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LDN-214117

Cat. No. M3889

LDN-214117 Structure
Size Price Availability Quantity
5mg USD 85 In stock
10mg USD 150 In stock
50mg USD 550 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

LDN-214117 is a highly BMP selective compound, significantly biased toward ALK2 and its cognate ligands including BMP6 and also demonstrates a high degree of kinome selectivity and low cytotoxicity. LDN-214117 may be useful as highly selective probes of BMP-mediated cellular physiology that may provide a useful complement to the dorsomorphin class of compounds. Furthermore, this class of BMP inhibitors offers a structurally distinct template for the development of therapeutics for the treatment of BMP signaling-mediated diseases such as FOP.

Protocol
Cell Experiment
Cell lines HepG2 hepatocarcinoma cells
Preparation method Seeding cells at 25000 cells per well in 96-well plates and incubatng for 2 h at 37℃ and 5% CO2. Diluting compounds of LDN-214117 or DMSO are in DMEM and adding at final compound concentrations of 1, 10, and 100 μM.Incubating cells for 4 and 24 h, after which the media is discarded. Cells are lysed by adding 30 μL of passive lysis buffer and shaken at RT for 15 min. Cell viability is determined by quantifying the ATP present in each well by adding 10 μL of Cell Titer Glo per well and measuring the light output by Spectramax L luminometer. Data is normalized to 100% viability for cells receiving only DMSO.
Concentrations 100 μM
Incubation time 24 h
Animal Experiment
Animal models
Formulation
Dosages
Administration
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 419.52
Formula C25H29N3O3
CAS Number 1627503-67-6
Purity >99%
Solubility DMSO
Storage at -20°C
References

Structure-activity relationship of 3,5-diaryl-2-aminopyridine ALK2 inhibitors reveals unaltered binding affinity for fibrodysplasia ossificans progressiva causing mutants.
Mohedas AH, et al. J Med Chem. 2014 Oct 9;57(19):7900-15. PMID: 25101911.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: LDN-214117 supplier, ALK, inhibitors

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