Product Details
| Product Name:
BLU2864 |
CAS No.:
2810747-89-6 |
| Purity:
99.73% |
Supply Ability:
10g |
| Release date:
2024/11/16 |
Product Introduction
Bioactivity
| 名稱 | BLU2864 |
| 描述 | BLU2864 is an orally active, highly selective, ATP-competitive PRKACA inhibitor with an IC50 of 0.3 nM, exhibiting anti-tumor activity and potential applications in cancer and polycystic kidney disease research [1] [2]. |
| 體外活性 | BLU2864 (40 nM and 200 nM; 5 d) inhibits forskolin-induced cystogenesis in vitro, reducing cyst formation in mIMCD3 cells cultured in Matrigel by 72% and 100% at 40 nM and 200 nM, respectively, compared to control[1]. |
| 體內(nèi)活性 | BLU2864 administered via oral gavage at doses of 45 mg/kg and 30 mg/kg once daily for 5 days showed significant inhibition of renal PKA activity and amelioration of polycystic kidney disease (PKD) in Pkd1 RC/RC mice, indicated by reduced kidney basal and total PKA activities, decreased kidney weights, volumes relative to body weights, and cyst indices. Kidney basal and total PKA activities were suppressed significantly in treated mice compared to controls, with a noted increase in urine output and improved PKD symptoms at a dosage of 30 mg/kg. Additionally, BLU2864 treatment at dosages of 30 mg/kg and 75 mg/kg once daily for 34 days effectively retarded FLC tumor growth in vivo in mice bearing FLC PDX tumors, achieving tumor growth inhibition rates of 48.5% and 45.3%, respectively. |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 50 mg/mL (110.51 mM), Sonication is recommended.
|
| 關(guān)鍵字 | BLU-2864 | BLU2864 | BLU 2864 |
| 相關(guān)庫 | 經(jīng)典已知活性庫 | 激酶抑制劑庫 | 抑制劑庫 | 已知活性化合物庫 | 抗癌化合物庫 | 抗癌活性化合物庫 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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Recommended supplier
| Product name |
Price |
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Suppliers |
Update time |
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$/ |
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Anhui Ruihan Technology Co., Ltd
|
2023-08-21 |
United States