LDN212854

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

LDN-212854 是一种新型 BMP 抑制剂，与 TGF-β I 型受体相比，它对 BMP 具有显着更高的选择性。

LDN-212854 is a novel BMP inhibitor that exhibits substantially greater selectivity for BMP versus the TGF-β type I receptors; possesses a bias towards ALK2(IC50=1.3 nM) versus ALK1 and ALK3 compared to other inhibitors.

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. Western Blot Analysis Cell Line:BMPR2-deficient pulmonary vascular smooth muscle cells Concentration:0, 1, 3, 6, 16, 39, 98, 244, 610, 1530, 3815 nM Incubation Time:Result:Inhibited the phosphorylation of SMAD1/5/8 induced by BMP7 with an IC50 value of 37 nM.

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.

LDN212854 | LDN 212854 | LDN-212854

Angiogenesis

ALK

ALK1| ALK2| ALK3| ALK4| ALK5

Cancer

——

1432597-26-6

406.48

C25H22N6

>98% (HPLC)

DMSO: 81 mg/mL warmed (199.27 mM)

C12=C(C3=C4N=CC(C5=CC=C(N6CCNCC6)C=C5)=CN4N=C3)C=CC=C1N=CC=C2

5-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline

(-20℃)

With Ice Pack

≥ 2 years