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Elacestrant dihydrochloride

Cat. No. M14629
Elacestrant dihydrochloride Structure
Synonym:

RAD1901 dihydrochloride

Size Price Availability Quantity
5mg USD 300  USD300 In stock
10mg USD 480  USD480 In stock
50mg USD 1500  USD1500 In stock
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Quality Control & Documentation
Biological Activity

Elacestrant dihydrochloride (RAD1901 dihydrochloride) is an orally available selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively.

Chemical Information
Molecular Weight 531.56
CAS Number 1349723-93-8
Solubility (25°C) DMSO 90 mg/mL
Water 50 mg/mL
Storage 2-8°C, dry, sealed
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] Aditya Bardia, et al. Phase I Study of Elacestrant (RAD1901), a Novel Selective Estrogen Receptor Degrader, in ER-Positive, HER2-Negative Advanced Breast Cancer

[2] Agnes Jager, et al. A phase 1b study evaluating the effect of elacestrant treatment on estrogen receptor availability and estradiol binding to the estrogen receptor in metastatic breast cancer lesions using 18 F-FES PET/CT imaging

[3] Hitisha K Patel, et al. Elacestrant (RAD1901) exhibits anti-tumor activity in multiple ER+ breast cancer models resistant to CDK4/6 inhibitors

[4] Aditya Bardia, et al. EMERALD: Phase III trial of elacestrant (RAD1901) vs endocrine therapy for previously treated ER+ advanced breast cancer

[5] Teeru Bihani, et al. Elacestrant (RAD1901), a Selective Estrogen Receptor Degrader (SERD), Has Antitumor Activity in Multiple ER + Breast Cancer Patient-derived Xenograft Models

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Keywords: Elacestrant dihydrochloride, RAD1901 dihydrochloride supplier, Estrogen Receptor, inhibitors, activators


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