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Elacestrant

Cat. No. M14628
Elacestrant Structure
Synonym:

RAD1901

Size Price Availability Quantity
5mg USD 400  USD400 In stock
10mg USD 560  USD560 In stock
50mg USD 1690  USD1690 In stock
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Quality Control & Documentation
Biological Activity

Elacestrant (RAD1901) 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 458.63
CAS Number 722533-56-4
Solubility (25°C) DMSO 100 mg/mL
Storage 2-8°C, protect from light, 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] Katherine G Sanchez, et al. Elacestrant and the Promise of Oral SERDs

[2] Francois-Clement Bidard, et al. Elacestrant (oral selective estrogen receptor degrader) Versus Standard Endocrine Therapy for Estrogen Receptor-Positive, Human Epidermal Growth Factor Receptor 2-Negative Advanced Breast Cancer: Results From the Randomized Phase III EMERALD Trial

[3] Aditya Bardia, et al. Phase I Study of Elacestrant (RAD1901), a Novel Selective Estrogen Receptor Degrader, in ER-Positive, HER2-Negative Advanced Breast Cancer

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

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

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


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