Art. -Nr.: HY-135145

Limantrafin

(Synonyms: CB-103)

11 Cited Publications

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Based on 11 publication(s) in Google Scholar

Limantrafin (CB-103) is a first-in-class, orally active protein-protein interaction (PPI) inhibitor of the NOTCH transcriptional activation complex. Limantrafin has anti-tumor activity.

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Reinheit: 99.97%
CAS. Nr.: 218457-67-1
Formel: C₁₅H₁₈N₂O
Molecular Weight:242.32

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Limantrafin Chemical Structure

CAS. Nr.: 218457-67-1

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (11)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

Limantrafin (CB-103) is a first-in-class, orally active protein-protein interaction (PPI) inhibitor of the NOTCH transcriptional activation complex. Limantrafin has anti-tumor activity^[1]^[2]^[3]^[4].

IC₅₀ & Target

notch signaling pathway^[1]

In Vitro

Limantrafin acts as a pan-NOTCH inhibitor by targeting NOTCH transcriptional activation complex^[2].
Limantrafin can block NOTCH signaling in human T cell acute lymphoblastic leukemia cancer cell lines^[2].
Limantrafin exhibits anti-tumor efficacy in GSI resistant T-ALL cell lines^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[1]

Cell Line:

RPMI 8402, KOPTK1, PANC1, nRas driven melanoma cells
Concentration:

10 μM
Incubation Time:

4 days, 6 days
Result:

Caused a significant reduction in their growth potential.

In Vivo

Limantrafin inhibits NOTCH dependent cellular processes in mice^[2].
Limantrafin blocks in vivo growth of PDX models of T-ALL^[2].
Limantrafin (25 mg/kg; i.p./p.o.; 2x daily; for 2 weeks) inhibits growth of GSI/Mab resistant triple negative breast cancer^[3].
Limantrafin exhibits anti-tumor activity in xenograft models of human T-ALL and mouse mammary tumors^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

NSG mice, triple negative breast cancer mouse xenograft model^[3]
Dosage:

25 mg/kg
Administration:

Oral administration/Intraperitoneal injection; 2x daily; for 2 weeks
Result:

Inhibited growth of GSI/Mab resistant triple negative breast cancer.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 218457-67-1
Appearance Solid
Molecular Weight 242.32
Formel C₁₅H₁₈N₂O
SMILES

NC1=CC=C(OC2=CC=C(C(C)(C)C)C=C2)N=C1
Synonyms

CB-103
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (11)

All Cell Proliferation/Viability AssayRT-PCRWB

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Journal Impact Factor

Nat Biotechnol

Functional analysis of structural variants in single cells using Strand-seq. [Abstract]

2023 Jun;41(6):832-844. PMID: 36424487
Mater Today Bio

A microfluidic model of human dental pulp angiogenesis for preclinical drug and biomaterial testing. [Abstract]

2026 Jan 6:37:102776. PMID: 41585433
Nat Struct Mol Biol

RNAi screens identify HES4 as a regulator of redox balance supporting pyrimidine synthesis and tumor growth. [Abstract]

2024 May 20. PMID: 38769389

Limantrafin purchased from MedChemExpress. Usage Cited in: Nat Struct Mol Biol. 2024 May 20. [Abstract]

The mRNA levels of HES1 and HES4 in A549 cells treated with or without 10 μM CB-103 (Limantrafin) for 24 hours were measured.

Limantrafin purchased from MedChemExpress. Usage Cited in: Nat Struct Mol Biol. 2024 May 20. [Abstract]

The protein levels of HES1 and HES4 in A549 cells treated with or without 10 μM CB-103 (Limantrafin) for 24 hours were measured.
Oncogene

Notch signaling regulates a metabolic switch through inhibiting PGC-1α and mitochondrial biogenesis in dedifferentiated liposarcoma. [Abstract]

2023 Aug;42(34):2521-2535. PMID: 37433985

Limantrafin purchased from MedChemExpress. Usage Cited in: Oncogene. 2023 Aug;42(34):2521-2535. [Abstract]

RT-qPCR results showed that CB103 (Limantrafin) inhibited the expression of NOTCH1 and HES1 genes in LPS246 cells.

Limantrafin purchased from MedChemExpress. Usage Cited in: Oncogene. 2023 Aug;42(34):2521-2535. [Abstract]

Representative dose-response curves of LPS246 cells to different concentrations of CB103 (Limantrafin) and their corresponding IC50 values.
ACS Biomater Sci Eng

Modeling Disease-Relevant Bile Duct Morphogenesis Defects in a Tunable In Vitro System. [Abstract]

2026 Jun 8;12(6):3103-3115. PMID: 42099289
Reprod Biol Endocrinol

Low-Intensity pulsed ultrasound reduces ovarian cryopreservation injury through the Notch signaling pathway. [Abstract]

2026 Jan 28;24(1):30. PMID: 41593705

Limantrafin purchased from MedChemExpress. Usage Cited in: Reprod Biol Endocrinol. 2026 Jan 28;24(1):30. [Abstract]

Western blot of the Ho-1 expression in the CP group, the CP + CB103 (Limantrafin) group, and the CP + CB103 + LIPUS group.
Mol Biol Rep

17β-estradiol inhibits Notch1 activation in murine macrophage cell line RAW 264.7. [Abstract]

2024 Nov 8;51(1):1134. PMID: 39514048
University of Zurich

2025 Feb 04.
University of Zagreb

2023 Jul 19.
Research Square Print

2022 May.
Research Square Preprint

2021 Jun.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (412.68 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

4.1268 mL

20.6339 mL

41.2677 mL

5 mM

0.8254 mL

4.1268 mL

8.2535 mL

10 mM

0.4127 mL

2.0634 mL

4.1268 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (10.32 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (10.32 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (8.58 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Freddy Radtke, et al. Inhibitors of notch signalling pathway and use thereof in treatment of cancers. US9296682B2.

[2]. R.Lehal, et al. Development of a novel first-in-class oral inhibitor of the NOTCH pathway.

[3]. Rajwinder Lehal, et al. Non clinical pharmacology, pharmacokinetics and safety profiling of CB-103: A novel first-in-class small molecule inhibitor of the NOTCH pathway.

[4]. Jose Manuel Perez Garcia, et al. First-in-human phase 1-2A study of CB-103, an oral Protein-Protein Interaction Inhibitor targeting pan-NOTCH signalling in advanced solid tumors and blood malignancies.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	4.1268 mL	20.6339 mL	41.2677 mL	103.1694 mL
	5 mM	0.8254 mL	4.1268 mL	8.2535 mL	20.6339 mL
	10 mM	0.4127 mL	2.0634 mL	4.1268 mL	10.3169 mL
	15 mM	0.2751 mL	1.3756 mL	2.7512 mL	6.8780 mL
	20 mM	0.2063 mL	1.0317 mL	2.0634 mL	5.1585 mL
	25 mM	0.1651 mL	0.8254 mL	1.6507 mL	4.1268 mL
	30 mM	0.1376 mL	0.6878 mL	1.3756 mL	3.4390 mL
	40 mM	0.1032 mL	0.5158 mL	1.0317 mL	2.5792 mL
	50 mM	0.0825 mL	0.4127 mL	0.8254 mL	2.0634 mL
	60 mM	0.0688 mL	0.3439 mL	0.6878 mL	1.7195 mL
	80 mM	0.0516 mL	0.2579 mL	0.5158 mL	1.2896 mL
	100 mM	0.0413 mL	0.2063 mL	0.4127 mL	1.0317 mL

Keywords

Limantrafin

11 Cited Publications

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Limantrafin

Neuronal Signaling Compound Library

Stem Cell Signaling Compound Library

Wnt/Hedgehog/Notch Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Differentiation Inducing Compound Library

Orally Active Compound Library

Anti-Breast Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Angiogenesis-Related Compound Library

Transcription Factor-Targeted Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Publications Citing Use of MedChemExpress (MCE) Limantrafin

Biologische Aktivität

Chemical Information

Publications (11)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Limantrafin

Neuronal Signaling Compound Library

Stem Cell Signaling Compound Library

Wnt/Hedgehog/Notch Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Differentiation Inducing Compound Library

Orally Active Compound Library

Anti-Breast Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Angiogenesis-Related Compound Library

Transcription Factor-Targeted Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Publications Citing Use of MedChemExpress (MCE) Limantrafin

Biologische Aktivität

Chemical Information

Publications (11)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Limantrafin Related Classifications

Art. -Nr.: HY-135145