For research use only. Not for therapeutic Use.
BLU2864 is an orally active, highly selective, ATP-competitive PRKACA inhibitor (IC50=0.3 nM). BLU2864 shows anti-tumor activity. BLU2864 can be used in cancer and polycystic kidney disease research[1][2].
BLU2864 (40 nM and 200 nM; 5 d) inhibits forskolin (HY-15371)-induced in vitro cystogenesis[1].
BLU2864 (oral gavage; 45 mg/kg; once daily; 5 d) inhibits renal PKA activity in Pkd1RC/RC mice[1].
BLU2864 (oral gavage; 30 mg/kg; once daily; 5 d) inhibits PKA activity and ameliorates PKD in Pkd1RC/RC mice[1].
BLU2864 (oral gavage; 30 mg/kg and 75 mg/kg; once daily; 34 d) reduces FLC tumor growth in vivo[2].
| Catalog Number | I042872 |
| CAS Number | 2810747-89-6 |
| Synonyms | N-[(1R,2S)-5-(difluoromethyl)-7-fluoro-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-6-(3-methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)pyridine-3-carboxamide |
| Molecular Formula | C24H19F3N4O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C24H19F3N4O2/c1-11-9-30-23-19(11)15(4-5-28-23)17-3-2-12(10-29-17)24(33)31-21-18(32)8-13-6-14(22(26)27)7-16(25)20(13)21/h2-7,9-10,18,21-22,32H,8H2,1H3,(H,28,30)(H,31,33)/t18-,21-/m0/s1 |
| InChIKey | VRPOVDLLZCQZEG-RXVVDRJESA-N |
| SMILES | CC1=CNC2=NC=CC(=C12)C3=NC=C(C=C3)C(=O)NC4C(CC5=C4C(=CC(=C5)C(F)F)F)O |
| Reference | [1]. Xiaofang Wang, et al. Protein Kinase A Downregulation Delays the Development and Progression of Polycystic Kidney Disease. J Am Soc Nephrol. 2022 Jun;33(6):1087-1104. [2]. Stefanie S. Schalm, et al. Evaluation of PRKACA as a Therapeutic Target for Fibrolamellar Carcinoma. bioRxiv 2022.01.31.477690. |
