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CAS RN: 68047-06-3 | 產品號碼: H1693
(Z)-4-Hydroxytamoxifen
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| 產品號碼 | H1693 |
| 純度/分析方法 | >95.0%(HPLC) |
| 分子式 / 分子量 | C__2__6H__2__9NO__2 = 387.52 |
| 外觀與形狀（20°C） | Solid |
| 儲存條件 | Frozen (<0°C) |
| 儲存在惰性氣體下 | Store under inert gas |
| 應避免的情況 | Air Sensitive,Hygroscopic,Heat Sensitive |
| CAS RN | 68047-06-3 |
| Reaxys-RN | 4910748 |
| MDL編號 | MFCD00468090 |
產品規格
| Appearance | White to Light yellow powder to crystal |
| Purity(HPLC) | min. 95.0 area% |
| Melting point | 152.0 to 156.0 °C |
| NMR | confirm to structure |
性質
| 熔點 | 154 °C |
GHS
| 圖形表示 |
|
| 信號詞 | Danger |
| 危險性說明 | H302 : Harmful if swallowed. H360 : May damage fertility or the unborn child. H362 : May cause harm to breast-fed children. H350 : May cause cancer. |
| 防範說明 | P501 : Dispose of contents/ container to an approved waste disposal plant. P263 : Avoid contact during pregnancy/ while nursing. P260 : Do not breathe dusts or mists. P270 : Do not eat, drink or smoke when using this product. P202 : Do not handle until all safety precautions have been read and understood. P201 : Obtain special instructions before use. P264 : Wash skin thoroughly after handling. P280 : Wear protective gloves/ protective clothing/ eye protection/ face protection. P308 + P313 : IF exposed or concerned: Get medical advice/ attention. P301 + P312 + P330 : IF SWALLOWED: Call a POISON CENTER/doctor if you feel unwell. Rinse mouth. P405 : Store locked up. |
相關法規
| RTECS # | SL1210000 |
運輸資料
| HS編碼* | 2922.19-000 |
Application
(Z)-4-Hydroxytamoxifen: An Active Metabolite of the Estrogen Receptor Modulator (SERM) Tamoxifem
Tamoxifen citrate [T2510] is a widely used non-steroidal antiestrogen agent for the treatment of hormone-dependent breast cancer. Tamoxifen is a prodrug and it is extensively metabolized by cytochrome P450 (CYP450) enzymes to active metabolites including (Z)-4-hydroxytamoxifen and endoxifen (4-hydroxy-N-desmethyltamoxifen). Each acts as an estrogen receptor antagonist in breast tissue. Tamoxifen is commonly referred to as a selective estrogen receptor modulator (SERM) because it acts as an estrogen receptor agonist in other tissues. (The product is for research purpose only.)
References
- Variable contribution of cytochromes P450 2D6, 2C9 and 3A4 to the 4-hydroxylation of tamoxifen by human liver microsomes
- Coactivator and corepressor regulation of the agonist/antagonist activity of the mixed antiestrogen, 4-hydroxytamoxifen
- Oxidative metabolism of tamoxifen to Z-4-hydroxytamoxifen hydroxytamoxifen by cytochrome P450 isoforms: An appraisal of in vitro studies (a review)
- Targeting of tamoxifen to enhance antitumour action for the treatment and prevention of breast cancer: The ‘personalised’ approach?
Application
CRISPR Genome Editing
(Z)-4-Hydroxytamoxifen enhances CRISPR-mediated homology-directed repair (HDR) efficiency.1-4)
References
- Small molecule-triggered Cas9 protein with improved genome-editing specificity
- Profiling of engineering hotspots identifies an allosteric CRISPR-Cas9 switch
- Multimode drug inducible CRISPR/Cas9 devices for transcriptional activation and genome editing
- HIT-Cas9: A CRISPR/Cas9 Genome-Editing Device under Tight and Effective Drug Control
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