BLU-782 | ALK2-IN-1 | Activin Receptor-like Kinase 2 Inhibitor 1;Fidrisertib;ALK2-IN-1 | ALK

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BLU-782 {[allProObj[0].p_purity_real_show]}

货号：A1177054 同义名： Activin Receptor-like Kinase 2 Inhibitor 1; Fidrisertib

BLU-782是一种有效且选择性的 ALK2 抑制剂，可在 FOP 小鼠模型中防止水肿和异位骨形成。

BLU-782 化学结构
CAS号：2141955-96-4

BLU-782 3D分子结构
CAS号：2141955-96-4

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BLU-782 纯度/质量文件产品仅供科研

货号：A1177054 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]; • Cell, 2025, 188, (21): 5847-5861.e11. Ambeed. [ A122167 ]; • Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]; • Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]; • Nat. Nanotechnol., 2025, 20, 1502-1513. Ambeed. [ A243018 , A1216705 , A522597 , A125401 , A1355641 ]; 更多 >

BLU-782 生物活性

描述

Fibrodysplasia ossificans progressive (FOP) is most commonly caused by a highly recurrent autosomal dominant gain-of-function missense mutation in the ACVR1/ALK2 gene which encodes the activin receptor type Ia^[1]. BLU-782 is an oral precision therapy specifically designed to selectively target mutant ALK2 with IC50 value of less than 10 nM^[2]. BLU-782 was derived from Blueprint Medicines' proprietary compound library and optimized via structure-guided medicinal chemistry for potent and selective targeting of mutant ALK2. BLU-782 demonstrated exquisite selectivity for R206H mutant ALK2 in cellular assays, while sparing closely related anti-targets including ALK1, ALK3, and ALK6. Additionally, BLU-782 potently inhibited mutant ALK2 in vitro, regardless of the activating ligand, including Activin A, Activin B and BMP6. In vivo studies in a conditional knock-in ALK2^R206H transgenic mouse model showed BLU-782 prevented the formation of injury-induced HO and edema, as measured by micro computed tomography and magnetic resonance imaging. In addition, BLU-782 prevented the formation of surgery-induced HO following fibular osteotomy surgery in ALK2^R206Hmice^[3].

BLU-782 参考文献

[1]Wentworth K L, Masharani U, Hsiao E C, et al. Therapeutic advances for blocking heterotopic ossification in fibrodysplasia ossificans progressiva. British Journal of Clinical Pharmacology, 2019, 85(6): 1180-1187

[2]Natasja Brooijmans, et al. Inhibitors of activin receptor-like kinase. WO2017181117A1

[3]Blueprint Medicines Presents Foundational Preclinical Data Supporting the Development of BLU-782, a Highly Selective ALK2 Inhibitor, for the Treatment of Patients with Fibrodysplasia Ossificans Progressiva

BLU-782 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

1.78mL

0.36mL

0.18mL

8.89mL

1.78mL

0.89mL

17.77mL

3.55mL

1.78mL

BLU-782 技术信息

CAS号	2141955-96-4
分子式	C₃₁H₄₂N₆O₄
分子量	562.7
SMILES Code	O=C(O[C@H]1COCC1)N(CC2)CCN2C(C3=C4)=CC=NN3C=C4C(C=C5)=NC=C5C6(CCN(C(C)C)CC6)OCC
MDL No.	MFCD32062780

别名	Activin Receptor-like Kinase 2 Inhibitor 1; Fidrisertib; ALK2-IN-1; IPN-60130
运输	蓝冰
InChI Key	SWVYYNLRVIYURK-AREMUKBSSA-N
Pubchem ID	132026427

存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, 2-8°C

溶解方案

细胞实验：

DMSO: 85 mg/mL(151.06 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

摩尔计算器

计算溶液所需的质量，体积或浓度。 Ambeed 摩尔浓度计算器基于以下方程式：

浓度 (mol/L) × 体积 (L) × 分子量 (g/mol)=质量 (g)

浓度

体积

分子量

质量

BLU-782 {[allProObj[0].p_purity_real_show]}

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