- AZD3514
| ASC-J9AR degradation enhancer,antiumor agent |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
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- Purity = 98.00%
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Chemical structure
Related Biological Data
| Description | ASC-J9 is an enhancer of androgen receptor degradation. | |||||
| Targets | PC-3 cell proliferation | LNCaP cell proliferation | ||||
| IC50 | 5.9 μM | 3.9 μM | ||||
| 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. | |
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| Cas No. | 52328-98-0 | SDF | Download SDF |
| Synonyms | GO-Y025; Dimethylcurcumin; ASC J9; GO Y025 | ||
| Chemical Name | (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 | ||
| Formula | C23H24O6 | M.Wt | 396.43 |
| Solubility | ≥16.65 mg/mL in DMSO, <2.22 mg/ml="" in="" etoh,=""><2.55 mg/ml="" in="" h2o=""> | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
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
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为了使供输血用的血液能保存一定时间，加入适当的抗凝剂，并尽量防止在保存期发生变质而用的液体。为了防止因糖的消失引起活力降低，尚加入葡萄糖。ACD液（含柠檬酸三钠、柠檬酸、葡萄糖）一般用于血库。添加ACD的血液放在4—6℃条件下保存，可保存三周。另外为防止柠檬酸盐的过量可用加磷酸钠的CPD液。此外还设计了加乳酸钠的ACDL液。如果加入甘油等防冻剂则可长时间冷冻保存红细胞。
目前选择这个都是北京博凌科为生物科技有限公司的
目前正在从新鲜病人肿瘤组织标本中提取细胞悬液进行阳性细胞的筛选，但由于实验室距离医院有3个小时的车程，请问什么储存方法或者储存液能短期保证肿瘤组织中细胞完整性？谢谢
