Fulvestrant-3-boronic acid (Synonyms: ZB716)

Cat. No.: HY-137144 Purity: 99.7%: Data Sheet
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Handling Instructions
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Fulvestrant-3-boronic acid is an orally active ERα inhibitor, which binds to ERα competitively (IC₅₀ = 4.1 nM) and effectively degrades ERα in breast cancer cells.

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Fulvestrant-3-boronic acid 화학구조

CAS No. : 1853279-29-4

사이즈	재고	수량
1 mg	해외재고보유	Estimated Time of Arrival: December 31
5 mg	해외재고보유	Estimated Time of Arrival: December 31
10 mg	견적 받기
50 mg	견적 받기

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Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

Biological Activity
순도&문서
References
고객리뷰

제품 설명

Fulvestrant-3-boronic acid is an orally active ERα inhibitor, which binds to ERα competitively (IC₅₀ = 4.1 nM) and effectively degrades ERα in breast cancer cells^[1].

Cellular Effect

Cell Line	Type	Value	Description	References
MCF7	IC₅₀	0.0032 μM Compound: 5; ZB716	Antiproliferative activity against human MCF7 cells after 5 days by coulter counter analysis Antiproliferative activity against human MCF7 cells after 5 days by coulter counter analysis	[PMID: 27529700]
MCF7	IC₅₀	0.069 μM Compound: 5; ZB716	Antiproliferative activity against human tamoxifen-resistant MCF7 cells after 5 days by coulter counter analysis Antiproliferative activity against human tamoxifen-resistant MCF7 cells after 5 days by coulter counter analysis	[PMID: 27529700]
T47D	IC₅₀	0.0061 μM Compound: 5; ZB716	Antiproliferative activity against human T47D cells after 5 days by coulter counter analysis Antiproliferative activity against human T47D cells after 5 days by coulter counter analysis	[PMID: 27529700]
T47D	IC₅₀	0.037 μM Compound: 5; ZB716	Antiproliferative activity against human tamoxifen-resistant T47D cells over-expressing PKC-alpha after 5 days by coulter counter analysis Antiproliferative activity against human tamoxifen-resistant T47D cells over-expressing PKC-alpha after 5 days by coulter counter analysis	[PMID: 27529700]
T47D	IC₅₀	12.7 nM Compound: 5; ZB716	Downregulation of ER-alpha expression in human tamoxifen-resistant T47D cells over-expressing PKC-alpha measured after 5 days by Western blot analysis Downregulation of ER-alpha expression in human tamoxifen-resistant T47D cells over-expressing PKC-alpha measured after 5 days by Western blot analysis	[PMID: 27529700]
T47D	IC₅₀	7.8 nM Compound: 5; ZB716	Downregulation of ER-alpha expression in human T47D cells measured after 5 days by Western blot analysis Downregulation of ER-alpha expression in human T47D cells measured after 5 days by Western blot analysis	[PMID: 27529700]

In Vitro

Fulvestrant-3-boronic acid (1-27 nM, 5 d) dramatically down-regulates ERα protein expression in a dose-dependent manner in T47D and T47D/PKCα cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Fulvestrant-3-boronic acid (8.3 mg/kg, p.o.) exerts a T_1/2 of 23.5 h, a C_max of 169.8 ng/mL and an AUC of 2547.1 ng•h/mL^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

분자량

634.59

화학식

C₃₂H₄₈BF₅O₄S

CAS No.

1853279-29-4

Appearance

Solid

Color

White to off-white

SMILES

FC(F)(F)C(F)(F)CCCS(CCCCCCCCC[C@H]1[C@]2([H])[C@@](CC[C@]3([C@@]2([H])CC[C@@H]3O)C)([H])C4=CC=C(B(O)O)C=C4C1)=O

선적

Room temperature in continental US; may vary elsewhere.

보관

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

순도&문서

Purity: 99.7%

Select Batch:

Data Sheet (265 KB) SDS (563 KB)

COA (244 KB) Elemental Analysis Report (102 KB)

Handling Instructions (2659 KB)

References

[1]. Liu J, et al. Fulvestrant-3 Boronic Acid (ZB716): An Orally Bioavailable Selective Estrogen Receptor Downregulator (SERD). J Med Chem. 2016 Sep 8;59(17):8134-40. [Content Brief]

Fulvestrant-3-boronic acid Related Classifications

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The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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	×		=		×
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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Fulvestrant-3-boronic acid1853279-29-4ZB716ZB 716ZB-716Estrogen Receptor/ERRorally activeERαdegraderbreast cancerInhibitorinhibitorinhibit

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Fulvestrant-3-boronic acid (Synonyms: ZB716)

Fulvestrant-3-boronic acid Related Antibodies