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> Palbociclib (isethionate) [827022-33-3]

Palbociclib (isethionate) [827022-33-3]

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Referencia HY-A0065-50mg

embalaje : 50mg

Marca : MedChemExpress


Descripciòn

Palbociclib (PD 0332991) isethionate is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib isethionate has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma[1][3][4].

IC50 & Target[1]

Cdk4/cyclin D3

9 nM (IC50)

Cdk4/cyclin D1

11 nM (IC50)

Cdk6/cyclin D2

16 nM (IC50)

DYRK1A

2000 nM (IC50)

MAPK

8000 nM (IC50)

In Vitro

Palbociclib dihydrochloride (0-1 μM, 24 h) inhibits Rb Phosphorylation at Ser795 in MDA-MB-435 cells with an IC50 value of 0.063 μM, and obtains similar effects on both Ser780 and Ser795 phosphorylation in the Colo-205 colon carcinoma[1].
Palbociclib dihydrochloride (0-10 μM, 24 h) arrests MDA-MB-453 cells exclusively in G1 phase[1].
Palbociclib dihydrochloride (500 nM, 7 days) increases expression of homologous genes (H2d1, H2k1, and B2m) in MDA-MB-453 and MDA-MB-361 cells[2].
Palbociclib dihydrochloride (0-1 μM, 6 days) inhibits growth of several luminal ER-positive as well as HER2-amplified breast cancer cell lines, with IC50 values ranging from 4 nM to 1 μM[3].
Palbociclib dihydrochloride (0-1 μM, 3 days) inhibits the proliferation of human liver cancer cell lines with IC50 values ranging from 0.01 μM to 3.49 μM, and induces a reversible cell cycle arrest[4].

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

Palbociclib isethionate Related Antibodies

Cell Cycle Analysis[1]

Cell Line: MDA-MB-453 cells
Concentration: 0-1 μM
Incubation Time: 24 h
Result: Arrested MDA-MB-453 cells in G1.

Cell Proliferation Assay[3]

Cell Line: ER-positive as well as HER2-amplified breast cancer cell lines (MDA-MB-175, ZR-75-30, CAMA-1, etc.)
Concentration: 0-10 μM
Incubation Time: 6 days
Result: Inhibited growth of luminal ER-positive as well as HER2-amplified breast cancer cell lines.
In Vivo

Palbociclib isethionate (oral adminstration, 75 or 150 mg/kg, daily for 14 days) produces rapid tumor regressions and delays tumor growth[1].
Palbociclib isethionate (oral adminstration, 90 mg/kg, daily for 12 days) reduces Treg numbers and the Treg:CD8 ratio in the spleen and lymph nodes in tumor-free mice, demonstrating the tumor-independent effects[2].
Palbociclib isethionate (oral administration, 100 mg/kg, daily for 1 week) has potent antitumour effects in genetically engineered mosaic mouse model of liver cancer[4].

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

Animal Model: Mice bearing Colo-205 colon carcinoma xenografts (p16 deleted)[1]
Dosage: 75, 150 mg/kg, daily for 14 days
Administration: Oral adminstration
Result: Produced rapid tumor regressions and a corresponding tumor growth delay of ~50 days.
Animal Model: Tumor-free female FVB mice[2]
Dosage: 90 mg/kg (diluted in 50 nM sodium D-lactate), daily for 12 days
Administration: Oral adminstration
Result: Reduced total thymic mass and immature CD4+ and CD8+ double-positive thymocytes, and increased the fractions of CD4+ and CD8+ single-positive thymocytes.
Animal Model: Genetically engineered mosaic mouse model of liver cancer (Myc;p53-sgRNA)[4]
Dosage: 100 mg/kg, daily for 1 week.
Administration: Oral adminstration
Result: Decreased the luminescence signal in liver and delayed tumour growth.
Peso molecular

573.66

Fòrmula

C26H35N7O6S
No. CAS
Appearance

Solid

Color

Light yellow to yellow

SMILES

CC(C1=C(N2C3CCCC3)N=C(NC4=NC=C(N5CCNCC5)C=C4)N=C1)=C(C(C)=O)C2=O.OCCS(O)(=O)=O
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

4°C, sealed storage, away from moisture

*In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)

Solvente y solubilidad
In Vitro: 

H2O : 50 mg/mL (87.16 mM; Need ultrasonic)

DMSO : 10 mg/mL (17.43 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 1.7432 mL 8.7160 mL 17.4319 mL
5 mM 0.3486 mL 1.7432 mL 3.4864 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, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 1 mg/mL (1.74 mM); Clear solution

    This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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.
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
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
Pureza y Documentación
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