Fidrisertib

Fidrisertib (BLU-782) is the orally active inhibitor for activin receptor-like kinase 2 (ALK2) that inhibits ALK2R206H, ALK2, ALK1, ALK6, ALK3, ALK4, TGFβR2 and ALK5 with IC50s of 0.2, 0.6, 3, 24, 45, 65, 67 and 155 nM, respectively[1][2].

Product Specifications

CAS Number

[2141955-96-4]

Product Name Alternative

BLU-782; IPN-60130; ALK2-IN-1

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

TGF-β Receptor

Type

Reference compound

Related Pathways

TGF-beta/Smad

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/ALK2-IN-1.html

Purity

98.17

Solubility

DMSO : 4.17 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C(N1CCN(C2=CC=NN3C2=CC(C4=NC=C(C5(OCC)CCN(C(C)C)CC5)C=C4)=C3)CC1)O[C@H]6COCC6

Molecular Formula

C31H42N6O4

Molecular Weight

562.70

Precautions

H302, H315, H319, H335

References & Citations

[1]Natasja Brooijmans, et al. Inhibitors of activin receptor-like kinase. WO2017181117A1.|[2]Davis AJ, et al., . An ALK2 inhibitor, BLU-782, prevents heterotopic ossification in a mouse model of fibrodysplasia ossificans progressiva. Sci Transl Med. 2024 May 29;16 (749) :eabp8334.