BLU0588
Based on 3 publication(s) in Google Scholar
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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 97.63%
- CAS 番号: 2810747-78-3
- 分子式: C26H25N5O
- 分子量:423.51
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
MedChemExpress(MCE)の使用を引用している文献 BLU0588
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生物活性
IC50: 1 nM (PRKACA)[1]
BLU0588 (1.5 μM, 1 day or 14 days) reverses a FLC-specific gene signature, leading to downregulation of genes that are overexpressed in FLC (CPS1 and G6PC, top) and upregulation of genes that are underexpressed in FLC[1].
BLU0588 (0-312.5 nM) reduces pVASP in FLC PDX cells in a dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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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]
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Dosage:30 mg/kg
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Administration:Orally, once daily, 34 days
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Result:Inhibited tumor growth in mice, by day 34 tumor growth was inhibited by 48.5%.
化学情報
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CAS 番号 2810747-78-3
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性状 Solid
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分子量 423.51
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分子式 C26H25N5O
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Color White to yellow
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SMILES
O=C(C1=CN=C(C2=C3C(NC=C3)=NC=C2)C=C1)N[C@H]4[C@H](N5CCCC5)CC6=CC=CC=C64
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (3)
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Journal Impact Factor
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Most Recent
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Proc Natl Acad Sci U S A
A PKA-selective inhibitor captures an open but more ordered conformation of the PKA catalytic subunit. [Abstract]2026 May 12;123(19):e2536312123. PMID: 42096309 -
Mol Cell Proteomics
Integrative proteomic analysis reveals the cytoskeleton regulation and mitophagy difference between ischemic cardiomyopathy and dilated cardiomyopathy. [Abstract]2023 Dec;22(12):100667. PMID: 37852321 -
Cancer Prev Res
Genome-wide CRISPR screening reveals a PKA-driven resistance mechanism to metformin for oral cancer prevention that can be exploited by combination with NSAIDs. [Abstract]2025 Dec 19. PMID: 41416398
溶剤 & 溶解度
DMSO : 83.33 mg/mL (196.76 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (277 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3612 mL | 11.8061 mL | 23.6122 mL | 59.0305 mL |
| 5 mM | 0.4722 mL | 2.3612 mL | 4.7224 mL | 11.8061 mL | |
| 10 mM | 0.2361 mL | 1.1806 mL | 2.3612 mL | 5.9030 mL | |
| 15 mM | 0.1574 mL | 0.7871 mL | 1.5741 mL | 3.9354 mL | |
| 20 mM | 0.1181 mL | 0.5903 mL | 1.1806 mL | 2.9515 mL | |
| 25 mM | 0.0944 mL | 0.4722 mL | 0.9445 mL | 2.3612 mL | |
| 30 mM | 0.0787 mL | 0.3935 mL | 0.7871 mL | 1.9677 mL | |
| 40 mM | 0.0590 mL | 0.2952 mL | 0.5903 mL | 1.4758 mL | |
| 50 mM | 0.0472 mL | 0.2361 mL | 0.4722 mL | 1.1806 mL | |
| 60 mM | 0.0394 mL | 0.1968 mL | 0.3935 mL | 0.9838 mL | |
| 80 mM | 0.0295 mL | 0.1476 mL | 0.2952 mL | 0.7379 mL | |
| 100 mM | 0.0236 mL | 0.1181 mL | 0.2361 mL | 0.5903 mL |