A selective estrogen receptor degrader; binds to rat uterine ER (IC50 = 44.8 nM); prevents increases in uterine weight induced by estradiol in immature rats (ED50 = 0.06 mg/kg per day); inhibits the growth of ER-positive MCF-7 human breast cancer cells at 1 µg/ml; prevents tumor growth in MCF-7 and Br10 breast cancer mouse xenograft models at 1 µg/ml; neuroprotective in vitro against neurotoxicity induced by glutamate- and Aβ42

Fulvestrant – 10 mg

Brand:
Cayman
CAS:
129453-61-8
Storage:
-20
UN-No:
Non-Hazardous - /

Fulvestrant is a selective estrogen receptor degrader (SERD) that downregulates and degrades estrogen receptor α (ERα).{16606,43228} It binds to rat uterine ER with an IC50 value of 44.8 nM and prevents uterine weight increases induced by estradiol in immature rats (ED50> = 0.06 mg/kg per day) but has no effect on uterine weight alone.{43229} It also decreases uterine weight in adult rats without affecting the production of luteinizing and follicle-stimulating hormones and prolactin. Fulvestrant inhibits the growth of ER-positive MCF-7 human breast cancer cells but not ER-negative BT-20 cells when used at a concentration of 1 µg/ml. It also prevents tumor growth in MCF-7 and Br10 breast cancer mouse xenograft models when used at a single dose of 5 mg per animal. Fulvestrant is neuroprotective in vitro against neurotoxicity induced by glutamate- and amyloid-β (1-42) (Aβ42) in primary rat hippocampal cells.{16605} Formulations containing fulvestrant have been used in the treatment of estrogen-sensitive breast cancer.  

 

Available on backorder

Add to quotes
SKU: 10011269 - 10 mg Category:

Description

A selective estrogen receptor degrader; binds to rat uterine ER (IC50 = 44.8 nM); prevents increases in uterine weight induced by estradiol in immature rats (ED50 = 0.06 mg/kg per day); inhibits the growth of ER-positive MCF-7 human breast cancer cells at 1 µg/ml; prevents tumor growth in MCF-7 and Br10 breast cancer mouse xenograft models at 1 µg/ml; neuroprotective in vitro against neurotoxicity induced by glutamate- and Aβ42

Formal name: 7α-[9-[(4,4,5,5,5-pentafluoropentyl)sulfinyl]nonyl]-estra-1,3,5(10)-triene-3,17β-diol

Synonyms:  ICI 182780

Molecular weight: 606.8

CAS: 129453-61-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Lipids|Sterol Lipids||Product Type|Biochemicals|Receptor Pharmacology||Research Area|Cancer||Research Area|Endocrinology & Metabolism|Hormones & Receptors|Estrogens & Progestins

Related products

  • A potent inhibitor of Cdk2/cyclin E with an IC50 value of 0.1 µM; also inhibits Cdk7/cyclin H

    (R)-Roscovitine – 5 mg

    Cyclin-dependent kinases (CDKs) are key regulators of cell cycle progression and are therefore promising targets for cancer therapy. (R)-Roscovitine is a potent inhibitor of Cdk2/cyclin E with an IC50 value of 0.1 µM.{14988} It also inhibits Cdk7/cyclin H, Cdk5/p35, and cell division cycle (cdc)/cyclin B with IC50 values of 0.49, 0.16, and 0.65 µM, respectively.{14987,14988,14991} (R)-Roscovitine inhibits the growth of rapidly proliferating cells with an average IC50 value of 15.2 µM against a panel of 19 human tumor cell lines.{14988} In murine models of polycystic kidney disease, (R)-roscovitine effectively inhibited disease progression at doses of 50-100 mg/kg.{14564}  

     

    Brand:
    Cayman
    SKU:10009569 - 5 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • PtdIns-(3

    PtdIns-(3,4,5)-P3-biotin (sodium salt) – 100 µg

    The PtdIn phosphates play an important role in the generation and transduction of intracellular signals.{8344,4096,14518} PtdIns-(3,4,5)-P3-biotin is an affinity probe which allows the PIP3 to be detected through an interaction with the biotin ligand. This design allows PtdIns-(3,4,5)-P3-biotin to serve as a general probe for any protein with a high affinity binding interaction with inositol-(3,4,5)-triphosphate phospholipids, such as phosphatidylinositol 3-kinase, PTEN, or PH-domain-containing proteins.  

     

    Brand:
    Cayman
    SKU:10009531 - 100 µg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • A zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers

    1,2-Dipalmitoyl-sn-glycero-3-PC – 100 mg

    1,2-Dipalmitoyl-sn-glycero-3-PC (DPPC) is a zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers, bilayers, and liposomes for use in a variety of applications.{14480,24261,14478,14479} It has been used in the formation of proteoliposomes for implantation of γ-glutamyl transpeptidase into human erythrocyte membranes.{14478} Incorporation of glycosphingolipid antigens into DPPC-containing liposomes increases the immunogenicity of the antigens in mice.{14479}  

     

    Brand:
    Cayman
    SKU:10009473 - 100 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • A powerful effector in both the TetR and revTetR transcriptional regulator systems

    Anhydrotetracycline (hydrochloride) – 500 mg

    The tetracycline repressor (TetR) is a transcriptional regulator which normally binds tightly to its palindromic tetO operator DNA, blocking gene expression.{17508} Tet causes the repressor to dissociate from the DNA, allowing transcription to occur. A novel reverse TetR (revTetR) requires tetracycline as a co-repressor to bind tetO and block transcription.{17509,17510} Anhydrotetracycline (hydrochloride) is a powerful effector in both the tetracycline repressor (TetR) and reverse TetR (revTetR) systems, binding the Tet repressor 35-fold more strongly than Tet.{17508,17511} Moreover, anhydrotetracycline poorly binds the 30S ribosomal subunit, compared to Tet,{17512} so it does not act as a general inhibitor of translation and is a poor antibiotic. Perhaps related to this, the concentration of anhydrotetracycline that inhibits eukaryotic cell growth is more than a 1,000-fold above the dose that alters transcription through TetR.{17508}  

     

    Brand:
    Cayman
    SKU:10009542 - 500 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page