Fulvestrant

Fulvestrant Structure
Fulvestrant structure
Common Name Fulvestrant
CAS Number 129453-61-8 Molecular Weight 606.771
Density 1.2±0.1 g/cm3 Boiling Point 674.8±55.0 °C at 760 mmHg
Molecular Formula C32H47F5O3S Melting Point 104-106°C
MSDS Chinese USA Flash Point 361.9±31.5 °C

Combined histone deacetylase inhibition and tamoxifen induces apoptosis in tamoxifen-resistant breast cancer models, by reversing Bcl-2 overexpression.

Breast Cancer Res. 17 , 26, (2015)

The emergence of hormone therapy resistance, despite continued expression of the estrogen receptor (ER), is a major challenge to curing breast cancer. Recent clinical studies suggest that epigenetic modulation by histone deacetylase (HDAC) inhibitors reverses...

PKA signaling drives mammary tumorigenesis through Src.

Oncogene 34(9) , 1160-73, (2015)

Protein kinase A (PKA) hyperactivation causes hereditary endocrine neoplasias; however, its role in sporadic epithelial cancers is unknown. Here, we show that heightened PKA activity in the mammary epithelium generates tumors. Mammary-restricted biallelic abl...

Elevated peritoneal expression and estrogen regulation of nociceptive ion channels in endometriosis.

J. Clin. Endocrinol. Metab. 99(9) , E1738-43, (2014)

Ovarian suppression is a common treatment for endometriosis-associated pelvic pain. Its exact mechanism of action is poorly understood, although it is assumed to reflect reduced production/action of estrogens.The objective of the study was to measure the expr...

Cross-talk between ER and HER2 regulates c-MYC-mediated glutamine metabolism in aromatase inhibitor resistant breast cancer cells.

J. Steroid Biochem. Mol. Biol. 149 , 118-27, (2015)

Resistance to endocrine therapies in hormone receptor (HR)-positive breast cancer is a significant clinical problem for a considerable number of patients. The oncogenic transcription factor c-MYC (hereafter referred to as MYC), which regulates glutamine metab...

Aromatase (Cyp19a1b) in the pituitary is dynamically involved in the upregulation of lhb but not fshb in the vitellogenic female ricefield eel Monopterus albus.

Endocrinology 155(11) , 4531-41, (2014)

Aromatase, encoded by Cyp19a1, is expressed in the pituitary of vertebrates; however, its physiological relevance remains poorly defined. In teleosts, the duplicated cyp19a1b is preferentially expressed in the pituitary where LH and FSH are synthesized in dis...

17β-Estradiol Abrogates Apoptosis Inhibiting PKCδ, JNK, and p66Shc Activation in C2C12 Cells.

J. Cell. Biochem. 116 , 1454-65, (2015)

17β-Estradiol (E2) protects several non-reproductive tissues from apoptosis, including skeletal muscle. Previously, we showed that E2 at physiological concentrations prevented apoptosis induced by H2O2 in skeletal myoblasts. As we have also demonstrated a cle...

Aurora kinase A and B as new treatment targets in aromatase inhibitor-resistant breast cancer cells.

Breast Cancer Res. Treat. 149(3) , 715-26, (2015)

Aromatase inhibitors (AIs) are used for treatment of estrogen receptor α (ER)-positive breast cancer; however, resistance is a major obstacle for optimal outcome. This preclinical study aimed at identifying potential new treatment targets in AI-resistant brea...

A kinase inhibitor screen identifies Mcl-1 and Aurora kinase A as novel treatment targets in antiestrogen-resistant breast cancer cells.

Oncogene 34 , 4199-210, (2015)

Antiestrogen resistance is a major problem in breast cancer treatment. Therefore, the search for new therapeutic targets and biomarkers for antiestrogen resistance is crucial. In this study, we performed a kinase inhibitor screen on antiestrogen responsive MC...

Aurora kinase B is important for antiestrogen resistant cell growth and a potential biomarker for tamoxifen resistant breast cancer.

BMC Cancer 15 , 239, (2015)

Resistance to antiestrogen therapy is a major clinical challenge in the treatment of estrogen receptor α (ER)-positive breast cancer. The aim of the study was to explore the growth promoting pathways of antiestrogen resistant breast cancer cells to identify b...

Overcoming endocrine resistance due to reduced PTEN levels in estrogen receptor-positive breast cancer by co-targeting mammalian target of rapamycin, protein kinase B, or mitogen-activated protein kinase kinase.

Breast Cancer Res. 16(5) , 430, (2015)

Activation of the phosphatidylinositol 3-kinase (PI3K) pathway in estrogen receptor α (ER)-positive breast cancer is associated with reduced ER expression and activity, luminal B subtype, and poor outcome. Phosphatase and tensin homolog (PTEN), a negative reg...