MedKoo Cat#: 206995 | Name: Giredestrant
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

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.

Chemical Structure

Giredestrant
Giredestrant
CAS#1953133-47-5 (free base)

Theoretical Analysis

MedKoo Cat#: 206995

Name: Giredestrant

CAS#: 1953133-47-5 (free base)

Chemical Formula: C27H31F5N4O

Exact Mass: 522.2418

Molecular Weight: 522.56

Elemental Analysis: C, 62.06; H, 5.98; F, 18.18; N, 10.72; O, 3.06

Price and Availability

Size Price Availability Quantity
10mg USD 450.00 2 Weeks
25mg USD 950.00 2 Weeks
50mg USD 1,450.00 2 Weeks
100mg USD 2,450.00 2 Weeks
200mg USD 4,050.00 2 Weeks
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Related CAS #
Synonym
GDC-9545; GDC9545; GDC 9545; RG6171; RG-6171; RG 6171; Giredestrant;
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
InChi Key
GQCXHIKRWBIQMD-AKJBCIBTSA-N
InChi Code
InChI=1S/C27H31F5N4O/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/h2-3,5-6,10-11,16,18,26,33-34,37H,4,7-9,12-15H2,1H3/t16-,26-/m1/s1
SMILES Code
C[C@@H]1CC(C2=C(N3)C=CC=C2)=C3[C@@H](C4=C(C=C(C=C4F)NC5CN(C5)CCCF)F)N1CC(CO)(F)F
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
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
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
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 522.56 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.

Recalculate based on batch purity %
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.