I4409

Fulvestrant

>98% (HPLC)

• 동의어(들): (7α,17β)-7-[9-[(4,4,5,5,5-Pentafluoropentyl)sulfinyl]nonyl]estra-1,3,5(10)-triene-3,17-diol, Faslodex, ICI 182,780, ZD 182780, ZD 9238, ZM 182780
• 실험식(Hill 표기법): C₃₂H₄₇F₅O₃S
• CAS Number: 129453-61-8
• Molecular Weight: 606.77
• MDL number: MFCD00903953
• UNSPSC 코드: 51111800
• PubChem Substance ID: 329815373
• NACRES: NA.77

속성

• Quality Level: 100
• 분석: >98% (HPLC)
• 양식: powder
• solubility: DMSO: >5 mg/mL
• 주관자: AstraZeneca
• 저장 온도: 2-8°C
• SMILES string: [H][C@]12CC[C@]3(C)[C@@H](O)CC[C@@]3([H])[C@]1([H])[C@H](CCCCCCCCCS(=O)CCCC(F)(F)C(F)(F)F)Cc4cc(O)ccc24
• InChI: 1S/C32H47F5O3S/c1-30-17-15-26-25-12-11-24(38)21-23(25)20-22(29(26)27(30)13-14-28(30)39)10-7-5-3-2-4-6-8-18-41(40)19-9-16-31(33,34)32(35,36)37/h11-12,21-22,26-29,38-39H,2-10,13-20H2,1H3/t22-,26-,27+,28+,29-,30+,41?/m1/s1
• InChI key: VWUXBMIQPBEWFH-WCCTWKNTSA-N
• 유전자 정보: human ... ESR1(2099) , ESR2(2100)

설명

애플리케이션

Fulvestrant has been used:

• as an antagonist of estrogen receptor (ERα and ERβ) to reduce hepatocytes proliferation[1]
• as an antagonist of ER for the suppression of estrogen responsive element in human breast cancer MCF-7 cells[2]
• as anti-estrogen in breast cancer cell lines[3]

생화학적/생리학적 작용

Fulvestrant (ICI 182,780) is a selective estrogen receptor down-regulator (SERD). Fulvestrant is a high affinity estrogen receptor antagonist. IC₅₀ = 0.29 nM. Fulvestrant is the first "pure" antiestrogen with no agonistic activity both in vitro and in vivo.

Fulvestrant is a 7α-alkylsulphinyl analog of 17β-oestradiol and is structurally different compared to other selective estrogen receptor (ER) modulators (SERMs). It reduces dimerization and nuclear localization of the estrogen receptor (ER). Fulvestrant lowers the level of ER protein in human breast cancer cells.[4] Fulvestrant is preferred for the treatment of women at their menopause having hormone-sensitive advanced breast cancer.[5]

Fulvestrant is a selective estrogen receptor down-regulator (SERD); high affinity estrogen receptor antagonist.

특징 및 장점

This compound is featured on the Nuclear Receptors (Steroids) page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

This compound was developed by AstraZeneca. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

안전성 정보

• 픽토그램: GHS08,GHS09
• 신호어: Danger
• 유해 및 위험 성명서: H360Df,H362,H410
• 예방조치 성명서: P202 - P260 - P263 - P264 - P273 - P308 + P313
• Hazard Classifications: Aquatic Chronic 1 - Lact. - Repr. 1B
• Storage Class Code: 6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
• WGK: WGK 3
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable
• 개인 보호 장비: Eyeshields, Gloves, type N95 (US)