产品
编 号:F195390
分子式:C25H29N3O3
分子量:419.52
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10mM*1mL in DMSO
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5mg
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10mg
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25mg
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50mg
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100mg
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生物活性:
LDN-214117 is an orally active ALK2 inhibitor with well-tolerated and good brain penetration. LDN-214117 has a high selectivity and low cytotoxicity for ALK2 with an IC50 value of 24 nM. LDN-214117 also is a specific bone morphogenetic proteins (BMPs) signaling inhibitor and has relatively selective inhibition for BMP6 with an IC50 value of 100 nM. LDN-214117 can be used for the research of fibrodysplasia ossificans progressiva (FOP), diffuse intrinsic pontine glioma (DIPG)
体内研究:
LDN-214117 (p.o., 25 mg/kg, daily, for 14 days) has well-tolerated in mice.Animal Model:NOD.SCID mice
Dosage:25 mg/kg
Administration:p.o., daily, for 14 days
Result:Showed good-tolerated in mice.

体外研究:
LDN-214117 has high inhibition and selectivity for ALK2 kinase proteins with an IC50 value of 24 nM.LDN-214117 has kinase activity for ALK1, ALK3 and ALK5 with IC50 values of 27 nM, 1,171 nM and 3,000 nM, respectively.LDN-214117 exhibits relatively selective inhibition for BMP6, BMP2 and BMP4 with IC50 values of 100 nM, 1,022 nM and 960 nM, respectively.LDN-214117 has inhibition of TGF-β1-induced transcriptional activity with an IC50 values of 16,000 nM.LDN-214117 (5 μM, 30 min, 3 h and 24 h) has time-dependent effect activity on gene regulation level and/ or a BMP signaling pathway other than SMAD-dependent that is responsible for ID1 targeting.LDN-214117 (5 μM, 24-120 h) reduces viability, proliferation and causes apoptosis of lung carcinoma cells LCLC-103H.LDN-214117 (5 μM, 0-48 h) suppresses wound healing and chemotactic potential of LCLC-103H cells.LDN-214117 (5 μM, 48 h) hinders growth of multicellular LCLC-103H spheroids.
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