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• 產(chǎn)品描述： 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)

• 靶點(diǎn)： IC50: 24 nM (ALK2); 27 nM (ALK1); 1,171 nM (ALK3); 3,000 nM (ALK5); 1,022 nM (BMP6); 27 nM (BMP2); 960 nM (BMP4); 16,000 nM (TGF-β1);ALK;TGF-beta/Smad

• 體外研究：
  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. Cell Viability Assay Cell Line: LCLC-103H cells Concentration: 5 μM Incubation Time: 24 h, 48 h, 72 h and 96 h Result: Decreased markedly with time, counting approximately 60% of the vehicle control level at the 96-h measurement point. Western Blot Analysis Cell Line: LCLC-103H cells Concentration: 5 μM Incubation Time: 30 min, 3 h and 24 h Result: Diminished the increase of ID1 protein. Apoptosis Analysis Cell Line: LCLC-103H cells Concentration: 5 μM Incubation Time: 24 h, 48 h, 72 h and 96 h Result: Induced considerable death of LCLC-103H cell

• 體內(nèi)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.

• 參考文獻(xiàn)：
  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 Mihajlovi?, 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.

• 溶解性： soluble  in  DMSO

• 保存條件： -20℃

• 配置溶液濃度參考：
  

  	1mg	5mg	10mg
  1 mM	2.384 ml	11.918 ml	23.837 ml
  5 mM	0.477 ml	2.384 ml	4.767 ml
  10 mM	0.238 ml	1.192 ml	2.384 ml
  50 mM	0.048 ml	0.238 ml	0.477 ml

• 注意：部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。

輸入產(chǎn)品批號(hào)：

本計(jì)算器可幫助您計(jì)算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關(guān)系，公式為：

質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *