H3B-6545 NEW
| Price | $1130 |
| Package | 25mg |
| Supply Ability: | 10g |
| Update Time: | 2026-05-11 |
Product Details
| Product Name: H3B-6545 | CAS No.: 2052130-80-8 |
| Supply Ability: 10g | Release date: 2026/05/11 |
Product Introduction
Bioactivity
| Name | H3B-6545 |
| Description | H3B-6545 is a selective estrogen receptor covalent antagonist (SERCA) that is orally available. As a novel class of ERα antagonists, H3B-6545 is used in the study of metastatic breast cancers, such as estrogen receptor-positive (ER), human epidermal growth factor receptor 2-negative (HER2-) breast cancer. |
| 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 demonstrated increased cellular potency of H3B-6545 under both continuous and washout treatment conditions.[1] |
| In vivo | H3B-6545, orally administered once daily, demonstrated potent activity and superior efficacy to fulvestrant in the MCF-7 xenograft model, with maximal antitumor activity at doses >10-fold below the maximum tolerated dose in mice. In addition, H3B-6545 demonstrated superior antitumor activity to tamoxifen and fulvestrant in xenograft models of estrogen receptor-positive breast cancer, including models harboring ERα mutations. In nonclinical safety studies in rats and monkeys, H3B-6545 was well tolerated over a wide dose range and at exposures significantly exceeding those required for efficacy in mouse xenograft models.[1] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween-80+45% Saline : 3.3 mg/mL (5.81 mM), Sonication is recommended. DMSO : 80 mg/mL (140.95 mM), Sonication is recommended. |
| Keywords | H3B-6545 | H-3B-6545 | H3B 6545 | Estrogen receptor |
| Inhibitors Related | Tamoxifen | Mifepristone | Estradiol | Astragaloside IV | Bisphenol B | Bisphenol Z | Mequinol | Phthalic acid | Ethisterone | Alpha-Estradiol | Ferrous Bisglycinate | Cholesterol |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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- Since: 2011-01-07
- Address: 36 Washington Street, Wellesley Hill, USA
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United States