GDC-0927 (Synonyms: SRN-927)

Name: GDC-0927
Brand: MedChemExpress
SKU: HY-111484
Rating: 5.0 (3 reviews)

Cat. No.: HY-111484 Purity: 99.98%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

GDC-0927 (SRN-927) is a potent, non-steroidal, orally bioavailable, selective estrogen receptor antagonist.

For research use only. We do not sell to patients.

GDC-0927 Chemical Structure

CAS No. : 1642297-01-5

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 660	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 660	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 240	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 600	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 900	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 1600	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 2500	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 3800	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of GDC-0927:

GDC-0927 Racemate Get quote
(R)-GDC-0927 Get quote

3 Publications Citing Use of MCE GDC-0927

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View All Estrogen Receptor/ERR Isoform Specific Products:

View All Isoforms

Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

Biological Activity
Purity & Documentation
References
Customer Review

Description

GDC-0927 (SRN-927) is a potent, non-steroidal, orally bioavailable, selective estrogen receptor antagonist^[1].

IC₅₀ & Target

Estrogen receptor^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
MCF7	IC₅₀	0.03 nM Compound: 5; GDC-0927	Induction of ERalpha degradation in human MCF7 cells after 4 hrs by FITC/Hoechst staining based immunofluorescence imaging analysis Induction of ERalpha degradation in human MCF7 cells after 4 hrs by FITC/Hoechst staining based immunofluorescence imaging analysis	[PMID: 32551022]
MCF7	IC₅₀	0.03 nM Compound: 3; GDC-0927	Induction of ERalpha degradation in human MCF7 cells after 4 hrs by FITC/Hoechst 33342 staining based immunofluorescence imaging analysis Induction of ERalpha degradation in human MCF7 cells after 4 hrs by FITC/Hoechst 33342 staining based immunofluorescence imaging analysis	[PMID: 31311734]
MCF7	IC₅₀	0.03 nM Compound: GDC-0927; 4	Induction of ERalpha degradation in human MCF7 cells after 4 hrs by Alexafluor-488 conjugate anti-mouse IgG antibody/Hoechst 33342 staining based immunofluorescence imaging analysis Induction of ERalpha degradation in human MCF7 cells after 4 hrs by Alexafluor-488 conjugate anti-mouse IgG antibody/Hoechst 33342 staining based immunofluorescence imaging analysis	[PMID: 30732944]
MCF7	IC₅₀	0.1 nM Compound: 17ha; GDC-0927; SRN-927	Antiproliferative activity against human MCF7 cells after 5 days by CellTiter-Glo assay Antiproliferative activity against human MCF7 cells after 5 days by CellTiter-Glo assay	[PMID: 30655946]
MCF7	IC₅₀	0.1 nM Compound: 17ha; GDC-0927; SRN-927	Induction of ERalpha degradation in human MCF7 cells assessed as decrease in ERalpha protein level after 4 hrs by InCell Western assay Induction of ERalpha degradation in human MCF7 cells assessed as decrease in ERalpha protein level after 4 hrs by InCell Western assay	[PMID: 30655946]
MCF7	IC₅₀	0.2 nM Compound: GDC-0927; 4	Antiproliferative activity against human MCF7 cells after 3 days by CellTiter-Glo luminescent cell viability assay Antiproliferative activity against human MCF7 cells after 3 days by CellTiter-Glo luminescent cell viability assay	[PMID: 30732944]
MCF7	IC₅₀	0.3 nM Compound: 5; GDC-0927	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by Celltiter-Glo assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by Celltiter-Glo assay	[PMID: 32551022]
MCF7	EC₅₀	0.3 nM Compound: 3; GDC-0927	Antiproliferative activity against human MCF7 cells after 72 hrs by Celltiter-Glo assay Antiproliferative activity against human MCF7 cells after 72 hrs by Celltiter-Glo assay	[PMID: 31311734]
MCF7	EC₅₀	0.3 nM Compound: 11; GDC-0927	Antiproliferative activity against human MCF-7 cells incubated for 72 hrs by Cell-titer Glo assay Antiproliferative activity against human MCF-7 cells incubated for 72 hrs by Cell-titer Glo assay	[PMID: 34251202]

In Vivo

GDC-0927 is a novel, potent, non-steroidal, orally bioavailable, selective ER antagonist/ER degrader (SERD) that induces tumor regression in estrogen receptor (ER)+breast cancer (BC) patient-derived xenograft models^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

461.52

Formula

C₂₈H₂₈FNO₄

CAS No.

1642297-01-5

Appearance

Solid

Color

Light yellow to yellow

SMILES

OC1=CC=C2C(C(C)=C(C3=CC=CC(O)=C3)[C@H](C4=CC=C(OCCN5CC(CF)C5)C=C4)O2)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 83.33 mg/mL (180.56 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1668 mL	10.8338 mL	21.6675 mL
5 mM	0.4334 mL	2.1668 mL	4.3335 mL
10 mM	0.2167 mL	1.0834 mL	2.1668 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.51 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.51 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (4.51 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.98%

Select Batch:

Data Sheet (272 KB) SDS (393 KB)

COA (247 KB) HNMR (232 KB) LCMS (138 KB)

Handling Instructions (2659 KB)

References

[1]. MN Dickler, et al. Abstract PD5-10: A first-in-human phase I study to evaluate the oral selective estrogen receptor degrader (SERD), GDC-0927, in postmenopausal women with estrogen receptor positive (ER+) HER2-negative metastatic breast cancer (BC). AACR; Cancer Res 2018;78(4 Suppl):Abstract nr PD5-10.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.1668 mL	10.8338 mL	21.6675 mL	54.1688 mL
	5 mM	0.4334 mL	2.1668 mL	4.3335 mL	10.8338 mL
	10 mM	0.2167 mL	1.0834 mL	2.1668 mL	5.4169 mL
	15 mM	0.1445 mL	0.7223 mL	1.4445 mL	3.6113 mL
	20 mM	0.1083 mL	0.5417 mL	1.0834 mL	2.7084 mL
	25 mM	0.0867 mL	0.4334 mL	0.8667 mL	2.1668 mL
	30 mM	0.0722 mL	0.3611 mL	0.7223 mL	1.8056 mL
	40 mM	0.0542 mL	0.2708 mL	0.5417 mL	1.3542 mL
	50 mM	0.0433 mL	0.2167 mL	0.4334 mL	1.0834 mL
	60 mM	0.0361 mL	0.1806 mL	0.3611 mL	0.9028 mL
	80 mM	0.0271 mL	0.1354 mL	0.2708 mL	0.6771 mL
	100 mM	0.0217 mL	0.1083 mL	0.2167 mL	0.5417 mL

GDC-0927 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GDC-09271642297-01-5SRN-927GDC0927GDC 0927SRN927SRN 927Estrogen Receptor/ERRInhibitorinhibitorinhibit

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GDC-0927 (Synonyms: SRN-927)

Customer Review

Other Forms of GDC-0927:

GDC-0927 Related Antibodies

3 Publications Citing Use of MCE GDC-0927

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Estrogen Receptor/ERR Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

GDC-0927 Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

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