- Afimoxifene
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- $10.00
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2022-06-10
- CAS:68392-35-8
- Purity: 98%
- Supply Ability: 10000kg
- Afimoxifene
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- $1.00
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2020-02-05
- CAS:68392-35-8
- Min. Order: 1KG
- Purity: 98%-99.9%HPLC
- Supply Ability: 100KG
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| | Afimoxifene Basic information |
| | Afimoxifene Chemical Properties |
| Melting point | 135-144°C | | Boiling point | 514.4±50.0 °C(Predicted) | | density | 1.092 | | storage temp. | 2-8°C | | solubility | methanol: soluble10mg/mL | | form | solution | | pka | 9.38±0.15(Predicted) | | color | white to off-white | | Appearance | white solid | | biological source | synthetic | | Major Application | forensics and toxicology
pharmaceutical (small molecule) | | InChI | 1S/2C26H29NO2/c2*1-4-25(20-8-6-5-7-9-20)26(21-10-14-23(28)15-11-21)22-12-16-24(17-13-22)29-19-18-27(2)3/h2*5-17,28H,4,18-19H2,1-3H3/b26-25+;26-25- | | InChIKey | ZJLDABGSDWXVGE-BDSXMVAQSA-N | | SMILES | CC\C(c1ccccc1)=C(/c2ccc(O)cc2)c3ccc(OCCN(C)C)cc3.CC\C(c4ccccc4)=C(\c5ccc(O)cc5)c6ccc(OCCN(C)C)cc6 |
| Hazard Codes | Xn | | Risk Statements | 63-20/21/22 | | Safety Statements | 22-23-36 | | RIDADR | UN1170 - class 3 - PG 2 - Ethanol, solution | | WGK Germany | 3 | | RTECS | SL1210000 | | Storage Class | 11 - Combustible Solids | | Hazard Classifications | Acute Tox. 4 Dermal
Acute Tox. 4 Inhalation
Acute Tox. 4 Oral
Eye Irrit. 2
Repr. 2
Skin Irrit. 2 |
| | Afimoxifene Usage And Synthesis |
| Description | (E/Z)-4-Hydroxytamoxifen (4-OHT, cis/trans-4-hydroxytamoxifen, afimoxifene) is a selective estrogen receptor (ER) modulator, an active metabolite of tamoxifen. 4-Hydroxytamoxifen is widely used as a research tool for inducible genome manipulation.
4-Hydroxytamoxifen is used in the inducible Cre-LoxP system to control CreER/CreERT2 recombinase activity and trigger tissue-specific gene expression or genome/genetic modification (e.g., gene deletion). 4-Hydroxytamoxifen is a part of the TRAP/TRAP2 (targeted recombination in active populations) systems providing genetic access to neuron activity. It is also used in CRISPR/Cas9 gene editing to activate inactivated Cas9 nuclease.
Also, 4-Hydroxytamoxifen was reported to be an intramembranous lipid peroxidation inhibitor, exhibiting peroxyl radical scavenging activity. | | Chemical Properties | Off-White Solid | | Uses | A selective estrogen receptor modulator. | | Uses | (E/Z)-4-Hydroxy Tamoxifen is selective estrogen receptor modulator. | | Definition | ChEBI: Afimoxifene is a tertiary amino compound that is tamoxifen in which the phenyl group which is in a Z- relationship to the ethyl substituent is hydroxylated at the para- position. It is the active metabolite of tamoxifen. It has a role as an antineoplastic agent, an estrogen receptor antagonist and a metabolite. It is a tertiary amino compound and a member of phenols. It is functionally related to a tamoxifen. | | Brand name | TamoGel (Ascend Therapeutics). | | General Description | 4-Hydroxytamoxifen is a first generation, selective estrogen receptor modulator (SERM) that functions as an antagonist in breast cancer cells but can display estrogen-like activities in the uterus and bone. | | Biological Activity | 4-hydroxytamoxifen is an estrogen receptor modulator.estrogen receptor can be selectively stimulated or inhibited, providing promising therapeutic opportunities for auto-immune diseases, prostate and breast cancer, as well as depression. | | Biochem/physiol Actions | Metabolite of the chemotherapeutic drug tamoxifen, exhibiting more potent estrogen agonist/antagonist activity than the parent drug. Also active as intra-membranous inhibitor of lipid peroxidation. | | in vitro | previous study was conducted to evaluate the effects of tamoxifen and its active metabolite 4-hydroxytamoxifen on isolated rat cardiac myocyte mechanical function and calcium handling. results showed that myocytes treated with 4-hydroxytamoxifen had similarly to tamoxifen-treated cells to both calcium handling and contractility [1]. | | in vivo | previous animal study compared the extent of dna adduct formation in sd rats treated with seven tamoxifen or 4-hydroxytamoxifen. results showed that the liver weights and microsomal rates were not changed by tamoxifen or 4-hydroxytamoxifen treatment. moreover, the uterine weights were significantly decreased and uterine peroxidase activity was marginally decreased in tamoxifen or 4-hydroxytamoxifen treated rats. in addition, hepatic dna adduct levels in rats treated with 4-hydroxytamoxifen did not differ from control rats. similaryly, the adduct levels in uterus dna from rats treated with tamoxifen or 4-hydroxytamoxifen were not different from those in control rats [2]. | | IC 50 | 27 and 18 μm for mcf-7 and mda-mb-231 cell proliferation | | storage | -20°C | | references | [1] asp ml,martindale jj,metzger jm. direct, differential effects of tamoxifen, 4-hydroxytamoxifen, and raloxifene on cardiac myocyte contractility and calcium handling. plos one.2013 oct 24;8(10):e78768.
[2] beland fa,mcdaniel lp,marques mm. comparison of the dna adducts formed by tamoxifen and 4-hydroxytamoxifen in vivo. carcinogenesis.1999 mar;20(3):471-7.
[3] lee o et al. a randomized phase ii presurgical trial of transdermal 4-hydroxytamoxifen gel versus oral tamoxifen in women with ductal carcinoma in situ of the breast. clin cancer res.2014 jul 15;20(14):3672-82. |
| | Afimoxifene Preparation Products And Raw materials |
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