Fidrisertib


CAS No. : 2141955-96-4

(Synonyms: BLU-782; IPN-60130; ALK2-IN-1)

2141955-96-4
Price and Availability of CAS No. : 2141955-96-4
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Cat. No. : HY-117887
M.Wt: 562.70
Formula: C31H42N6O4
Purity: >98 %
Solubility: DMSO : 83.33 mg/mL (ultrasonic)
Introduction of 2141955-96-4 :

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]. IC50 & Target:IC50: <10 nM (ALK2)[1] In Vitro:Fidrisertib inhibits the activity of ALK2R206H in cell HEK293T/ALK3KO with an IC50 of 7 nM[2].
Fidrisertib blocks the signaling pathway activated by ligands such as BMP and activin, reduces the phosphorylation of SMAD1, thereby inhibiting the heterotopic ossification[2]. In Vivo:Fidrisertib (50 mg/kg, po or ip, once daily for 3-7 days) prevents heterotopic ossification in mice after muscle injury and fracture, promotes muscle repair and bone healing without significant toxicity[2].

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