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品質等級
化驗
≥98% (HPLC)
形狀
powder
顏色
white to beige
溶解度
DMSO: 5 mg/mL, clear
儲存溫度
−20°C
SMILES 字串
C[C@]12C(C[C@@H](OC(C)=O)CC2)=CC[C@]3([H])[C@]1([H])CC[C@@]4(C)[C@@]3([H])CC=C4C5=CC=CN=C5
InChI
1S/C26H33NO2/c1-17(28)29-20-10-12-25(2)19(15-20)6-7-21-23-9-8-22(18-5-4-14-27-16-18)26(23,3)13-11-24(21)25/h4-6,8,14,16,20-21,23-24H,7,9-13,15H2,1-3H3/t20-,21-,23-,24-,25-,26+/m0/s1
InChI 密鑰
UVIQSJCZCSLXRZ-UBUQANBQSA-N
基因資訊
human ... CYP17A1(1586)
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應用
醋酸阿比特龙已被用于研究其抗肿瘤操作的三维微小肿瘤平台。
生化/生理作用
醋酸阿比特龙是阿比特龙的前药,是 CYP17A1 (CYP450c17) 的强效、选择性和口服生物利用度抑制剂,CYP17A1 是催化两个关键系列反应(17α羟化酶和 17,20 裂解酶)在雄激素和雌激素生物合成中导致 DHEA 和雄烯二酮的形成,最终可能被代谢为睾酮。CYP17 是睾丸和肾上腺中雄激素生物合成的关键酶,因此对它的抑制应停止两地雄激素的产生。醋酸阿比特龙用于治疗转移性去势抵抗性前列腺癌。 醋酸阿比特龙在多西他赛治疗后 CRPC(去势抵抗性前列腺癌)患者中具有显著的抗肿瘤活性。对睾丸、肾上腺和前列腺组织中的雄激素生物合成高度必需。
訊號詞
Danger
危險聲明
危險分類
Aquatic Chronic 1 - Repr. 1B - STOT RE 2
標靶器官
Endocrine system
儲存類別代碼
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
水污染物質分類(WGK)
WGK 3
閃點(°F)
Not applicable
閃點(°C)
Not applicable
其他客户在看
Journal of clinical oncology : official journal of the American Society of Clinical Oncology, 28(9), 1481-1488 (2010-02-18)
Abiraterone acetate is a prodrug of abiraterone, a selective inhibitor of CYP17, the enzyme catalyst for two essential steps in androgen biosynthesis. In castration-resistant prostate cancers (CRPCs), extragonadal androgen sources may sustain tumor growth despite a castrate environment. This phase
Journal of clinical oncology : official journal of the American Society of Clinical Oncology, 27(23), 3742-3748 (2009-05-28)
It has been postulated that castration-resistant prostate cancer (CRPC) commonly remains hormone dependent. Abiraterone acetate is a potent, selective, and orally available inhibitor of CYP17, the key enzyme in androgen and estrogen biosynthesis. This was a phase I/II study of
The Microwell-mesh: A high-throughput 3D prostate cancer spheroid and drug-testing platform.
Scientific Reports, 8(1) (2018)
Cancer research, 69(12), 4937-4940 (2009-06-11)
Abiraterone acetate is a potent, selective, and orally bioavailable small molecule inhibitor of CYP17, an enzyme that catalyzes two key serial reactions (17 alpha hydroxylase and 17,20 lyase) in androgen and estrogen biosynthesis. Clinical trials have confirmed that specific inhibition
Journal of clinical oncology : official journal of the American Society of Clinical Oncology, 28(9), 1489-1495 (2010-02-18)
The principal objective of this trial was to evaluate the antitumor activity of abiraterone acetate, an oral, specific, irreversible inhibitor of CYP17 in docetaxel-treated patients with castration-resistant prostate cancer (CRPC). In this multicenter, two-stage, phase II study, abiraterone acetate 1,000
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