2. Vitamin D Related/Nuclear Receptor
  3. Estrogen Receptor/ERR
  4. GNE-149

GNE-149 is an orally bioavailable full antagonist of estrogen receptor α (ERα; IC50=0.053 nM). GNE-149 is a selective estrogen receptor degrader (SERD). GNE-149 can be used for the research of breast cancer.

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

GNE-149 Chemical Structure

GNE-149 Chemical Structure

CAS No. : 1953132-75-6

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Based on 1 publication(s) in Google Scholar

GNE-149 Related Antibodies

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Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

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Description

GNE-149 is an orally bioavailable full antagonist of estrogen receptor α (ERα; IC50=0.053 nM). GNE-149 is a selective estrogen receptor degrader (SERD). GNE-149 can be used for the research of breast cancer[1].

IC50 & Target[1]

ERα

0.053 nM (IC50)

In Vitro

GNE-149 exhibits antiproliferative activity in MCF7 and T47D cells with IC50s of 0.66 and 0.69 nM, respectively[1].
GNE-149 exhibits ERα Degradation in MCF7 and T47D cells with IC50s of 0.053 and 0.031 nM, respectively[1].

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

GNE-149 Related Antibodies
In Vivo

GNE-149 (0.3-30 mg/kg) exhibits in vivo efficacy in an MCF7 xenograft mouse model harboring either wild-type (WT) ERα or overexpressed Y537S mutant[1].
GNE-149 has favorable pharmacokinetic profile, including total clearance (CL; 19, 8, and 13 mL/min/kg for Rat, Dog, and Cyno) and oral bioavailability (F; 31%, 49%, and 28% for Rat, Dog, and Cyno)[1].

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

Animal Model: Female Crl:NU Foxn1 nu mice (at 7 weeks of age) bearing wild-type (WT) ERαor overexpressed Y537S mutant MCF7 tumor[1]
Dosage: 0.3, 1, 3, 10, and 30 mg/kg
Administration: Orally q.d. for 21 days
Result: Exhibited dose-dependent efficacy in the MCF7 WT and Y537S mutant xenograft model, with tumor regression observed at all doses above 0.3 mg/kg in Y537S mutant xenograft model.
Molecular Weight

503.57

Formula

C28H33F4N3O
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

CC(C)(F)CN1[C@@](C2=C(C=C(C=C2F)OC3CN(C3)CCCF)F)([H])C4=C(C[C@H]1C)C5=CC=CC=C5N4
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 : 50 mg/mL (99.29 mM; ultrasonic and warming and heat to 60°C; 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 1.9858 mL 9.9291 mL 19.8582 mL
5 mM 0.3972 mL 1.9858 mL 3.9716 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.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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

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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 1.9858 mL 9.9291 mL 19.8582 mL 49.6455 mL
5 mM 0.3972 mL 1.9858 mL 3.9716 mL 9.9291 mL
10 mM 0.1986 mL 0.9929 mL 1.9858 mL 4.9646 mL
15 mM 0.1324 mL 0.6619 mL 1.3239 mL 3.3097 mL
20 mM 0.0993 mL 0.4965 mL 0.9929 mL 2.4823 mL
25 mM 0.0794 mL 0.3972 mL 0.7943 mL 1.9858 mL
30 mM 0.0662 mL 0.3310 mL 0.6619 mL 1.6549 mL
40 mM 0.0496 mL 0.2482 mL 0.4965 mL 1.2411 mL
50 mM 0.0397 mL 0.1986 mL 0.3972 mL 0.9929 mL
60 mM 0.0331 mL 0.1655 mL 0.3310 mL 0.8274 mL
80 mM 0.0248 mL 0.1241 mL 0.2482 mL 0.6206 mL
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GNE-149 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-1491953132-75-6GNE149GNE 149Estrogen Receptor/ERRMCF7T47DERαSERDantagonistbreast cancerpure antiestrogenestrogen receptorERα antagonistselective estrogen receptor degraderInhibitorinhibitorinhibit

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