tamoxifen

Tamoxifen is an orally active selective estrogen receptor modulator (SERM) that acts as an estrogen antagonist in breast cells and an agonist in bone, liver, and uterine cells. It can be used to induce gene knockout and liver injury models in mice, and also exhibits multiple biological activities, including activation of Hsp90, induction of autophagy and apoptosis, and inhibition of EBOV and MARV viral infections.

Tamoxifen-d5 is a deuterium labeled Tamoxifen. Tamoxifen is a selective modulator of estrogen receptor (SERM). Tamoxifen is a potent activator of Hsp90 and enhances the Hsp90 molecular chaperone ATPase activity.

Tamoxifen Citrate is an orally active selective estrogen receptor modulator (SERM) that blocks estrogen activity in breast cells while activating estrogen signaling in cells such as those of the bone, liver, and uterus. As an Hsp90 activator, it enhances the ATPase activity of the Hsp90 chaperone complex, induces autophagy and apoptosis, and can be used to generate gene knockout models in CreER(T2) transgenic mice as well as liver injury models.

4-Hydroxytamoxifen (ICI 79280) is the active metabolite of Tamoxifen, an estrogen receptor modulator (SERM) with selective and oral potency. 4-Hydroxytamoxifen has antitumor activity and may be used in breast cancer research.

α-Hydroxytamoxifen, a metabolite of tamoxifen, reacts with DNA and forms DNA adducts.

Tamoxifen analog II is a potent growth inhibitor. Tamoxifen analog II displays activity against various cancer cell lines.

FLTX1 is a fluorescent derivative of Tamoxifen, designed to efficiently target and label intracellular Tamoxifen-binding sites (estrogen receptors) both under permeabilized and non-permeabilized conditions. Additionally, FLTX1 demonstrates strong antiestrogenic activity in breast cancer cells, resembling the potent antiestrogenic properties of Tamoxifen. Notably, FLTX1 does not exhibit any estrogenic agonistic effect on the uterus.

(E/Z)-Endoxifen ((E/Z)-Endoxifen) is an active metabolite of tamoxifen produced by the sequential action of cytochrome P450 (CYP) isoforms, including CYP2D6. It is a strong anti-estrogen, as it has an approximately 100-fold greater affinity for estrogen receptors than tamoxifen. As the efficient conversion of tamoxifen to endoxifen depends on CYP2D6, polymorphisms in this CYP isoform can impact the effectiveness of TMX treatment.

Melatonin-Tamoxifen Conjugate (compound 16c) is an anticancer drug conjugate made of Melatonin and Tamoxifen, serving as an effective antagonist of ERα (IC50 = 863 nM). In cells expressing the hMT1 receptor, it binds to MLT receptors (Ki = 3.1 nM) and exhibits the ability to promote β-arrestin activation (EC50 = 914 nM) and ERK activation (EC50 = 98 nM). The IC50 values for Melatonin-Tamoxifen Conjugate in MCF-7, MDA-MB-231, and HT-1080 cell lines are 6.8 μM, 6.4 μM, and 1.7 μM, respectively.

Tamoxifen-PEG-Clozapine is an estrogen receptor α (ERα) PROTAC degrader. It targets ERα for degradation through the ubiquitin-proteasome system by utilizing the E3 ubiquitin ligase component N-recognin 5. This compound is applicable in cancer research. (Pink: ERα inhibitor; Black: linker; Blue: CRBN Ligand)

It is a metabolite of tamoxifen and an estrogen receptor modulator.

Tamoxifen-d3 hydrochloride is a deuterium-labeled derivative of Tamoxifen (Citrate), which is an orally active selective estrogen receptor modulator (SERM). It inhibits estrogen activity in breast cells while activating estrogen receptors in other cells such as those in bone, liver, and uterus. Tamoxifen Citrate acts as a potent Hsp90 activator, enhancing the ATPase activity of the Hsp90 molecular chaperone. Furthermore, it effectively suppresses infectious EBOV Zaire and Marburg (MARV) viruses with IC50 values of 0.1 μM and 1.8 μM, respectively. Tamoxifen Citrate also stimulates autophagy and induces apoptosis, and is capable of triggering gene knockout in CreER(T2) transgenic mice.

Tamoxifen (Standard) is the standard substance of Tamoxifen, and it is applicable for quantitative analysis, quality control, and related research in biochemical experiments. Tamoxifen is an orally active selective estrogen receptor modulator (SERM) that acts as an estrogen antagonist in breast cells and an agonist in bone, liver, and uterine cells. It can be used to induce gene knockout and liver injury models in mice, and also exhibits multiple biological activities, including activation of Hsp90, induction of autophagy and apoptosis, and inhibition of EBOV and MARV viral infections.

Tamoxifen citrate (Standard) is the standard substance of Tamoxifen citrate, and it is applicable for quantitative analysis, quality control, and related research in biochemical experiments. Tamoxifen Citrate is an orally active selective estrogen receptor modulator (SERM) that blocks estrogen activity in breast cells while activating estrogen signaling in cells such as those of the bone, liver, and uterus. As an Hsp90 activator, it enhances the ATPase activity of the Hsp90 chaperone complex, induces autophagy and apoptosis, and can be used to generate gene knockout models in CreER(T2) transgenic mice as well as liver injury models.

N-Desmethyltamoxifen hydrochloride is the primary metabolite of tamoxifen in humans.

N-Desmethyltamoxifen, the principal metabolite of tamoxifen in humans, serves as an efficacious modulator of ceramide metabolism within human AML cells by inhibiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation. Although it demonstrates weak antiestrogenic properties, it acts as a protein kinase C (PKC) inhibitor with a potency ten times greater than that of tamoxifen.

4'-Hydroxytamoxifen TFA, a salt form of a metabolite of Tamoxifen, demonstrates higher affinity for ER compared to Tamoxifen itself. This compound induces non-apoptotic cytotoxicity in human endometrial adenocarcinoma cells.

Tamoxifen is a medication that is used to prevent breast cancer patients.

(E)-4-Hydroxytamoxifen is a less active isomer of (Z)-4-hydroxytamoxifen and also is an estrogen receptor modulator.

(E/Z)-4-Hydroxytamoxifen (Afimoxifene) is a novel estrogen inhibitor, commonly used in research for various estrogen-dependent conditions, including cyclic mastalgia and gynecomastia.

(E)-4-Hydroxytamoxifen-d5 ((E)-Afimoxifene-d5) is the deuterated form of (E)-4-Hydroxytamoxifen. (E)-4-Hydroxytamoxifen ((E)-Afimoxifene) acts as an isomer of lower activity compared to (Z)-4-hydroxytamoxifen and functions as a modulator for the estrogen receptor.

Droloxifene (3-Hydroxytamoxifen), a tamoxifen derivative, is an oral active and selective estrogen receptor modulator.Droloxifene induced p53 expression and apoptosis in McF-7 cells.Fluroxifene has anti-estrogen and anti-implantation effects.Fluroxifene prevented bone loss in ovariectomized rats.

(E/Z)-Droloxifene is a mixture comprising (E)-Droloxifene, known as a selective estrogen receptor modulator, and (Z)-Droloxifene. (E)-Droloxifene binds to estrogen receptors (ER) in rabbit uterine homogenate with an IC50 of 24 nM. It increases uterine weight in immature rats and reduces the uterine weight increase caused by estradiol in juvenile rats. Additionally, (E)-Droloxifene inhibits the growth of human breast cancer cells MCF-7, ZR-75-1, and T47D stimulated by 17β-estradiol. In contrast, (Z)-Droloxifene shows weak binding to ER and exhibits neither estrogenic nor anti-estrogenic activity.

SIM010603 is a structurally novel, oral, multi-targeted receptor tyrosine kinase inhibitor. SIM010603 inhibited stem cell factor receptor (Kit), vascular endothelial growth factor receptor-2 (VEGFR-2), platelet-derived growth factor receptor-β (PDGFR-β), glial cell line-derived neurotrophic factor receptor (Rearranged during Transfection; RET), and Fms-like tyrosine kinase-3 (FLT3) with IC(50) values between 5.0 and 68.1 nmol/l. SIM010603 inhibited the phosphorylation of PDGFR-β and VEGFR-2. Moreover, SIM010603 inhibited endothelial cell proliferation, endothelial cells chemotaxis, and corneal angiogenesis.