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Description: H3B-6545 is a novel, potent, orally bioavailable and selective small molecule modulator of wild-type and mutant Estrogen Receptor (ERalpha). Preclinical data indicates H3B-6545 inhibits the growth of cell line and patient-derived xenograft models of wild-type and mutant ERalpha with improved activity over standard-of-care therapies.
References:
1. PeterG. Smith, et al. Abstract DDT01-04: Discovery and development ofH3B-6545: A novel, oral, selective estrogen receptor covalent antagonist(SERCA) for the treatment of breast cancer.AACR Annual Meeting 2017; April 1-5.
2. Manav Korpal, et al. Development of a First-in-Class Oral Selective ER Covalent Antagonist (SERCA) for the Treatment of ERalphaWT and ERalphaMUT Breast Cancer.
3. Nonclinical pharmacokinetics and in vitro metabolism of H3B-6545, a novelselective ERalpha covalent antagonist (SERCA). Cancer Chemother Pharmacol. 2018 Nov1. doi: 10.1007/s00280-018-3716-3.
Note: The presented information and documents (Manual, Product Datasheet, Safety Datasheet and Certificate of Analysis) correspond to our latest update and should serve for orientational purpose only. We do not guarantee the topicality. We would kindly ask you to make a request for specific requirements, if necessary.
All products are intended for research use only (RUO). Not for human, veterinary or therapeutic use.
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