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H3B-6545

Cat. No. M14631
H3B-6545 Structure
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Biological Activity

H3B-6545 is an oral, selective estrogen receptor covalent antagonist (SERCA) for the research of metastatic ER-positive, HER2-negative breast cancer.

Chemical Information
Molecular Weight 567.58
CAS Number 2052130-80-8
Solubility (25°C) DMSO 150 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Craig Furman, et al. Covalent ERα Antagonist H3B-6545 Demonstrates Encouraging Preclinical Activity in Therapy-Resistant Breast Cancer

[2] No authors listed. Novel Agents Show Promise Against Acquired Endocrine Resistance in ER+ Advanced Breast Cancer

[3] Dong Zhang, et al. Characterization of the metabolites of H3B-6545 in vitro and in vivo by using ultra-high performance liquid chromatography combined with electrospray ionization linear ion trap-orbitrap tandem mass spectrometry

[4] Yingying Ge, et al. Pharmacokinetics and metabolism of H3B-6545, a selective estrogen receptor covalent antagonist, in dog plasma by liquid chromatography combined with electrospray ionization tandem mass spectrometry

[5] Nathalie Rioux, et al. Nonclinical pharmacokinetics and in vitro metabolism of H3B-6545, a novel selective ERα covalent antagonist (SERCA)

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Keywords: H3B-6545 supplier, Estrogen Receptor, inhibitors, activators


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