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| Size | Price | Stock |
|---|---|---|
| 250mg | $700 | Check With Us |
| 500mg | $1150 | Check With Us |
| 1g | $1725 | Check With Us |
: Cat #: V33910 CAS #: 110025-28-0 Purity ≥ 99%
Description: Endoxifen, an active metabolite of Tamoxifen, is a potent and selective estrogen receptor antagonist and has been found to be effective in patients that have failed previous hormonal therapies. Endoxifen shows anti-estrogenic effects, and decreases the E2-induced PR expression in MCF-7 cells. Endoxifen also blocks ER-alpha transcriptional activity and inhibits estrogen-induced breast cancer cell proliferation. In MCF7, HS 578T, and BT-549 cells, Endoxifen significantly inhibits cell proliferation. Endoxifen also exhibits four-fold higher inhibition on PKC activity compared to tamoxifen.
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| Molecular Weight (MW) | 373.49 |
|---|---|
| Molecular Formula | C₂₅H₂₇NO₂ |
| CAS No. | 110025-28-0 |
| SMILES Code | CC/C(C1=CC=CC=C1)=C(C2=CC=C(O)C=C2)/C3=CC=C(OCCNC)C=C3 |
| Synonyms | Endoxifen; |
| Protocol | In Vitro | Endoxifen, a hydroxylated Tamoxifen metabolite, is approximately 100-fold more potent as an antagonist of the ER than tamoxifen. It also suggests that endoxifen but not 4-hydroxytamoxifen results in ER-alpha degradation in addition to its effects on the ER at the level of transcription. |
|---|---|---|
| In Vivo | Orally administered Endoxifen is rapidly absorbed and systemically available when tested in female rats. The Endoxifen-treated rats show 787% higher exposure (AUC0–∞) and 1,500% higher concentration (Cmax) levels of Endoxifen when compared with Tamoxifen. Oral Endoxifen administration once a day for 28 consecutive days at dosages 2, 4, and 8 mg/kg proves safe and results in progressive inhibition of the growth of the human mammary tumor xenografts in female mice. |
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 2.6774 mL | 13.3872 mL | 26.7745 mL | 53.5490 mL |
| 5mM | 0.5355 mL | 2.6774 mL | 5.3549 mL | 10.7098 mL |
| 10mM | 0.2677 mL | 1.3387 mL | 2.6774 mL | 5.3549 mL |
| 20mM | 0.1339 mL | 0.6694 mL | 1.3387 mL | 2.6774 mL |
This equation is commonly abbreviated as: C1 V1 = C2 V2
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.