Rucaparib monocamsylate NEW
Price | $55 | $97 | $163 |
Package | 5mg | 10mg | 25mg |
Min. Order: | |
Supply Ability: | 10g |
Update Time: | 2024-11-18 |
Product Details
Product Name: Rucaparib monocamsylate | CAS No.: 1859053-21-6 |
Purity: 99.8% | Supply Ability: 10g |
Release date: 2024/11/18 |
Product Introduction
Bioactivity
名稱 | Rucaparib monocamsylate |
描述 | Rucaparib monocamsylate (Rucaparib Camsylate) is a PARP inhibitor (PARP1,Ki of 1.4 nM). Rucaparib Camsylate also displays binding affinity to eight other PARP domains. |
體外活性 | Rucaparib is the most effective PARP inhibitor in enzyme assays (Ki: 1.4 nM). Rucaparib inhibits PARP-1 activity by 97.1% at a concentration of 1 μM in permeabilized D283Med cells. Rucaparib could target NF-κB activated by DNA damage and overcome toxicity observed with classical NF-κB inhibitors without compromising other vital inflammatory functions. The radio-sensitization by Rucaparib is due to downstream inhibition of activation of NF-κB and is independent of SSB repair inhibition [1][2][3]. |
體內(nèi)活性 | Rucaparib is not toxic but obviously enhances temozolomide-induced TGD in the DNA repair protein-competent D384Med xenografts. Rucaparib and AG14584 obviously (P < 0.05) increase temozolomide toxicity. Rucaparib enhances the antitumor activity of temozolomide and indicates complete and sustained tumor regression in NB1691 and SHSY5Y xenografts. Rucaparib significantly potentiates the cytotoxicity of topotecan and temozolomide in NB-1691, SH-SY-5Y, and SKNBE (2c) cells. Rucaparib (1 mg/kg) significantly increases temozolomide-induced body weight loss. Rucaparib (0.1 mg/kg) results in a 50% increase in the temozolomide-induced tumor growth delay. Pharmacokinetics studies also show that Rucaparib is detected in the brain tissue, which indicates that Rucaparib has potential in intra-cranial malignancy therapy [1][3][4]. |
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 : 82.33 mg/mL (148.17 mM) |
關(guān)鍵字 | repair | H6PD | PARP | BRCA1 | poly ADP ribose polymerase | AG14644 | SSB | PF-01367338 monocamsylate | Capan-1 | Inhibitor | AG014699 monocamsylate | NF-κB | Rucaparib monocamsylate | inhibit | MX-1 | BRCA2 |
相關(guān)產(chǎn)品 | 4'-Methoxychalcone | VPC-70063 | 3-Aminobenzamide | XAV-939 | Niraparib | 3-Methoxybenzamide | NU1025 | Olaparib | Benzamide | OUL35 |
相關(guān)庫 | 經(jīng)典已知活性庫 | EMA 上市藥物庫 | 抗癌臨床化合物庫 | 藥物功能重定位化合物庫 | 抑制劑庫 | 抗癌上市藥物庫 | 抗衰老化合物庫 | 已知活性化合物庫 | 抗癌活性化合物庫 | 抗癌藥物庫 |
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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