Limantrafin (CB-103)

Catalog No.S9719 Batch:S971901

Technical Data

Formula

C₁₅H₁₈N₂O

Molecular Weight

242.32

CAS No.

218457-67-1

Solubility (25°C)*

In vitro

DMSO

48 mg/mL (198.08 mM)

Ethanol

48 mg/mL (198.08 mM)

Water

Insoluble

In vivo (Add solvents to the product individually and in order)

Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	2.4mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 48 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil	2.4mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 48 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

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 Assay:^{^[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 Study:^{^[1]}	Animal Models NOD/SCIDγc^-/- mice, C57Bl/6 wt mice Dosages 20 mg/kg, 25 mg/kg Administration Oral gavage

Cell Assay:^{^[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 Study:^{^[1]}

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

References

[1] Rajwinder Lehal, et al. Proc Natl Acad Sci U S A. 2020 Jul 14;117(28):16292-16301.

Selleck's Limantrafin (CB-103) has been cited by 5 publications

Notch1 Phase Separation Coupled Percolation facilitates target gene expression and enhancer looping [ Sci Rep, 2024, 14(1):21912]	PubMed: 39300145
Familial Alzheimer's disease-associated PSEN1 mutations affect neurodevelopment through increased Notch signaling [ Stem Cell Reports, 2023, 18(7):1516-1533]	PubMed: 37352850
Evaluation of the anticancer activity of RIN-1, a Notch signaling modulator, in head and neck squamous cell carcinoma [ Sci Rep, 2023, 13(1):13700]	PubMed: 37607974
Evaluation of the anticancer activity of RIN-1, a Notch signaling modulator, in head and neck squamous cell carcinoma [ Sci Rep, 2023, 13(1):13700]	PubMed: 37607974
GALNT2 promotes cell proliferation, migration, and invasion by activating the Notch/Hes1-PTEN-PI3K/Akt signaling pathway in lung adenocarcinoma [ Life Sci, 2021, 276:119439]	PubMed: 33785338

RETURN POLICY
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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