LDN-212854
Based on 2 publication(s) in Google Scholar
LDN-212854 is a bone morphogenetic protein (BMP) inhibitor that potently inhibits ALK2 (IC50: 1.3 nM). LDN-212854 also inhibits ALK1 (IC50: 2.40 nM). LDN-212854 can be used in the research of fibrodysplasia ossificans progressive and cancers, such as hepatocellular carcinoma (HCC).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.62%
- No. CAS: 1432597-26-6
- Fòrmula: C25H22N6
- Peso molecular:406.48
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) LDN-212854
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Actividad biológica
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ACVR1 1.3 nM (IC50) |
ALK1 2.4 nM (IC50) |
BMPR1A 85.8 nM (IC50) |
ALK4 2133 nM (IC50) |
ALK5 9276 nM (IC50) |
LDN-212854 (0-3.815 μM) blocks the phosphorylation of SMAD1/5/8 induced by BMP7 in BMPR2 / cells[1].
LDN-212854 (2.5 μM, 5 days ) inhibits cell proliferation in Huh7 and MT cells[2].
LDN-212854 (0.5 μM, 48 h ) suppresses ID1 and EpCAM expression in Huh7 and MT cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BMPR2-deficient pulmonary vascular smooth muscle cells
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Concentration:0, 1, 3, 6, 16, 39, 98, 244, 610, 1530, 3815 nM
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Incubation Time:
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Result:Inhibited the phosphorylation of SMAD1/5/8 induced by BMP7 with an IC50 value of 37 nM.
LDN-212854 (intraperitoneal injection, 6 mg/kg, twice daily for 10-14 days) suppresses HCC tumor progression through repression of ID1 in HCC xenografts model[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Murine inducible transgenic ALK2Q207D model of heterotopic ossification[1]
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Dosage:6 mg/kg
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Administration:Intraperitoneal injection , twice daily for 4 weeks
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Result:Prevented the formation of heterotopic bone and preserved limb range of motion with minimal or no impairment in the majority of mice.
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Animal Model:HCC xenografts (Huh7 or MT cell)[1]
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Dosage:6 mg/kg
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Administration:Intraperitoneal injection, twice daily for 10-14 days.
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Result:Inhibited tumor growth and showed less spheroid/colony formation ability than PBS-treated tumor cells.
Chemical Information
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No. CAS 1432597-26-6
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Appearance Solid
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Peso molecular 406.48
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Fòrmula C25H22N6
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Color Light yellow to yellow
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SMILES
C12=C(C3=C4N=CC(C5=CC=C(N6CCNCC6)C=C5)=CN4N=C3)C=CC=C1N=CC=C2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Adv Sci (Weinh)
2024 Mar;11(12):e2306499. PMID: 38229201 -
Solvente y solubilidad
DMSO : ≥ 30 mg/mL (73.80 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (6.15 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (6.15 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Ficha de datos (281 KB)
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SDS (479 KB)
- English - EN (479 KB)
- Français - FR (479 KB)
- Deutsch - DE (479 KB)
- Norwegian - NO (479 KB)
- Español - ES (479 KB)
- Swedish - SV (479 KB)
- Italian - IT (479 KB)
- Portuguese - PT (479 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Mohedas AH, et al. Development of an ALK2-biased BMP type I receptor kinase inhibitor. ACS Chem Biol. 2013;8(6):1291-302. [Content Brief]
[2]. Han Chen, et al. BMP9-ID1 signaling promotes EpCAM-positive cancer stem cell properties in hepatocellular carcinoma. Mol Oncol. 2021 Aug;15(8):2203-2218. [Content Brief]
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 | 2.4601 mL | 12.3007 mL | 24.6015 mL | 61.5036 mL |
| 5 mM | 0.4920 mL | 2.4601 mL | 4.9203 mL | 12.3007 mL | |
| 10 mM | 0.2460 mL | 1.2301 mL | 2.4601 mL | 6.1504 mL | |
| 15 mM | 0.1640 mL | 0.8200 mL | 1.6401 mL | 4.1002 mL | |
| 20 mM | 0.1230 mL | 0.6150 mL | 1.2301 mL | 3.0752 mL | |
| 25 mM | 0.0984 mL | 0.4920 mL | 0.9841 mL | 2.4601 mL | |
| 30 mM | 0.0820 mL | 0.4100 mL | 0.8200 mL | 2.0501 mL | |
| 40 mM | 0.0615 mL | 0.3075 mL | 0.6150 mL | 1.5376 mL | |
| 50 mM | 0.0492 mL | 0.2460 mL | 0.4920 mL | 1.2301 mL | |
| 60 mM | 0.0410 mL | 0.2050 mL | 0.4100 mL | 1.0251 mL |
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