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[CAS NO. 827022-33-3]  Palbociclibisethionate

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PRODUCTS SPECIFICATIONS [827022-33-3]

Catelog
HY-A0065
Brand
MCE
CAS
827022-33-3

DESCRIPTION [827022-33-3]

Overview

MDLMFCD22666589
Molecular Weight573.66
Molecular FormulaC26H35N7O6S
SMILESCC(C1=C(N2C3CCCC3)N=C(NC4=NC=C(N5CCNCC5)C=C4)N=C1)=C(C(C)=O)C2=O.OCCS(O)(=O)=O

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

99 Publications Citing Use of MCE


Summary

Palbociclib (PD 0332991) isethionate is an orally active selective CDK4 and CDK6 inhibitor with IC 50 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

Cdk4/cyclin D3

9 nM (IC 50 )

Cdk4/cyclin D1

11 nM (IC 50 )

Cdk6/cyclin D2

16 nM (IC 50 )

DYRK1A

2000 nM (IC 50 )

MAPK

8000 nM (IC 50 )


In Vitro

Palbociclib dihydrochloride (0-1 μM, 24 h) inhibits Rb Phosphorylation at Ser 795 in MDA-MB-435 cells with an IC 50 value of 0.063 μM, and obtains similar effects on both Ser 780 and Ser 795 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 IC 50 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 IC 50 values ranging from 0.01 μM to 3.49 μM, and induces a reversible cell cycle arrest [4] .

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

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] .

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.

Clinical Trial

NCT Number Sponsor Condition Start Date Phase
NCT05361655 Pfizer
Metastatic Breast Cancer
September 1, 2021
NCT03285568 Rush University Medical Center
Metastatic Breast Cancer|Advanced Breast Cancer|Estrogen Receptor-positive Breast Cancer|Human Epidermal Growth Factor 2 Negative Carcinoma of Breast
February 3, 2015
NCT04916509 Pfizer
Breast Neoplasms
October 1, 2021

Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

4°C, sealed storage, away from moisture

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


Solvent & Solubility

In Vitro:

H 2 O : 50 mg/mL ( 87.16 mM ; Need ultrasonic)

DMSO : 10 mg/mL ( 17.43 mM ; Need ultrasonic)

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
10 mM 0.1743 mL 0.8716 mL 1.7432 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

* All of the co-solvents are available by MCE.


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