2. Vitamin D Related/Nuclear Receptor
  3. Estrogen Receptor/ERR
  4. Taragarestrant

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.

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Taragarestrant

Taragarestrant 構造式

CAS 番号 : 2118899-51-5

容量 在庫状況
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Other Forms of Taragarestrant:

Taragarestrant 関連抗体

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Estrogen Receptor/ERR アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

  • 生物活性

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製品説明

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[1][2].

Cellular Effect
Cell Line Type Value Description References
ES-2 IC50
46.4 1
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]
ES-2 IC50
46.4 1
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 1
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]
MCF7 IC50
2.07 1
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]
MCF7 IC50
2.07 1
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]
ES-2 IC50
46.4 1
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]
体内実験

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.
分子量

475.38

分子式

C25H25Cl2FN2O2
CAS 番号
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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
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Taragarestrant Related Classifications

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一般には略語で表示されます：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:

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

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製品名:
Taragarestrant
製品番号:
HY-147402
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