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Purity: ≥98%
LDN-214117 (LDN 214117; LDN214117) is a novel, potent and selective ALK2 (BMP type I receptor kinase) inhibitor with potential anticancer activity. It inhibits ALK2 with an IC50 of 24 nM.
| ln Vitro |
At an IC50 of 24 nM, LDN-214117 exhibits good selectivity and inhibition of ALK2 kinase proteins[1]. LDN-214117 has kinase activity against ALK1, ALK3, and ALK5, with corresponding IC50 values of 27 nM, 1,171 nM, and 3,000 nM[1]. Using IC50 values of 100 nM, 1,022 nM, and 960 nM, respectively, LDN-214117 shows comparatively specific inhibition for BMP6, BMP2, and BMP4[1]. LDN-214117 exhibits an IC50 value of 16,000 nM for the suppression of TGF-β1-induced transcriptional activity[1]. ID1 targeting is caused by a BMP signaling route other than SMAD-dependent one, and LDN-214117 (5 μM, 30 min, 3 h, and 24 h) exhibits time-dependent effect activity on gene regulation level[2]. LDN-214117 (5 μM, 24-120 h) inhibits lung cancer cells LCLC-103H's viability, growth, and induces apoptosis[2]. The chemotactic potential and wound healing of LCLC-103H cells are suppressed by LDN-214117 (5 μM, 0-48 h)[2]. Multicellular LCLC-103H spheroids grow less quickly when exposed to LDN-214117 (5 μM, 48 h)[2].
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| ln Vivo |
Mice have responded favorably to LDN-214117 (po, 25 mg/kg, daily, for 14 days)[3].
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| Cell Assay |
Cell Viability Assay[2]
Cell Types: LCLC-103H cells Tested Concentrations: 5 μM Incubation Duration: 24 h, 48 h, 72 h and 96 h Experimental Results: diminished markedly with time, counting approximately 60% of the vehicle control level at the 96-h measurement point. Western Blot Analysis[2] Cell Types: LCLC -103H cells Tested Concentrations: 5 μM Incubation Duration: 30 min, 3 h and 24 h Experimental Results: Diminished the increase of ID1 protein. Apoptosis Analysis[2] Cell Types: LCLC-103H cells Tested Concentrations: 5 μM Incubation Duration: 24 h, 48 h, 72 h and 96 h Experimental Results: Induced considerable death of LCLC-103H cells. RT-PCR[2] Cell Types: LCLC-103H cells Tested Concentrations: 5 μM Incubation Duration: 24 h, 48 h and 72 h Experimental Results: Induced distinct gene expression patterns for the two EMTTFs. Cell Migration Assay [2] Cell Types: LCLC-103H cells Tested Concentrations: 5 μM Incubation Duration: 0 h, 24 h and 48 h Experimental Results: Dramatically hindered the migration of LCLC-103H cells into the wound area by Inhibiting of BMP signaling. |
| Animal Protocol |
Animal/Disease Models: NOD.SCID (severe combined immunodeficient) mouse[3]
Doses: 25 mg/kg Route of Administration: po, daily, for 14 days Experimental Results: demonstrated good-tolerated in mice. |
| References |
[1]. Agustin H Mohedas, et al. Structure-activity relationship of 3,5-diaryl-2-aminopyridine ALK2 inhibitors reveals unaltered binding affinity for fibrodysplasia ossificans progressiva causing mutants. J Med Chem. 2014 Oct 9;57(19):7900-15.
[2]. Jelena Mihajlović, et al. Inhibition of bone morphogenetic protein signaling reduces viability, growth and migratory potential of non-small cell lung carcinoma cells. J Cancer Res Clin Oncol. 2019 Nov;145(11):2675-2687. [3]. Diana Carvalho, et al. ALK2 inhibitors display beneficial effects in preclinical models of ACVR1 mutant diffuse intrinsic pontine glioma. Commun Biol. 2019 May 9;2:156. |
| Molecular Formula |
C25H29N3O3
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| Molecular Weight |
419.52
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| CAS # |
1627503-67-6
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| Related CAS # |
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| SMILES |
O(C([H])([H])[H])C1C(=C(C([H])=C(C=1[H])C1=C(C([H])([H])[H])N=C([H])C(=C1[H])C1C([H])=C([H])C(=C([H])C=1[H])N1C([H])([H])C([H])([H])N([H])C([H])([H])C1([H])[H])OC([H])([H])[H])OC([H])([H])[H]
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| InChi Key |
BHUXVRVMMYAXKN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H29N3O3/c1-17-22(19-14-23(29-2)25(31-4)24(15-19)30-3)13-20(16-27-17)18-5-7-21(8-6-18)28-11-9-26-10-12-28/h5-8,13-16,26H,9-12H2,1-4H3
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| Chemical Name |
1-(4-(6-methyl-5-(3,4,5-trimethoxyphenyl)pyridin-3-yl)phenyl)piperazine
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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 mg/mL (4.77 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 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 mg/mL (4.77 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 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. View More
Solubility in Formulation 3: ≥ 2 mg/mL (4.77 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3837 mL | 11.9184 mL | 23.8368 mL | |
| 5 mM | 0.4767 mL | 2.3837 mL | 4.7674 mL | |
| 10 mM | 0.2384 mL | 1.1918 mL | 2.3837 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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