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编 号:F161811
分子式:C25H22N6
分子量:406.48
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10mM*1mL in DMSO
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1mg
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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-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).

体内研究:
LDN-212854 (intraperitoneal injection, 6 mg/kg, twice daily for 4 weeks) potently inhibits heterotopic ossification in an inducible transgenic mutant ALK2 mouse model of fibrodysplasia ossificans progressiva.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.Animal Model:Murine inducible transgenic ALK2Q207D model of heterotopic ossification
Dosage:6 mg/kg
Administration:Intraperitoneal injection , twice daily for 4 weeks
Result:Prevented the formation of heterotopic bone and preserved limb range of motion with minimal or no impairment in the majority of mice.
Animal Model:HCC xenografts (Huh7 or MT cell)
Dosage:6 mg/kg
Administration:Intraperitoneal injection, twice daily for 10-14 days.
Result:Inhibited tumor growth and showed less spheroid/colony formation ability than PBS-treated tumor cells.

体外研究:
LDN-212854 (0-3.815 μM) blocks the phosphorylation of SMAD1/5/8 induced by BMP7 in BMPR2?/? cells.LDN-212854 (2.5 μM, 5 days ) inhibits cell proliferation in Huh7 and MT cells.LDN-212854 (0.5 μM, 48 h ) suppresses ID1 and EpCAM expression in Huh7 and MT cells.
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