Palazestrant |
| Catalog No.GC71052 |
Palazestrant est un anti - oestrogène et un médicament anti - tumoral.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2092925-89-6
Sample solution is provided at 25 µL, 10mM.
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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].
Palazestrant (0-100 mg/kg/day for 3 days. p.o.) alone or in combination with Palbociclib , Ribociclib or Alpelisib can effectively inhibit the proliferation and brain metastasis of ER-positive breast cancer[3].
References:
[1]. Harmon CL, et al. Methods of treating estrogen receptor-associated diseases such as ER+/HER2+ cancer using an estrogen receptor antagonist: World Intellectual Property Organization, WO2023283329. 2023-01-12.
[2]. WHO Drug Information-World Health Organization (WHO).
[3]. Parisian AD, et al. Palazestrant (OP-1250), A Complete Estrogen Receptor Antagonist, Inhibits Wild-type and Mutant ER-positive Breast Cancer Models as Monotherapy and in Combination. Mol Cancer Ther. 2024 Mar 4;23(3):285-300.
| Cas No. | 2092925-89-6 | SDF | |
| Formula | C28H36FN3O | M.Wt | 449.6 |
| Solubility | 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) | Storage | -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.2242 mL | 11.121 mL | 22.242 mL |
| 5 mM | 0.4448 mL | 2.2242 mL | 4.4484 mL |
| 10 mM | 0.2224 mL | 1.1121 mL | 2.2242 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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