| Identification | Back Directory | [Name]
BLU-0588 | [CAS]
2810747-78-3 | [Synonyms]
BLU-0588
3-Pyridinecarboxamide, N-[(1R,2R)-2,3-dihydro-2-(1-pyrrolidinyl)-1H-inden-1-yl]-6-(1H-pyrrolo[2,3-b]pyridin-4-yl)- | [Molecular Formula]
C26H25N5O | [MOL File]
2810747-78-3.mol | [Molecular Weight]
423.51 |
| Hazard Information | Back Directory | [Uses]
BLU0588 is an orally active, potent and selective PRKACA (protein kinase cAMP-activated catalytic subunit alpha) kinase inhibitor, with an IC50 of 1 nM and dissociation constant (Kd) of 4 nM. BLU0588 can be used for fibrolamellar carcinoma (FLC) research[1]. | [in vivo]
BLU0588 (30-75 mg/kg, orally, once) can inhibit PRKACA, effectively inhibits downstream signaling of PRKACA, phosphorylated VASP levels returns to baseline levels by 24 hours[1].
The highest tolerated dose of BLU0588 for more than 3 weeks of continuous dosing was established as 30 mg/kg QD in mice[1].
BLU0588 (30 mg/kg, orally, once daily, 34 days) can inhibits tumor growth in mice[1].
| Animal Model: | female NOD-SCID mice harboring FLC PDX tumors (6-8-week-old, FLC PDX shRNA cell lines or Hep3B cells were implanted)[1] | | Dosage: | 30 mg/kg | | Administration: | Orally, once daily, 34 days | | Result: | Inhibited tumor growth in mice, by day 34 tumor growth was inhibited by 48.5%. |
| [References]
[1] Stefanie S. Schalm, et al. Evaluation of Protein Kinase cAMP-Activated Catalytic Subunit Alpha as a Therapeutic Target for Fibrolamellar Carcinoma. Gastro Hep Advances. Volume 2, Issue 3, 2023, Pages 307-321. |
|
|