SML1527
醋酸阿比特龙
≥98% (HPLC), CYP17A1 inhibitor, powder
别名:
CB 7598, 17-（吡啶-3-基）雄甾-5,16-二烯-3β-乙酸基
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关于此项目
经验公式（希尔记法）:
C26H33NO2
化学文摘社编号:
分子量:
391.55
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
MDL number:
产品名称
醋酸阿比特龙, ≥98% (HPLC)
SMILES string
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 key
UVIQSJCZCSLXRZ-UBUQANBQSA-N
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 5 mg/mL, clear
storage temp.
−20°C
Quality Level
Gene Information
human ... CYP17A1(1586)
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Application
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。
Biochem/physiol Actions
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。
signalword
Danger
hcodes
Hazard Classifications
Aquatic Chronic 1 - Repr. 1B - STOT RE 2
target_organs
Endocrine system
存储类别
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
涉药品监管产品
此项目有
Daniel C Danila et al.
Journal of clinical oncology : official journal of the American Society of Clinical Oncology, 28(9), 1496-1501 (2010-02-18)
Persistence of ligand-mediated androgen receptor signaling has been documented in castration-resistant prostate cancers (CRPCs). Abiraterone acetate (AA) is a potent and selective inhibitor of CYP17, which is required for androgen biosynthesis in the testes, adrenal glands, and prostate tissue. This
The Microwell-mesh: A high-throughput 3D prostate cancer spheroid and drug-testing platform.
E. O. Mosaad, et al.
Scientific Reports, 8(1) (2018)
Gerhardt Attard et al.
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
Charles J Ryan et al.
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
Gerhardt Attard et al.
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
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