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SML1527

醋酸阿比特龙

Name: 醋酸阿比特龙
Brand: SIGMA

≥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:

154229-18-2

分子量:

391.55

UNSPSC Code:

12352200

PubChem Substance ID:

329825944

NACRES:

NA.77

MDL number:

MFCD00934213

Assay:

≥98% (HPLC)

Form:

powder

Quality level:

100

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属性

产品名称

醋酸阿比特龙, ≥98% (HPLC)

Quality Level

100

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 5 mg/mL, clear

storage temp.

−20°C

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

Gene Information

human ... CYP17A1(1586)

说明

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。

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pictograms

GHS08,GHS09

signalword

Danger

hcodes

H360F,H373,H410

pcodes

P202 - P260 - P273 - P280 - P308 + P313 - P391

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

新产品

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历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

0000474873

0000353757

0000335765

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Antitumor activity with CYP17 blockade indicates that castration-resistant prostate cancer frequently remains hormone driven.

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

Abiraterone acetate preferentially enriches for the gut commensal Akkermansia muciniphila in castrate-resistant prostate cancer patients.

Brendan A Daisley et al.

Nature communications, 11(1), 4822-4822 (2020-09-26)

Abiraterone acetate (AA) is an inhibitor of androgen biosynthesis, though this cannot fully explain its efficacy against androgen-independent prostate cancer. Here, we demonstrate that androgen deprivation therapy depletes androgen-utilizing Corynebacterium spp. in prostate cancer patients and that oral AA further

Significant and sustained antitumor activity in post-docetaxel, castration-resistant prostate cancer with the CYP17 inhibitor abiraterone acetate.

Alison H M Reid et al.

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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货号	GTIN
SML1527-25MG	04061832868653
SML1527-5MG	04061832868660