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| 25mg |
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Purity: ≥98%
LDN-212854 (LDN 212854; LDN212854) is a potent and selective inhibitor of BMP (bone morphogenetic protein) receptor with potential antineoplastic activity. It inhibits ALK2 with an IC50 of 1.3 nM. In vivoLDN-212854 potently inhibits heterotopic ossification in an inducible transgenic mutant ALK2 mouse model of fibrodysplasia ossificans progressiva. In vitro, LDN-212854 exhibits some selectivity for ALK2 in preference to other BMP type I receptors, ALK1 and ALK3, which may permit the interrogation of ALK2-mediated signaling, transcriptional activity and function.
| ln Vitro |
In BMPR2−/− cells, BMP7-induced phosphorylation of SMAD1/5/8 is blocked by LDN-212854 (0-3.815 μM)[1]. In Huh7 and MT cells, LDN-212854 (2.5 μM, 5 days) suppresses cell proliferation[2]. Huh7 and MT cells' expression of ID1 and EpCAM is suppressed by LDN-212854 (0.5 μM, 48 h)[2].
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| ln Vivo |
In an inducible transgenic mutant ALK2 mouse model of fibrodysplasia ossificans progressiva, potently suppresses heterotopic ossification when administered intraperitoneally twice daily for four weeks at a dose of 6 mg/kg [1]. By suppressing ID1, LDN-212854 (intraperitoneal injection, 6 mg/kg, twice daily for 4 weeks) inhibits the growth of HCC tumors in HCC xenograft models[2].
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: BMPR2-deficient pulmonary vascular smooth muscle cells Tested Concentrations: 0, 1, 3, 6, 16, 39, 98, 244, 610, 1530, 3815 nM Incubation Duration: Experimental Results: Inhibited the phosphorylation of SMAD1/5/8 induced by BMP7 with an IC50 value of 37 nM. |
| Animal Protocol |
Animal/Disease Models: Murine inducible transgenic ALK2Q207D model of heterotopic ossification[1]
Doses: 6 mg/kg Route of Administration: intraperitoneal (ip)injection , twice (two times) daily for 4 weeks Experimental Results: Prevented the formation of heterotopic bone and preserved limb range of motion with minimal or no impairment in the majority of mice. Animal/Disease Models: HCC xenografts (Huh7 or MT cell)[1] Doses: 6 mg/kg Route of Administration: intraperitoneal (ip)injection, twice (two times) daily for 10-14 days. Experimental Results: Inhibited tumor growth and demonstrated less spheroid/colony formation ability than PBS-treated tumor cells. |
| References |
[1]. Mohedas AH, et al. Development of an ALK2-biased BMP type I receptor kinase inhibitor. ACS Chem Biol. 2013;8(6):1291-302.
[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. |
| Molecular Formula |
C25H22N6
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| Molecular Weight |
406.48
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| CAS # |
1432597-26-6
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| Related CAS # |
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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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| InChi Key |
BBDGBGOVJPEFBT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H22N6/c1-3-21(22-4-2-10-27-24(22)5-1)23-16-29-31-17-19(15-28-25(23)31)18-6-8-20(9-7-18)30-13-11-26-12-14-30/h1-10,15-17,26H,11-14H2
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| Chemical Name |
5-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (6.15 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (6.15 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4601 mL | 12.3007 mL | 24.6015 mL | |
| 5 mM | 0.4920 mL | 2.4601 mL | 4.9203 mL | |
| 10 mM | 0.2460 mL | 1.2301 mL | 2.4601 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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