| Bioactivity | Bicalutamide-d5 is deuterated labeled Bicalutamide (HY-14249). Bicalutamide is an orally active non-steroidal androgen receptor (AR) antagonist. Bicalutamide can be used for the research of prostate cancer[1]. |
| Invitro | 氢、碳和其他元素的稳定重同位素已被纳入药物分子中，主要作为药物开发过程中定量的示踪剂。氘化引起了人们的关注，因为它可能影响药物的药代动力学和代谢谱[1]。在全细胞结合试验 (LNCaP/AR (cs) 细胞) 中，Bicalutamide 与雄激素竞争结合 AR，IC50 为 160 nM[2]。Bicalutamide 以剂量依赖性方式诱导 VCaP 细胞增殖，同时部分拮抗 R1881 (合成雄激素)[2]的作用。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Bicalutamide-d5 相关抗体: |
| In Vivo | Bicalutamide (10 mg/kg；ig；每天；持续 28 天) 在前列腺癌小鼠模型中表现出抗肿瘤活性[2]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
| Formula | C18H9D5F4N2O4S |
| Molar Mass | 435.40 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216. [2]. Nicola J. Clegg,1 John Wongvipat,1,2 Jim Joseph, ARN-509: a novel anti-androgen for prostate cancer treatment. Cancer Res. 2012 March 15; 72(6): 1494-1503. |