2. Vitamin D Related/Nuclear Receptor
  3. Estrogen Receptor/ERR
  4. Palazestrant

Palazestrant  (Synonyms: OP-1250)

Cat. No.: HY-148789 Purity: 98.96%
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Palazestrant is an antiestrogen and antineoplastic agent. Palazestrant can completely inhibit the activity of 17b-estradiol (E2) with IC50 value of 6.4 nM, and inhibit the proliferation of MCF7 and CAMA-1 cells with IC50 value of 1.4-1.6 nM. Palazestrant can inhibit ER+/HER2+ cancer.

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

Palazestrant Chemical Structure

Palazestrant Chemical Structure

CAS No. : 2092925-89-6

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

Palazestrant Related Antibodies

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View All Estrogen Receptor/ERR Isoform Specific Products:

View All Isoforms
Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

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Description

Palazestrant is an antiestrogen and antineoplastic agent. Palazestrant can completely inhibit the activity of 17b-estradiol (E2) with IC50 value of 6.4 nM, and inhibit the proliferation of MCF7 and CAMA-1 cells with IC50 value of 1.4-1.6 nM. Palazestrant can inhibit ER+/HER2+ cancer[1][2][3].

IC50 & Target

17b-estradiol (E2)

6.4 nM (IC50)

ER

 

In Vitro

Palazestrant (0-300 nM, 24 h) can completely inhibit the activity of 17b-estradiol (E2) with IC50 value of 6.4 nM, and inhibit the proliferation of MCF7 and CAMA-1 cells with IC50 value of 1.4-1.6 nM[3].

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

Palazestrant Related Antibodies
In Vivo

Palazestrant (0-100 mg/kg/day for 3 days. p.o.) alone or in combination with Palbociclib (HY-50767), Ribociclib (HY-15777) or Alpelisib (HY-15244) can effectively inhibit the proliferation and brain metastasis of ER-positive breast cancer[3].

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

449.60

Formula

C28H36FN3O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC(C)(F)CN1[C@H](C2=CC=C(C=C2)OC3CN(C3)CCC)C4=C(C[C@H]1C)C5=CC=CC=C5N4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 22.22 mg/mL (49.42 mM; ultrasonic and adjust pH to 3 with 1M HCl; 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 2.2242 mL 11.1210 mL 22.2420 mL
5 mM 0.4448 mL 2.2242 mL 4.4484 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. 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
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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:

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g

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(per animal)

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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. 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 2.2242 mL 11.1210 mL 22.2420 mL 55.6050 mL
5 mM 0.4448 mL 2.2242 mL 4.4484 mL 11.1210 mL
10 mM 0.2224 mL 1.1121 mL 2.2242 mL 5.5605 mL
15 mM 0.1483 mL 0.7414 mL 1.4828 mL 3.7070 mL
20 mM 0.1112 mL 0.5560 mL 1.1121 mL 2.7802 mL
25 mM 0.0890 mL 0.4448 mL 0.8897 mL 2.2242 mL
30 mM 0.0741 mL 0.3707 mL 0.7414 mL 1.8535 mL
40 mM 0.0556 mL 0.2780 mL 0.5560 mL 1.3901 mL
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Palazestrant 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:

Palazestrant2092925-89-6OP-1250OP1250OP 1250Estrogen Receptor/ERRER-positive Breast Cancer Modelsanti-cancerMCF7 cellCAMA-1 cellInhibitorinhibitorinhibit

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