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ASC-J9 Sale

(Synonyms: 二甲基姜黄素,GO-Y025; Dimethylcurcumin; ASC J9; GO Y025) 目录号 : GC10547

A selective enhancer of AR degradation

ASC-J9 Chemical Structure

Cas No.:52328-98-0

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥577.00
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5mg
¥486.00
现货
10mg
¥810.00
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50mg
¥2,916.00
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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

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实验参考方法

Cell experiment [1]:

Cell lines

Human C4-2B/human THP1 cells and mouse TRAMP-C1/mouse RAW264.7 cells.

Preparation method

Soluble in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reaction Conditions

5 μM; 3 days.

Applications

ASC-J9 suppresses macrophage recruitment and suppresses PCa invasion.

Animal experiment [1]:

Animal models

Male 6- to 8-week-old nude mice with orthotopically xenografted 106 TRAMP-C1 cells.

Dosage form

75 mg/kg; i.p. injected three times per week for 3 weeks.

Applications

In mice, ASC-J9 significantly decreases developing distant metastatic tumors in diaphragm and lymph nodes. There are little change in mice body weight among all the mice treated.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Lin TH, Izumi K, Lee SO, et al. Anti-androgen receptor ASC-J9 versus anti-androgens MDV3100 (Enzalutamide) or Casodex (Bicalutamide) leads to opposite effects on prostate cancer metastasis via differential modulation of macrophage infiltration and STAT3-CCL2 signaling. Cell Death Dis, 2013, 4: e764.

产品描述

ASC-J9, is antitumor agent. ASC-J9 suppresses castration-resistant prostate cancer growth via degradation of full-length and splice variant androgen receptors targeting both fAR- and AR3-mediated PCa growth by ASC-J9 may represent the novel therapeutic approach to suppress castration-resistant PCa. ASC-J9 ameliorates spinal and bulbar muscular atrophy phenotype via degradation of androgen receptor.

The androgen receptor (AR) is a type of nuclear receptor that is activated by binding either of the androgenic hormones, testosterone, or dihydrotestosterone in the cytoplasm and then translocating into the nucleus. [1]The binding of an androgen to the androgen receptor(AR) results into a conformational change, in turn, which causes dissociation of HSP, transport from the cytosol into the cell nucleus, and dimerization. The AR dimer binds to a specific sequence of DNA known as HRE which can interact with other proteins in the nucleus, leading to up-regulation or down-regulation of specific gene transcription.[2]

ASC-J9, the AR degradation enhancer, suppressed both macrophage migration and subsequent PCa cell invasion. Additionally, ASC-J9 can regulate pSTAT3-CCL2 signaling using two pathways: an AR-dependent pathway via inhibiting PIAS3 expression and an AR-independent pathway via direct inhibition of the STAT3 phosphorylation/activation through mouse model in vivo with orthotopically injected TRAMP-C1 cells. In conclusion,a new and better therapeutic strategies using ASC-J9 alone or a combinational therapy that simultaneously targets androgens/AR signaling and PIAS3-pSTAT3-CCL2 signaling to better battle PCa growth and metastasis at castration-resistant stage.[3]

References:

1. Lu NZ. et al. "International Union of Pharmacology. LXV. The pharmacology and classification of the nuclear receptor superfamily: glucocorticoid, mineralocorticoid, progesterone, and androgen receptors". Pharmacol. Rev. 2006, 58 (4): 782–97.

2. Heemers HV, Tindall DJ. "Androgen receptor (AR) coregulators: a diversity of functions converging on and regulating the AR transcriptional complex". Endocr. Rev. 2007, 28 (7): 778–808.

3. Lin TH. et al. “Anti-androgen receptor ASC-J9 versus anti-androgens MDV3100 (Enzalutamide) or Casodex (Bicalutamide) leads to opposite effects on prostate cancer metastasis via differential modulation of macrophage infiltration and STAT3-CCL2 signaling.” Cell Death

Dis. 2013,4:e764

.

Chemical Properties

Cas No. 52328-98-0 SDF
别名 二甲基姜黄素,GO-Y025; Dimethylcurcumin; ASC J9; GO Y025
化学名 (1E,4Z,6E)-1,7-bis(3,4-dimethoxyphenyl)-5-hydroxyhepta-1,4,6-trien-3-one
Canonical SMILES COC1=C(C=C(C=C1)C=CC(=CC(=O)C=CC2=CC(=C(C=C2)OC)OC)O)OC
分子式 C23H24O6 分子量 396.43
溶解度 ≥ 16.65 mg/mL in DMSO 储存条件 Store at -20°C
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.5225 mL 12.6126 mL 25.2251 mL
5 mM 0.5045 mL 2.5225 mL 5.045 mL
10 mM 0.2523 mL 1.2613 mL 2.5225 mL
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