Product Details
| Product Name:
Bavdegalutamide |
CAS No.:
2222112-77-6 |
| Purity:
99.04% |
Supply Ability:
10g |
| Release date:
2024/11/18 |
Product Introduction
Bioactivity
| 名稱(chēng) | Bavdegalutamide |
| 描述 | Bavdegalutamide (ARV-110) is an oral protein degrader that specifically binds to AR and mediates its degradation. Bavdegalutamide can degrade clinically relevant mutant AR proteins, maintain activity in a high androgen environment, and has an acceptable safety profile. |
| 體外活性 | Bavdegalutamide (ARV-110) completely degrades AR in all cell lines tested, with an observed 50% degradation concentration (DC50) of < 1 nM. [3] |
| 體內(nèi)活性 | METHODS: The mean plasma concentration-time profiles of Bavdegalutamide (ARV-110) were measured in rats and mice after intravenous administration of Bavdegalutamide (2 mg/kg, intravenous injection) and (5 mg/kg, oral administration) using the developed LC-MS/MS method.
RESULTS: In rats, after intravenous injection of Bavdegalutamide, the calculated total clearance (CL) value was 413.6 ± 31.7 mL/h/kg, and the steady-state (VSS) value (5775 ± 320 mL/kg) indicated that ARV-110 was well distributed in tissues; after oral administration, the peak plasma concentration (Cmax) value was 110.5 ± 9.2 ng/mL, at 5.5 ± 1.9 hours, and the oral bioavailability of ARV-110 in rats was moderate (23.8%); after intravenous administration in mice, the CL value of ARV-110 was lower than the hepatic blood flow rate of mice (90 mL/min/kg), and Bavdegalutamide showed a relatively large VSS value (2366 ± 402.2 mL/kg), indicating that the drug was mainly confined to tissues; after oral administration, the Cmax value was 612.0 ± 88.38 ng/mL. [2]
METHODS: Bavdegalutamide (1 mg/kg, orally, once a day) was used to treat xenograft model mice, and the degree of AR degradation and tumor growth in the mice were observed.
RESULTS: With over 90% AR degradation in mice, Bavdegalutamide achieved significant inhibition of tumor growth and AR signaling in both intact and castrated conditions. [3] |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 46 mg/mL (56.63 mM), Sonication is recommended.
|
| 關(guān)鍵字 | ARV 110 | prostate | Bavdegalutamide | castration-resistant prostate cancer | receptor | androgen | ARV110 | Androgen Receptor | inhibit | cancer | Inhibitor | metastatic |
| 相關(guān)產(chǎn)品 | Dehydroisoandrosterone 3-acetate | Bicalutamide | S-23 | Enzalutamide | Adrenosterone | Allura Red AC | SK33 | Sunset Yellow FCF | Ostarine | Flutamide |
| 相關(guān)庫(kù) | 經(jīng)典已知活性庫(kù) | 抗癌臨床化合物庫(kù) | 藥物功能重定位化合物庫(kù) | 口服活性化合物庫(kù) | 臨床期小分子藥物庫(kù) | 已知活性化合物庫(kù) | 抗癌化合物庫(kù) | 抗癌藥物庫(kù) | 抗癌活性化合物庫(kù) | 轉(zhuǎn)錄因子庫(kù) |
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 |
|
Suppliers |
Update time |
|
|
$0.00/1KG |
VIP3Y
|
Henan Aochuang Chemical Co.,Ltd.
|
2022-09-29 |
United States