LDN-211904 oxalate

Name: LDN-211904 oxalate
Brand: MedChemExpress
SKU: HY-107460
Rating: 4.5 (1 reviews)

Cat. No.: HY-107460 Pureza: 99.0%: Ficha de datos
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LDN-211904 oxalate is a potent and reversible EphB3 inhibitor with an IC₅₀ of 79 nM. LDN-211904 oxalate shows good metabolic stability in mouse liver microsomes. LDN-211904 oxalate with Cetuximab (HY-P9905) could be effective in inhibiting STAT3-activated colorectal cancer (CRC) stemness and Cetuximab resistance in CRC.

Para uso exclusivo en investigación. No vendemos a pacientes.

LDN-211904 oxalate Estructura química

No. CAS : 1198408-78-4

Tamaño	Stock	Cantidad
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	En stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	En stock	Estimated Time of Arrival: December 31
Solid
1 mg	En stock	Estimated Time of Arrival: December 31
5 mg	En stock	Estimated Time of Arrival: December 31
10 mg	En stock	Estimated Time of Arrival: December 31
25 mg	En stock	Estimated Time of Arrival: December 31
50 mg	En stock	Estimated Time of Arrival: December 31
100 mg	Obtener un presupuesto
200 mg	Obtener un presupuesto

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Revisión del cliente

Based on 1 publication(s) in Google Scholar

Other Forms of LDN-211904 oxalate:

LDN-211904 Obtener un presupuesto
LDN-211904 oxalate (Standard) Obtener un presupuesto

1 Publications Citing Use of MCE LDN-211904 oxalate

•Technical University of Munich. 24.01.2018.

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Ver todos los productos específicos de isoformas Ephrin Receptor:

Ver todas las isoformas

EphB EphA

Actividad biológica
Pureza y Documentación
Referencias
Revisión del cliente

Descripciòn

IC₅₀ & Target

IC₅₀: 0.079 µM (EphB3)^[1]

In Vitro

LDN-211904 (20 μM; 24 h) oxalate induces apoptosis by increasing c-PARP in SW48 resistant cells^[2].
LDN-211904 (20 μM; 4-20 h) oxalate decreases the levels of p-STAT3, GLI-1, SOX2 and Vimentin in SW48 resistant cells^[2].

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

Apoptosis Analysis^[2]

Cell Line:	SW48 and SW48 Cetuximab-resistant (SW48R) cells
Concentration:	20 μM
Incubation Time:	24 h
Result:	Induced apoptosis by increasing c-PARP.

Western Blot Analysis^[2]

Cell Line:	SW48 and SW48 Cetuximab-resistant (SW48R) cells
Concentration:	20 μM
Incubation Time:	4 h, 8 h, 20 h
Result:	The levels of p-STAT3, GLI-1, SOX2 and Vimentin in SW48 resistant cells were decreased.

In Vivo

LDN-211904 (0.1 mg/kg; i.p.; three times a week; for 21 days) oxalate inhibits and overcomes Cetuximab (HY-P9905) resistance in vivo^[2].

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

Animal Model:	Four-week-old female BALB/c nude mice were implanted subcutaneously SW48 cells^[2]
Dosage:	0.1 mg/kg
Administration:	i.p.; three times a week; for 21 days
Result:	Inhibited tumor growth.

Peso molecular

444.87

Fòrmula

C₂₁H₂₁ClN₄O₅

No. CAS

1198408-78-4

Appearance

Solid

Color

White to off-white

SMILES

O=C(C(O)=O)O.O=C(C1=CN=C2C=CC(C3CCNCC3)=CN21)NC4=C(Cl)C=CC=C4

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvente y solubilidad

In Vitro:

DMSO : 100 mg/mL (224.78 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	2.2478 mL	11.2392 mL	22.4785 mL
5 mM	0.4496 mL	2.2478 mL	4.4957 mL
10 mM	0.2248 mL	1.1239 mL	2.2478 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculadora de molaridad
Calculadora de dilución

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.62 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 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.62 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 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.62 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)

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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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.

Pureza y Documentación

Purity: 99.0%

Select Batch:

Ficha de datos (276 KB) SDS (252 KB)

COA (249 KB)

Instrucciones de manejo (2659 KB)

Referencias

[1]. Qiao L, et al. Structure-activity relationship study of EphB3 receptor tyrosine kinase inhibitors. Bioorg Med Chem Lett. 2009 Nov 1;19(21):6122-6. [Content Brief]

[2]. Park SH, et al. Sonic hedgehog pathway activation is associated with cetuximab resistance and EPHB3 receptor induction in colorectal cancer. Theranostics. 2019 Apr 12;9(8):2235-2251. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.2478 mL	11.2392 mL	22.4785 mL	56.1962 mL
	5 mM	0.4496 mL	2.2478 mL	4.4957 mL	11.2392 mL
	10 mM	0.2248 mL	1.1239 mL	2.2478 mL	5.6196 mL
	15 mM	0.1499 mL	0.7493 mL	1.4986 mL	3.7464 mL
	20 mM	0.1124 mL	0.5620 mL	1.1239 mL	2.8098 mL
	25 mM	0.0899 mL	0.4496 mL	0.8991 mL	2.2478 mL
	30 mM	0.0749 mL	0.3746 mL	0.7493 mL	1.8732 mL
	40 mM	0.0562 mL	0.2810 mL	0.5620 mL	1.4049 mL
	50 mM	0.0450 mL	0.2248 mL	0.4496 mL	1.1239 mL
	60 mM	0.0375 mL	0.1873 mL	0.3746 mL	0.9366 mL
	80 mM	0.0281 mL	0.1405 mL	0.2810 mL	0.7025 mL
	100 mM	0.0225 mL	0.1124 mL	0.2248 mL	0.5620 mL