R1128 B
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| Category | Bioactive by-products |
| Catalog number | BBF-03358 |
| CAS | 135161-97-6 |
| Molecular Weight | 312.3 |
| Molecular Formula | C18H16O5 |
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Description
R1128 B is a non-steroidal estrogen-receptor antagonist produced by Streptomyces sp. No. 1128. The IC50 value of R1128 B for partially purified rat uterine cytosol receptor was 1.2 x 10(-7) M.
Specification
| Synonyms | R1128B; R-1128B |
| IUPAC Name | 1-butyl-3,6,8-trihydroxyanthracene-9,10-dione |
| Canonical SMILES | CCCCC1=C2C(=CC(=C1)O)C(=O)C3=C(C2=O)C(=CC(=C3)O)O |
| InChI | InChI=1S/C18H16O5/c1-2-3-4-9-5-10(19)6-12-15(9)18(23)16-13(17(12)22)7-11(20)8-14(16)21/h5-8,19-21H,2-4H2,1H3 |
| InChI Key | PPZYTBDLRLLDOP-UHFFFAOYSA-N |
Properties
| Appearance | Brown Powder |
| Melting Point | 250-255°C |
Reference Reading
1. R1128 substances, novel non-steroidal estrogen-receptor antagonists produced by a Streptomyces. III. Pharmacological properties and antitumor activities
Y Hori, Y Abe, M Nishimura, T Goto, M Okuhara, M Kohsaka J Antibiot (Tokyo). 1993 Jul;46(7):1069-75. doi: 10.7164/antibiotics.46.1069.
R1128 B (1,3,6-trihydroxy-8-n-butylanthraquinone), a new antibiotic produced by Streptomyces sp. No. 1128, inhibited estrogen binding to its receptor. The IC50 value of R1128 B for partially purified rat uterine cytosol receptor was 1.2 x 10(-7) M. However, the IC50 value of R1128 B against androgen-receptor binding was about 50-fold greater than that against estrogen-receptor binding. R1128 B was a competitive inhibitor against estrogen-receptor binding. R1128 B inhibited the growth of estrogen-responsive human mammary adenocarcinoma MCF-7 cells in soft agar. This inhibition, however, was reversed when estradiol was added to the culture medium. R1128 B showed antitumor activities against MCF-7 both xenografted to nude mice and implanted in subrenal capsule of mice (SRC assay). The potency of R1128 B was about 8-fold lower than that of tamoxifen both in vitro and in vivo.
2. R1128 substances, novel non-steroidal estrogen-receptor antagonists produced by a Streptomyces. I. Taxonomy, fermentation, isolation and biological properties
Y Hori, Y Abe, M Ezaki, T Goto, M Okuhara, M Kohsaka J Antibiot (Tokyo). 1993 Jul;46(7):1055-62. doi: 10.7164/antibiotics.46.1055.
New non-steroidal estrogen-receptor antagonists, R1128 A, B, C and D, were isolated from the cultured broth of Streptomyces sp. No. 1128 by solvent extraction, silica gel chromatography, reverse phase chromatography and preparative HPLC. These compounds inhibited estrogen binding to its receptor. The IC50 values of R1128 A, B, C and D for partially purified rat uterine cytosol receptor were 1.1 x 10(-7) M, 1.2 x 10(-7) M, 2.6 x 10(-7) M and 2.7 x 10(-7) M, respectively.
3. R1128 substances, novel non-steroidal estrogen-receptor antagonists produced by a Streptomyces. II. Physico-chemical properties and structure determination
Y Hori, S Takase, N Shigematsu, T Goto, M Okuhara, M Kohsaka J Antibiot (Tokyo). 1993 Jul;46(7):1063-8. doi: 10.7164/antibiotics.46.1063.
R1128 A, B, C and D, new non-steroidal estrogen-receptor antagonists, were isolated from the cultured broth of Streptomyces sp. No. 1128. Their structures were elucidated to be 1,3,6-trihydroxy-8-alkylanthraquinones on the basis of their physico-chemical properties and spectroscopic data.
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Bio Calculators
* Our calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
It is commonly abbreviated as: C1V1 = C2V2
* Total Molecular Weight:
g/mol
Tip: Chemical formula is case sensitive. C22H30N4O √ c22h30n40 ╳
