2. Vitamin D Related/Nuclear Receptor
  3. Estrogen Receptor/ERR
  4. GNE-502

GNE-502 is an orally active and potent degrader for estrogen receptor (ER). GNE-502 can be used for the research of breast cancer.

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

GNE-502 Chemical Structure

GNE-502 Chemical Structure

CAS No. : 1953134-16-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 622 In-stock
Solution
10 mM * 1 mL in DMSO USD 622 In-stock
Solid
5 mg USD 600 In-stock
10 mg USD 960 In-stock
25 mg USD 1800 In-stock
50 mg USD 2900 In-stock
100 mg USD 4500 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of GNE-502:

GNE-502 Related Antibodies

Top Publications Citing Use of Products

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

GNE-502 is an orally active and potent degrader for estrogen receptor (ER). GNE-502 can be used for the research of breast cancer[1].

IC50 & Target

ER[1]
Cellular Effect
Cell Line Type Value Description References
MCF7 IC50
0.5 nM
Compound: GNE-502
Antiproliferation activity against human MCF7 cells assessed as reduction in cell viability measured by CellTiter-Glo luminescent assay assay
Antiproliferation activity against human MCF7 cells assessed as reduction in cell viability measured by CellTiter-Glo luminescent assay assay
[PMID: 34425201]
In Vivo

GNE-502 (10 and 100 mg/kg; p.o.) possesses sufficient oral exposure to be tested in a WT MCF7 tumor xenograft model[1].
GNE-502 shows dose dependent tumor growth inhibition at 10 mg/kg and 30 mg/kg, with tumor stasis at 100 mg/kg[1].

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

Animal Model: Mouse[1]
Dosage: 10 and 100 mg/kg (Pharmacokinetic Analysis)
Administration: p.o.; single dosage
Result: Possessed sufficient oral exposure to be tested in a WT MCF7 tumor xenograft model.
Molecular Weight

471.59

Formula

C25H30FN3O3S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C[C@@H]1CC(C2=CC=CC=C2N3)=C3[C@@H](C4=CC=C(C=C4)OCCN5CC(C5)CF)N1S(=O)(C)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (212.05 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 2.1205 mL 10.6024 mL 21.2049 mL
5 mM 0.4241 mL 2.1205 mL 4.2410 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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

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C2

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V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1205 mL 10.6024 mL 21.2049 mL 53.0122 mL
5 mM 0.4241 mL 2.1205 mL 4.2410 mL 10.6024 mL
10 mM 0.2120 mL 1.0602 mL 2.1205 mL 5.3012 mL
15 mM 0.1414 mL 0.7068 mL 1.4137 mL 3.5341 mL
20 mM 0.1060 mL 0.5301 mL 1.0602 mL 2.6506 mL
25 mM 0.0848 mL 0.4241 mL 0.8482 mL 2.1205 mL
30 mM 0.0707 mL 0.3534 mL 0.7068 mL 1.7671 mL
40 mM 0.0530 mL 0.2651 mL 0.5301 mL 1.3253 mL
50 mM 0.0424 mL 0.2120 mL 0.4241 mL 1.0602 mL
60 mM 0.0353 mL 0.1767 mL 0.3534 mL 0.8835 mL
80 mM 0.0265 mL 0.1325 mL 0.2651 mL 0.6627 mL
100 mM 0.0212 mL 0.1060 mL 0.2120 mL 0.5301 mL
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GNE-502 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:

GNE-5021953134-16-1GNE502GNE 502Estrogen Receptor/ERRorallyactivepotentestrogenreceptorbreastcancerInhibitorinhibitorinhibit

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