| Bioactivity | 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]. | ||||||||||||
| Target | IC50: 0.3 nM (PRKACA) | ||||||||||||
| Invitro | BLU2864 (40 nM and 200 nM; 5 d) inhibits forskolin (HY-15371)-induced in vitro cystogenesis[1]. Cell Viability Assay[1] Cell Line: | ||||||||||||
| In Vivo | 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]. Animal Model: | ||||||||||||
| Name | BLU2864 | ||||||||||||
| CAS | 2810747-89-6 | ||||||||||||
| Formula | C24H19F3N4O2 | ||||||||||||
| Molar Mass | 452.43 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| 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. |
BLU2864
CAS: 2810747-89-6 F: C24H19F3N4O2 W: 452.43
BLU2864 is an orally active, highly selective, ATP-competitive PRKACA inhibitor (IC50=0.3 nM). BLU2864 shows anti-tumor
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