LDN-212854 5-（6-（4-（哌嗪-1-基）苯基）吡唑并[1,5-a]嘧啶-3-基）喹啉|cas:1432597-26-6|西域试剂

LDN-212854 5-（6-（4-（哌嗪-1-基）苯基）吡唑并[1,5-a]嘧啶-3-基）喹啉,99.70%

产品编号：Bellancom-15897| CAS NO：1432597-26-6| 分子式：C₂₅H₂₂N₆| 分子量：406.48

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-15897	￥780.00	杭州北京（现货）
Bellancom-15897	￥1350.00	杭州北京（现货）
Bellancom-15897	￥2700.00	杭州北京（现货）
Bellancom-15897	￥4600.00	杭州北京（现货）
Bellancom-15897	￥6800.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

LDN-212854 5-（6-（4-（哌嗪-1-基）苯基）吡唑并[1,5-a]嘧啶-3-基）喹啉

产品介绍

LDN-212854 是一种骨形态发生蛋白 (BMP) 抑制剂，可有效抑制 ALK2 (IC₅₀: 1.3 nM)。LDN-212854 还可抑制 ALK1 (IC₅₀: 2.40 nM)。LDN-212854 可用于研究进行性骨化纤维发育不良和癌症，如肝细胞癌 (HCC)。

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.

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

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.

体内研究
(In Vivo)

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.

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

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.

体内研究

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

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.

体内研究

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

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.

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 30 mg/mL (73.80 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.4601 mL	12.3007 mL	24.6015 mL
5 mM	0.4920 mL	2.4601 mL	4.9203 mL
10 mM	0.2460 mL	1.2301 mL	2.4601 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: 2.5 mg/mL (6.15 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (6.15 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 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: 2.5 mg/mL (6.15 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (6.15 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 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