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
* <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.)

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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

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 4 publications

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

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SHIPPING AND STORAGE
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