2. Neuronal Signaling Stem Cell/Wnt
  3. Notch
  4. Limantrafin

Limantrafin  (Synonyms: CB-103)

Cat. No.: HY-135145 Purity: 98.86%
COA Handling Instructions

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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.

For research use only. We do not sell to patients.

Limantrafin Chemical Structure

Limantrafin Chemical Structure

CAS No. : 218457-67-1

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 55 In-stock
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Based on 6 publication(s) in Google Scholar

Limantrafin Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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.

Limantrafin Related Antibodies

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
Molecular Weight

242.32

Formula

C15H18N2O
CAS No.
Appearance

Solid

Color

White to light brown

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.1268 mL 20.6339 mL 41.2677 mL
5 mM 0.8254 mL 4.1268 mL 8.2535 mL
View the Complete Stock Solution Preparation Table

* 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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

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.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
  • 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.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.77%

COA (244 KB) HNMR (187 KB) LCMS (121 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* 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.

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
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Limantrafin Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Limantrafin218457-67-1CB-103CB103CB 103NotchnotchsignalingpathwayleukemiaInhibitorinhibitorinhibit

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