H3B-6545 NEW
| Price | $1130 |
| Package | 25mg |
| Supply Ability: | 10g |
| Update Time: | 2025-09-17 |
Product Details
| Product Name: H3B-6545 | CAS No.: 2052130-80-8 |
| Supply Ability: 10g | Release date: 2025/09/17 |
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 | DMSO : 80 mg/mL (140.95 mM), Sonication is recommended. |
| Keywords | H3B-6545 | H-3B-6545 | H3B 6545 | Estrogen receptor |
| Inhibitors Related | Kaempferol | Mifepristone | Estradiol | Astragaloside IV | Estradiol benzoate | Progesterone | Melatonin | Allura Red AC | 17α-Hydroxyprogesterone | Natamycin | Ethisterone | Estrone |
Company Profile Introduction
TargetMol Chemicals Inc. is headquartered in Boston, MA, and specializes in products and services that serve the research needs of chemical and biological scientists worldwide. With a client base in 40+ countries, TargetMol has evolved into one of the biggest global research suppliers for compound libraries and small molecule compounds.
170+ Compound Libraries， 10000+ Noval Small Molecucles，16000+ Nature Compounds
TargetMol diligently updates and offers over 170 types of compound libraries and a wide range of high-quality research chemicals, including inhibitors, activators, natural products, peptides, antibodies , and novel life-science kits for laboratory and scientific use. In addition, our lab allows us to conduct CADD (computer-aided drug design) and chemical synthesis to meet the customization needs of our clients.
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United States- Since: 2011-01-07
- Address: 36 Washington Street, Wellesley Hill, Massachusetts, USA
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