WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 333075
CAS#: 2407529-33-1 (tartrate)
Description: Giredestrant, also known as GDC-9545 and RG6171, is a SERD. GDC-9545 is an orally available selective estrogen receptor degrader/downregulator (SERD), with potential antineoplastic activity. Upon oral administration, SERD GDC-9545 specifically targets and binds to the estrogen receptor (ER) and induces a conformational change that promotes ER degradation.
MedKoo Cat#: 333075
Name: Giredestrant tartrate
CAS#: 2407529-33-1 (tartrate)
Chemical Formula: C31H37F5N4O7
Exact Mass:
Molecular Weight: 672.65
Elemental Analysis: C, 55.35; H, 5.54; F, 14.12; N, 8.33; O, 16.65
Related CAS #: 1953133-47-5 (free base) 2407529-33-1 (tartrate) 2407529-48-8 (fumarate)
Synonym: GDC-9545; GDC9545; GDC 9545; RG6171; RG-6171; RG 6171; Giredestrant tartrate;
IUPAC/Chemical Name: 3-((1R,3R)-1-(2,6-difluoro-4-((1-(3-fluoropropyl)azetidin-3-yl)amino)phenyl)-3-methyl-1,3,4,9-tetrahydro-2H-pyrido[3,4-b]indol-2-yl)-2,2-difluoropropan-1-ol tartrate
InChi Key: QZOTWXMHTSEIJY-TWIHJBRTSA-N
InChi Code: InChI=1S/C27H31F5N4O.C4H6O6/c1-16-9-20-19-5-2-3-6-23(19)34-25(20)26(36(16)14-27(31,32)15-37)24-21(29)10-17(11-22(24)30)33-18-12-35(13-18)8-4-7-28;5-1(3(7)8)2(6)4(9)10/h2-3,5-6,10-11,16,18,26,33-34,37H,4,7-9,12-15H2,1H3;1-2,5-6H,(H,7,8)(H,9,10)/t16-,26-;1-,2-/m10/s1
SMILES Code: OCC(F)(F)CN([C@@H]1C2=C(F)C=C(NC3CN(CCCF)C3)C=C2F)[C@H](C)CC4=C1NC5=C4C=CC=C5.O[C@@H]([C@@H](C(O)=O)O)C(O)=O
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: To be determined
Shelf Life: >2 years if stored properly
Drug Formulation: To be determined
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 672.65 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
1: Chen YC, Yu J, Metcalfe C, De Bruyn T, Gelzleichter T, Malhi V, Perez-Moreno PD, Wang X. Latest generation estrogen receptor degraders for the treatment of hormone receptor-positive breast cancer. Expert Opin Investig Drugs. 2021 Oct 25:1-15. doi: 10.1080/13543784.2021.1983542. Epub ahead of print. PMID: 34694932.
2: Shao P. A New Era in ER+ Breast Cancer: Best-in-Class Oral Selective Estrogen Receptor Degrader (SERD) Designed as an Endocrine Backbone Treatment. J Med Chem. 2021 Aug 26;64(16):11837-11840. doi: 10.1021/acs.jmedchem.1c01268. Epub 2021 Aug 2. PMID: 34339201.
3: Liang J, Zbieg JR, Blake RA, Chang JH, Daly S, DiPasquale AG, Friedman LS, Gelzleichter T, Gill M, Giltnane JM, Goodacre S, Guan J, Hartman SJ, Ingalla ER, Kategaya L, Kiefer JR, Kleinheinz T, Labadie SS, Lai T, Li J, Liao J, Liu Z, Mody V, McLean N, Metcalfe C, Nannini MA, Oeh J, O'Rourke MG, Ortwine DF, Ran Y, Ray NC, Roussel F, Sambrone A, Sampath D, Schutt LK, Vinogradova M, Wai J, Wang T, Wertz IE, White JR, Yeap SK, Young A, Zhang B, Zheng X, Zhou W, Zhong Y, Wang X. GDC-9545 (Giredestrant): A Potent and Orally Bioavailable Selective Estrogen Receptor Antagonist and Degrader with an Exceptional Preclinical Profile for ER+ Breast Cancer. J Med Chem. 2021 Aug 26;64(16):11841-11856. doi: 10.1021/acs.jmedchem.1c00847. Epub 2021 Jul 12. PMID: 34251202.
4: Novel Agents Show Promise Against Acquired Endocrine Resistance in ER+ Advanced Breast Cancer. Oncologist. 2021 Jul;26 Suppl 3(Suppl 3):S15-S16. doi: 10.1002/onco.13874. Epub 2021 Jun 26. PMID: 34173302; PMCID: PMC8262303.
