Giredestrant | CAS#1953133-47-5 | SERD

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

MedKoo CAT#: 206995

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

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.

Chemical Structure

Giredestrant

CAS# 1953133-47-5 (free base)

Instruction

Theoretical Analysis

MedKoo Cat#: 206995
Name: Giredestrant
CAS#: 1953133-47-5 (free base)
Chemical Formula: C27H31F5N4O
Exact Mass: 522.24
Molecular Weight: 522.564
Elemental Analysis: C, 62.06; H, 5.98; F, 18.18; N, 10.72; O, 3.06

Price and Availability

Size	Price	Availability
10mg	USD 550	2 Weeks
25mg	USD 1150	2 Weeks
50mg	USD 1850	2 Weeks
100mg	USD 2950	2 Weeks
200mg	USD 4350	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

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;

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:

Instruction:

View handling instruction

Biological target:
In vitro activity:
In vivo activity:

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.

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

Formulation protocol:
In vitro protocol:
In vivo protocol:

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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.

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