LDN-214117|1627503-67-6|-陌孚医药/Medlife

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LDN-214117

目录号: PC16103 纯度: ≥98%

CAS No. :1627503-67-6

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中文名称

LDN-214117

中文别名

LDN-214117 抑制剂

英文名称

LDN-214117

英文别名

LDN-214117;1-(4-(6-Methyl-5-(3,4,5-trimethoxyphenyl)pyridin-3-yl)phenyl)piperazine;1-[4-[6-methyl-5-(3,4,5-trimethoxyphenyl)pyridin-3-yl]phenyl]piperazine;1-{4-[6-methyl-5-(3,4,5-trimethoxyphenyl)pyridin-3-yl]phenyl}piperazine;compound 10 [PMID: 25101911];GTPL8481;AOB6448;BCP12392;3772AH;BDBM50056676;s7627;LDN214117;LDN 214117;SB19490;A16096;1-[4-[6-Methyl-

Cas No.

1627503-67-6

分子式

C₂₅N₃O₃H₂₉

分子量

419.52

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

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)

性状

Solid

IC50 & Target[1][2]

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)

体外研究(In Vitro)

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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

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 cells.

RT-PCR

Cell Line:	LCLC-103H cells
Concentration:	5 μM
Incubation Time:	24 h, 48 h and 72 h
Result:	Induced distinct gene expression patterns for the two EMTTFs.

Cell Migration Assay

Cell Line:	LCLC-103H cells
Concentration:	5 μM
Incubation Time:	0 h, 24 h and 48 h
Result:	Significantly hindered the migration of LCLC-103H cells into the wound area by Inhibiting of BMP signaling.

体内研究(In Vivo)

LDN-214117 (p.o., 25 mg/kg, daily, for 14 days) has well-tolerated in mice.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	NOD.SCID mice
Dosage:	25 mg/kg
Administration:	p.o., daily, for 14 days
Result:	Showed good-tolerated in mice.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

参考文献

[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. [Information]

[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. [Information]

[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. [Information]

溶解度数据

体外研究:

DMSO : 20 mg/mL (47.67 mM; ultrasonic and warming and heat to 60°C)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3837 mL	11.9184 mL	23.8368 mL
5 mM	0.4767 mL	2.3837 mL	4.7674 mL
10 mM	0.2384 mL	1.1918 mL	2.3837 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2 mg/mL (4.77 mM); Clear solution

此方案可获得 ≥ 2 mg/mL (4.77 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2 mg/mL (4.77 mM); Clear solution

此方案可获得 ≥ 2 mg/mL (4.77 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2 mg/mL (4.77 mM); Clear solution

此方案可获得 ≥ 2 mg/mL (4.77 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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