151533-34-5 Usage
Description
The prodrug EM-800 is an orally active nonsteroidal anties trogen and is a triphenylethylene rigid analogue. EM-800 undergoes ester hydrolysis to the active m etabolite acolbifene. This fourth-generation antiestrogen is 200-fold more potent than tam oxifen in breast and uterine cancer cells and is effective in patients for whom tamoxifen therapy has failed. The mechanistic rationale for the effectiveness of acolbifene in tamoxifen-resistant tumors is based on the fact that it inhibits both the AF-1 and AF-2 activation pathways and does not poss ess any intrinsic estrogenic action. Acolbifene enjoys a 60% breast cancer cure rate. Structurally, acolbifene resembles raloxifene, with a benzopyran ring substituted for the benz othiophene ring. An additional benefit observed with acolbifene is its protective effect on bone loss. Adverse effects include nausea and vomiting.
Uses
rac-Acolbifene is a reacemic compound of Acolbifene (A190230) which is a selective estrogen receptor modulator (SERM) acting as pure antiestrogen. Acolbifene is also the orally active antiestrogen which is the most potent of the known antiestrogens and exerts pure antiestrogenic activity in the mammary gland and endometrium.
Check Digit Verification of cas no
The CAS Registry Mumber 151533-34-5 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,5,1,5,3 and 3 respectively; the second part has 2 digits, 3 and 4 respectively.
Calculate Digit Verification of CAS Registry Number 151533-34:
(8*1)+(7*5)+(6*1)+(5*5)+(4*3)+(3*3)+(2*3)+(1*4)=105
105 % 10 = 5
So 151533-34-5 is a valid CAS Registry Number.
151533-34-5Relevant articles and documents
Benzopyran-containing compounds and prodrug forms thereof
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Page 15, (2008/06/13)
Certain benzopyran antiestrogens are disclosed for treating estrogen sensitive diseases such as breast cancer. Prodrug forms provide ease of manufacturing, good shelf life, and bioavailibility.
