bs-76422C

DATASHEET

Formulation Powder

Storage: Stable for 2 years after receipt when stored at +4°C.

Product Information:

CAS Number: 68392-35-8

Molecular formula: C26H29NO2

Molecular weight: 387.51

Purity: >98% (HPLC)

Appearance: White to yellow powder.

Solubility: Soluble in ethanol or methanol (both 5mg/ml).

InChiKey: TXUZVZSFRXZGTL-QPLCGJKRSA-N

SMILES: CC/C(C1=CC=CC=C1)=C(C2=CC=C(O)C=C2)/C3=CC=C(OCCN(C)C)C=C3

SMILES: CCC(=C(C1=CC=C(O)C=C1)C1=CC=C(OCCN(C)C)C=C1)C1=CC=CC=C1

Description:

4-Hydroxytamoxifen is an active metabolite of the chemotherapeutic drug tamoxifen, a selective estrogen receptor modulator (SERM) that acts as an agonist or antagonist in various tissues. 4-Hydroxytamoxifen acts as a tissue-selective agonist-antagonist of the estrogen receptors ERalpha and ERbeta. 4-Hydroxytamoxifen is an isoform-specific inhibitor of orphan estrogen-receptor-related (ERR) nuclear receptors beta and gamma. 4-Hydroxytamoxifen exhibits anticancer chemotherapeutic activity, inducing autophagy and vacuole formation as well as KRAS degradation in various cancer cell lines. In cardiac myocytes, 4-hydroxytamoxifen decreases Ca2+ amplitude, slowing relaxation and decreasing contractility. 4-Hydroxytamoxifen has also shown to be a potent inhibitor of the mitochondrial permeability transition (MPT).