2141955-96-4 in stock 2141955-96-4 good supplier High Quality BLU-782 CAS NO.2141955-96-4

2141955-96-4 in stock 2141955-96-4 good supplier High Quality BLU-782

BLU-782 (BLU782) is a novel potent, selective inhibitor of Activin receptor-like kinase (ALK2) mutant R206H with binding IC50 of <10 nM. BLU-782 is a development candidate for the treatment of fibrodysplasia ossificans progressiva, example 876 in patent WO 2017181117 A1

BLU-667 is a highly potent and selective RET inhibitor with an IC50 of 0.4 nM for WT RET. It also demonstrates potent activity (IC50 0.4 nmol/L) against common oncogenic RET alterations, including RET (M918T).

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. BLU-782 is an oral precision therapy specifically designed to selectively target mutant ALK2 with IC50 value of less than 10 nM. 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