| Bioactivity | 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]. |
| Target | IC50: 1 nM (PRKACA) |
| Invitro | BLU0588（1.5 μM，1 天或 14 天）可逆转 FLC 特异性基因特征，导致 FLC 中过表达的基因（CPS1 和 G6PC，顶部）下调以及 FLC 中表达不足的基因[1 ]。BLU0588 (0-312.5 nM) 以剂量依赖性方式降低 FLC PDX 细胞中的 pVASP[1]。 |
| In Vivo | BLU0588（30-75 mg/kg，口服，一次）可抑制 PRKACA，有效抑制 PRKACA 下游信号传导，磷酸化 VASP 水平在 24 小时内恢复至基线水平[1]。小鼠连续给药超过 3 周的 BLU0588 最高耐受剂量为 30 mg/kg QD[1]。BLU0588（30 mg/kg，口服，每日一次，34 天）可抑制小鼠肿瘤生长[1]。 Animal Model: |
| Name | BLU0588 |
| CAS | 2810747-78-3 |
| Formula | C26H25N5O |
| Molar Mass | 423.51 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |