A selective estrogen receptor (ER) modulator used as adjuvant therapy for estrogen-dependent breast cancer; increases ER activity in bone

Tamoxifen (citrate) – 5 g

Brand:
Cayman
CAS:
54965-24-1
Storage:
-20
UN-No:
Non-Hazardous - /

Tamoxifen (TMX) is a selective estrogen receptor (ER) modulator used as adjuvant therapy for estrogen-dependent breast cancer.{17814} TMX treatment serves to increase ER activity in bone, uterus, and the cardiovasculature system as it decreases ER activity in breast tissues.{10559} TMX is metabolized by cytochrome P450 (CYP450) enzymes to the active metabolites N-desmethyl-TMX, 4-hydroxy-N-desmethyl-TMX (endoxifen), and 4-hydroxy-TMX, indicating that certain CYP450 isoforms may be crucial for some of the effects of TMX.{20776} In addition, TMX binds microsomal antiestrogen binding sites, altering cholesterol esterification at therapeutic doses and impacting breast cancer cell differentiation, apoptosis, and autophagy.{20775}  

 

Available on backorder

Add to quotes
SKU: 11629 - 5 g Category:

Description

A selective estrogen receptor (ER) modulator used as adjuvant therapy for estrogen-dependent breast cancer; increases ER activity in bone, uterus, and the cardiovasculature system as it decreases ER activity in breast tissues; metabolized by CYP450 enzymes to active metabolites; alters cholesterol esterification at therapeutic doses

Formal name: 2-[4-[(1Z)-1,2-diphenyl-1-buten-1-yl]phenoxy]-N,N-dimethyl-ethanamine, 2-hydroxy-1,2,3-propanetricarboxylate

Synonyms:  ICI 46474|Istubal|Kessar|Noltam|Nolvadex|TMX|Valodex|Zemide

Molecular weight: 563.6

CAS: 54965-24-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Cancer|Autophagy||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Endocrinology & Metabolism|Bone Growth & Remodeling||Research Area|Endocrinology & Metabolism|Hormones & Receptors|Estrogens & Progestins||Research Area|Endocrinology & Metabolism|Reproductive Biology

Related products

  • A powerful effector in both the TetR and revTetR transcriptional regulator systems

    Anhydrotetracycline (hydrochloride) – 250 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 - 250 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • 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
  • 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
  • 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