Veliparib dihydrochloride NEW
| Price | $30 | $40 | $71 |
| Package | 5mg | 10mg | 25mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-17 |
Product Details
| Product Name: Veliparib dihydrochloride | CAS No.: 912445-05-7 |
| Purity: 98% | Supply Ability: 10g |
| Release date: 2024/11/17 |
Product Introduction
Bioactivity
| 名稱 | Veliparib dihydrochloride |
| 描述 | Veliparib dihydrochloride (ABT-888 dihydrochloride) is a potent inhibitor of PARP1 and PARP2 with Ki of 5.2 nM and 2.9 nM in cell-free assays, respectively. It is inactive to SIRT2. |
| 激酶實(shí)驗(yàn) | PARP assays are conducted in a buffer containing 50 mM Tris (pH 8.0), 1 mM DTT, 1.5 μM [3H]NAD+?(1.6 μCi/mmol), 200 nM biotinylated histone H1, 200 nM slDNA, and 1 nM PARP-1 or 4 nM PARP-2 enzyme. Reactions are terminated with 1.5 mM benzamide, transferred to streptavidin Flash plates, and counted using a TopCount microplate scintillation counter. |
| 體外活性 | Veliparib demonstrates inactivity towards SIRT2 at concentrations greater than 5 μM[1] and exhibits potent inhibition of PARP activity, with an EC50 of 2 nM in C41 cells[2]. It effectively reduces PAR levels in H460 cells, regardless of irradiation status, and significantly impairs clonogenic survival by hindering DNA repair via PARP-1 inhibition. Additionally, when used in conjunction with radiation, Veliparib promotes apoptosis and autophagy in H460 cells[3]. Its ability to inhibit PARP activity extends to H1299, DU145, and 22RV1 cells, a process not influenced by p53 function. At a concentration of 10 μM, Veliparib diminishes the surviving fraction in clonogenic H1299 cells by 43%, enhancing radiosensitivity, particularly in oxygen-rich environments. Furthermore, it reduces the surviving fraction in H1299, DU145, and 22RV1 cells under hypoxic-irradiated conditions[4], confirming its role in sensitizing cancer cells to radiation by targeting PARP-dependent mechanisms. |
| 體內(nèi)活性 | Veliparib exhibits an oral bioavailability ranging from 56% to 92% across different species, including mice, SD rats, beagle dogs, and cynomolgus monkeys[1]. At a dosage of 25 mg/kg (i.p.), it enhances tumor growth delay in NCI-H460 xenograft models and, when combined with radiation, decreases tumor vessel formation[3]. Additionally, Veliparib significantly reduces intratumor PAR levels by over 95% at dosages of 3 and 12.5 mg/kg in A375 and Colo829 xenograft models, with this suppression sustained over time[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 : 3.2 mg/mL (10.09 mM) H2O : 50 mg/mL (157.62 mM) |
| 關(guān)鍵字 | Autophagy | Veliparib | poly ADP ribose polymerase | ABT 888 Dihydrochloride | ABT888 | inhibit | Veliparib dihydrochloride | ABT-888 Dihydrochloride | Inhibitor | ABT-888 | Veliparib Dihydrochloride | ABT888 Dihydrochloride | ABT 888 | PARP |
| 相關(guān)產(chǎn)品 | Hydroxychloroquine | Guanidine hydrochloride |
| 相關(guān)庫 | 經(jīng)典已知活性庫 | 抗癌臨床化合物庫 | 藥物功能重定位化合物庫 | 抑制劑庫 | 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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