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H3B-6545
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Catalog No. T11530LCas No. 2052130-80-8
Alias H3B6545
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.
H3B-6545
😃Good
Catalog No. T11530LAlias H3B6545Cas No. 2052130-80-8
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.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $197 | 8-10 weeks | |
| 5 mg | $492 | 8-10 weeks | |
| 10 mg | $729 | 8-10 weeks | |
| 25 mg | $1,130 | 8-10 weeks | |
| 1 mL x 10 mM (in DMSO) | $618 | 8-10 weeks |
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Product Introduction
Bioactivity
Chemical Properties
| 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] |
| Alias | H3B6545 |
| Molecular Weight | 567.58 |
| Formula | C30H29F4N5O2 |
| Cas No. | 2052130-80-8 |
| Relative Density. | 1.286 g/cm3 (Predicted) |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 80 mg/mL (140.95 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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