1. Others
  2. Estrogen Receptor/ERR
  3. H3B-6545

H3B-6545 

Cat. No.: HY-112596 Purity: >99.0%
Handling Instructions

H3B-6545 is an oral, selective estrogen receptor covalent antagonist (SERCA) for the research of metastatic ER-positive, HER2-negative breast cancer.

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

H3B-6545 Chemical Structure

H3B-6545 Chemical Structure

CAS No. : 2052130-80-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 437 In-stock
Estimated Time of Arrival: December 31
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3050 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of H3B-6545:

Top Publications Citing Use of Products

View All Estrogen Receptor/ERR Isoform Specific Products:

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

H3B-6545 is an oral, selective estrogen receptor covalent antagonist (SERCA) for the research of metastatic ER-positive, HER2-negative breast cancer[1][2].

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].

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

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].

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

Clinical Trial
Molecular Weight

567.58

Formula

C₃₀H₂₉F₄N₅O₂

CAS No.

2052130-80-8

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
References

Purity: >99.0%

  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

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

Keywords:

H3B-6545Estrogen Receptor/ERRInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
H3B-6545
Cat. No.:
HY-112596
Quantity:
MCE Japan Authorized Agent: