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H3B-6545 Hydrochloride 

Cat. No.: HY-112596A
Handling Instructions

H3B-6545 Hydrochloride is an oral, selective estrogen receptor covalent antagonist (SERCA).

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

H3B-6545 Hydrochloride Chemical Structure

H3B-6545 Hydrochloride Chemical Structure

CAS No. : 2052132-51-9

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Other Forms of H3B-6545 Hydrochloride:

  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

Description

H3B-6545 Hydrochloride is an oral, selective estrogen receptor covalent antagonist (SERCA).

IC50 & Target

Estrogen receptor[1]

In Vitro

H3B-6545 is a highly selective small molecule that potently antagonizes wild-type and mutant ERα in biochemical and cell based assays. In vitro comparisons with standard of care and other experimental agents confirm increased cell potency of H3B-6545 under continuous as well as washout treatment conditions[1]. H3B-6545, a member of a novel class of ERα antagonists refer to as selective ER covalent antagonist (SERCA), which inactivates both wild-type and mutant ERα by targeting C530 and enforcing a unique antagonist conformation. H3B-6545 is a first-in-class selective ER covalent antagonist (SERCA). H3B-6545 inhibits ERαWT activity and growth of ERαWT -positive breast cancer lines. H3B-6545 potently inhibits ERαWT activity and suppresses proliferation of ERαWT -positive breast cancer lines. With GI50s of 0.3-0.4, 1.0, 0.5, 5.2, and 0.2 nM for MCF7, HCC1428, BT483, T47D and CAMA-1 cell lines[1].

In Vivo

In vivo, once daily oral dosing of H3B-6545 shows potent activity and superior efficacy to fulvestrant in the MCF-7 xenograft model with maximal antitumor activity at doses >10x below the maximum tolerated dose in mice. In addition, H3B-6545 shows superior antitumor activity to Tamoxifen and Fulvestrant in patient derived xenograft models of estrogen receptor positive breast cancer including models carrying ERα mutations in rat and monkeys, H3B-6545 is well tolerated across a broad dose range and at exposures that significantly exceed those required for efficacy in mouse xenograft models[1].

Clinical Trial
Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6555 mL 8.2776 mL 16.5552 mL
5 mM 0.3311 mL 1.6555 mL 3.3110 mL
10 mM 0.1656 mL 0.8278 mL 1.6555 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

604.04

Formula

C₃₀H₃₀ClF₄N₅O₂

CAS No.

2052132-51-9

SMILES

O=C(N(C)C)/C=C/CNCCOC1=NC=C(/C(C2=CC3=C(NN=C3F)C=C2)=C(C4=CC=CC=C4)/CC(F)(F)F)C=C1.Cl

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-6545 Hydrochloride
Cat. No.:
HY-112596A
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H3B-6545 Hydrochloride

Cat. No.: HY-112596A