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Giredestrant

Cat. No. M10923
Giredestrant Structure
Synonym:

GDC-9545; RG6171

Size Price Availability Quantity
5mg USD 340  USD340 In stock
10mg USD 540  USD540 In stock
25mg USD 950  USD950 In stock
50mg USD 1500  USD1500 In stock
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Quality Control & Documentation
Biological Activity

Giredestrant (GDC-9545) is an orally active, selective estrogen receptor degrader (SERD) with best-in-class potential to compete with estradiol in the ER ligand binding domain and induce conformational changes.Giredestrant has antitumor activity.



Chemical Information
Molecular Weight 522.55
Formula C27H31F5N4O
CAS Number 1953133-47-5
Solubility (25°C) DMSO ≥ 40 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] Christoph Thomssen, et al. Geburtshilfe Frauenheilkd. Update Breast Cancer 2021 Part 4 - Prevention and Early Stages

[2] Ya-Chi Chen, et al. Expert Opin Investig Drugs. Latest generation estrogen receptor degraders for the treatment of hormone receptor-positive breast cancer

[3] Pengcheng Shao. J Med Chem. A New Era in ER+ Breast Cancer: Best-in-Class Oral Selective Estrogen Receptor Degrader (SERD) Designed as an Endocrine Backbone Treatment

[4] Jun Liang, et al. J Med Chem. GDC-9545 (Giredestrant): A Potent and Orally Bioavailable Selective Estrogen Receptor Antagonist and Degrader with an Exceptional Preclinical Profile for ER+ Breast Cancer

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

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Keywords: Giredestrant, GDC-9545; RG6171 supplier, Estrogen Receptor, inhibitors, activators


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