Taragarestrant (Synonyms: D-0502)

Cat. No.: HY-147402: FAQs
Data Sheet Handling Instructions Technical Support

Taragarestrant (D-0502) is a potent, orally active and selective estrogen receptor degrader (SERD). Taragarestrant shows potent activity in various ER+ breast cancer cell lines and xenograft models.

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

Taragarestrant Chemical Structure

CAS No. : 2118899-51-5

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Other Forms of Taragarestrant:

Taragarestrant meglumine Get quote

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View All Estrogen Receptor/ERR Isoform Specific Products:

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Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

Biological Activity
Purity & Documentation
References
Customer Review

Description

Cellular Effect

Cell Line	Type	Value	Description	References
ES-2	IC₅₀	46.4 nM Compound: D4	Displacement of Fluormone ES2 from full length human ERalpha incubated for 60 min by fluorescent polarization assay Displacement of Fluormone ES2 from full length human ERalpha incubated for 60 min by fluorescent polarization assay	[PMID: 34056898]
MCF7	IC₅₀	2.07 nM Compound: D4	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 5 days by Cell Titer Glo assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 5 days by Cell Titer Glo assay	[PMID: 34056898]

In Vivo

Taragarestrant (D-0502) exhibits superior PK profiles suitable for clinical development^[1].

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

Clinical Trial

Molecular Weight

475.38

Formula

C₂₅H₂₅Cl₂FN₂O₂

CAS No.

2118899-51-5

SMILES

CC(C)(F)CN1[C@@](C2=C(C=C(C=C2Cl)/C=C/C(O)=O)Cl)([H])C3=C(C[C@H]1C)C4=CC=CC=C4N3

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]. Lin WY, et, al. Abstract 5776: Pharmacologic and PK/PD study of D-0502: An orally bioavailable SERD with potent antitumor activity in ER-positive breast cancer cell lines and xenograft models. 2018 Jul 1;78(13):5776.

[2]. WHO Drug Information. International Nonproprietary Names for Pharmaceutical

Taragarestrant Related Classifications

Cancer

Molarity Calculator
Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass		Concentration		Volume		Molecular Weight *
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The dilution calculator equation

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)	×	Volume _(start)	=	Concentration _(final)	×	Volume _(final)
	×		=		×
C1		V1		C2		V2

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:

Taragarestrant2118899-51-5D-0502D0502D 0502Estrogen Receptor/ERRbreast cancer cellanticancerorally activeSERDInhibitorinhibitorinhibit

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