: Oral gavage

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 242.32
Formula

C15H18N2O

CAS No. 218457-67-1
Storage 3 years -20°C powder
2 years -80°C in solvent

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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05464836 Not yet recruiting Drug: CB-103|Drug: Venetoclax Leukemia Lymphoblastic|Leukemia M.D. Anderson Cancer Center December 30 2022 Phase 2
NCT04714619 Active not recruiting Drug: CB-103 Advanced Breast Cancer MedSIR|Cellestia Biotech AG May 6 2021 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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