H3B-6545 Hydrochloride NEW
| Price | $1140 | $1490 | $2530 |
| Package | 25mg | 50mg | 100mg |
| Supply Ability: | 10g |
| Update Time: | 2025-07-19 |
Product Details
| Product Name: H3B-6545 Hydrochloride | CAS No.: 2052132-51-9 |
| Supply Ability: 10g | Release date: 2025/07/19 |
Product Introduction
Bioactivity
| Name | H3B-6545 Hydrochloride |
| Description | H3B-6545 Hydrochloride is a selective, oral estrogen receptor covalent antagonist (SERCA). |
| In vitro | H3B-6545 is a highly selective small molecule that inhibits both wild-type (ERαWT) and mutant estrogen receptors (ERα), demonstrating potent activity against ERαWT-positive breast cancer cell lines (MCF7, HCC1428, BT483, T47D, and CAMA-1) with GI50s of 0.2-5.2 nM. It shows superior efficacy in biochemical and cell-based assays compared to standard treatments and other experimental agents, under continuous and washout conditions. H3B-6545 uniquely targets C530, enforcing a specific antagonist conformation, and is classified as a selective ER covalent antagonist (SERCA), representing a first-in-class therapeutic approach. |
| In vivo | Administered orally once daily, H3B-6545 demonstrates potent and superior anti-tumor efficacy compared to fulvestrant in the MCF-7 xenograft model, achieving maximal effectiveness at doses notably lower than the maximum tolerated dose in mice. Furthermore, H3B-6545 exhibits enhanced anti-tumor effects over Tamoxifen and Fulvestrant in patient-derived xenograft models of estrogen receptor-positive breast cancer, including those with ERα mutations, across various species including rats and monkeys. Notably, H3B-6545 is well-tolerated across a wide dosage range, maintaining significant efficacy at exposures well above those necessary in mouse xenograft models. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Keywords | H3B-6545 Hydrochloride | H-3B-6545 Hydrochloride | H3B6545 Hydrochloride | H3B 6545 Hydrochloride | Estrogen receptor |
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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- Address: 36 Washington Street, Wellesley Hill, USA
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