LDN-214117|cas:1627503-67-6|西域试剂

LDN-214117,99.95%

产品编号：Bellancom-16712| CAS NO：1627503-67-6| 分子式：C₂₅H₂₉N₃O₃| 分子量：419.52

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-16712	￥600.00	杭州北京（现货）
Bellancom-16712	￥1100.00	杭州北京（现货）
Bellancom-16712	￥2200.00	杭州北京（现货）
Bellancom-16712	￥3800.00	杭州北京（现货）
Bellancom-16712	￥5900.00	杭州北京（现货）

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LDN-214117

产品介绍

LDN-214117 是一种 ALK2 抑制剂，具有口服活性，耐受性好，脑穿透性好。LDN-214117 对 ALK2 具有较高的选择性和较低的细胞毒性，其 IC₅₀ 值为 24 nM。LDN-214117 也是一种特异性的骨形态发生蛋白 (BMPs) 信号抑制剂，对 BMP6 具有相对选择的抑制作用，其 IC₅₀ 值为 100 nM。LDN-214117 可用于进行性骨化性纤维发育不良 (FOP) 和弥漫性内源性桥脑胶质瘤 (DIPG) 的研究。

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.

西域 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.

西域 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.

体内研究

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

西域 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.

体内研究

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

西域 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.

性状

Solid

溶解性数据

In Vitro:

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

配制储备液

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

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，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，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 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.

请依序添加每种溶剂： 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 ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 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.

请依序添加每种溶剂： 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。