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  2. Estrogen Receptor/ERR

H3B-5942 

Cat. No.: HY-112611
Handling Instructions

H3B-5942 is a selective, irreversible and orally active estrogen receptor covalent antagonist, inactivates both wild-type and mutant ERα by targeting Cys530, with Kis of 1 nM and 0.41 nM, respectively. H3B-5942 reduces ERα target gene GREB1, shows potent antitumor activity both in multiple cell lines or animals bearing ERαWT or ERα mutations.

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

H3B-5942 Chemical Structure

H3B-5942 Chemical Structure

CAS No. : 2052128-15-9

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  • Biological Activity

  • Technical Information

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Description

H3B-5942 is a selective, irreversible and orally active estrogen receptor covalent antagonist, inactivates both wild-type and mutant ERα by targeting Cys530, with Kis of 1 nM and 0.41 nM, respectively. H3B-5942 reduces ERα target gene GREB1, shows potent antitumor activity both in multiple cell lines or animals bearing ERαWT or ERα mutations[1].

IC50 & Target[1]

ERαY537S

0.41 nM (Ki)

ERαWT

1 nM (Ki)

In Vitro

H3B-5942 is a selective and irreversible estrogen receptor covalent antagonist, inactivates both wild-type and mutant ERα by targeting Cys530, with Kis of 1 nM and 0.41 nM, respectively[1].
H3B-5942 elevates ERα protein level distinct from SERMs/SERD, blocks ERα-dependent transcription in breast cancer cells. H3B-5942 (0.01-10 μM) reduces ERα target gene GREB1 in MCF7-ERαWT, various MCF7-ERαMUT lines, and the PDX-ERαY537S/WT line[1].
H3B-5942 also decreases proliferation of MCF7-Parental, MCF7-LTED-ERαWT, and MCF7-LTED-ERαY537C lines with GI50s of 0.5, 2, and 30 nM, respectively. H3B-5942 (10-25 nM) in combination with CDK4/6 inhibitors (≥25 pM) has synergic inhibitory effect on multiple cell lines bearing ERαWT or clinically frequent ERα mutations[1].

In Vivo

H3B-5942 (1, 3, 10, or 30 mg/kg, p.o, q.d.) dose-dependently inhibits tumor growth in MCF7 xenograft model in athymic female nude mice. H3B-5942 (3, 10, 30, 100, and 200 mg/kg, p.o, q.d.) exhibits similar anti-tumor activity in the ERαY537S/WT ST941 model in athymic female nude mice[1].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0217 mL 10.1086 mL 20.2171 mL
5 mM 0.4043 mL 2.0217 mL 4.0434 mL
10 mM 0.2022 mL 1.0109 mL 2.0217 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

494.63

Formula

C₃₁H₃₄N₄O₂

CAS No.

2052128-15-9

SMILES

CC/C(C1=CC=CC=C1)=C(C2=CC=C(OCCNC/C=C/C(N(C)C)=O)C=C2)\C3=CC(C=NN4)=C4C=C3

Storage

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

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
H3B-5942
Cat. No.:
HY-112611
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H3B-5942

Cat. No.: HY-112611