Fulvestrant-3-boronic acid (Synonyms: ZB716)

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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.

For research use only. We do not sell to patients.

Fulvestrant-3-boronic acid Chemical Structure

CAS No. : 1853279-29-4

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Description

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.

Molecular Weight

634.59

Formula

C₃₂H₄₈BF₅O₄S

CAS No.

1853279-29-4

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

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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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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