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Palbociclib (PD0332991) Isethionate

CDK4/6 inhibitor,highly selective CAS# 827022-33-3

Palbociclib (PD0332991) Isethionate

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Chemical structure

Palbociclib (PD0332991) Isethionate

3D structure

Chemical Properties of Palbociclib (PD0332991) Isethionate

Cas No. 827022-33-3 SDF Download SDF
PubChem ID 11478676 Appearance Powder
Formula C26H35N7O6S M.Wt 573.66
Type of Compound N/A Storage Desiccate at -20°C
Synonyms PD 0332991 isethionate
Solubility H2O : 50 mg/mL (87.16 mM; Need ultrasonic)
DMSO : 10 mg/mL (17.43 mM; Need ultrasonic)
Chemical Name 6-acetyl-8-cyclopentyl-5-methyl-2-[(5-piperazin-1-ylpyridin-2-yl)amino]pyrido[2,3-d]pyrimidin-7-one;2-hydroxyethanesulfonic acid
SMILES CC1=C(C(=O)N(C2=NC(=NC=C12)NC3=NC=C(C=C3)N4CCNCC4)C5CCCC5)C(=O)C.C(CS(=O)(=O)O)O
Standard InChIKey LYYVFHRFIJKPOV-UHFFFAOYSA-N
Standard InChI InChI=1S/C24H29N7O2.C2H6O4S/c1-15-19-14-27-24(28-20-8-7-18(13-26-20)30-11-9-25-10-12-30)29-22(19)31(17-5-3-4-6-17)23(33)21(15)16(2)32;3-1-2-7(4,5)6/h7-8,13-14,17,25H,3-6,9-12H2,1-2H3,(H,26,27,28,29);3H,1-2H2,(H,4,5,6)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Palbociclib (PD0332991) Isethionate

DescriptionPalbociclib (PD0332991) Isethionate is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM.
TargetsCDK4CDK6    
IC5011 nM16 nM    

Protocol

Cell Assay [3]
Cells are seeded in duplicate at 5,000 to 10,000 cells per well in 24-well plates. The day after plating, different concentrations of Palbociclib are added. Control wells without drug are also seeded. At the end of incubation, cells are trypsinizated and placed in Isotone solution and counted immediately using a Coulter Z2 particle counter.

Animal Administration [1]
Mice (18-22 g) are randomized and then implanted s.c. with tumor fragments (appr 30 mg) into the region of the right axilla. Treatment is initiated when tumors reach 100 to 150 mg. Palbociclib is given according to the schedule and dose indicated in the table and figure legends by gavage as a solution in sodium lactate buffer (50 mM, pH 4.0) based on mean group body weight. In all experiments, there are 12 mice in the control group and 8 mice each in the treated groups. Additional details for each experiment are given in the table legends.

References:
[1]. Fry DW, et al. Specific inhibition of cyclin-dependent kinase 4/6 by PD 0332991 and associated antitumor activity in human tumor xenografts. Mol Cancer Ther, 2004, 3(11), 1427-1438. [2]. Baughn LB, et al. A novel orally active small molecule potently induces G1 arrest in primary myeloma cells and prevents tumor growth by specific inhibition of cyclin-dependent kinase 4/6. Cancer Res. 2006 Aug 1;66(15):7661-7. [3]. Finn RS, et al. PD 0332991, a selective cyclin D kinase 4/6 inhibitor, preferentially inhibits proliferation of luminal estrogen receptor-positive human breast cancer cell lines in vitro. Breast Cancer Res. 2009;11(5):R77.

Palbociclib (PD0332991) Isethionate Dilution Calculator

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Palbociclib (PD0332991) Isethionate Molarity Calculator

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Preparing Stock Solutions of Palbociclib (PD0332991) Isethionate

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.7432 mL 8.716 mL 17.4319 mL 34.8639 mL 43.5798 mL
5 mM 0.3486 mL 1.7432 mL 3.4864 mL 6.9728 mL 8.716 mL
10 mM 0.1743 mL 0.8716 mL 1.7432 mL 3.4864 mL 4.358 mL
50 mM 0.0349 mL 0.1743 mL 0.3486 mL 0.6973 mL 0.8716 mL
100 mM 0.0174 mL 0.0872 mL 0.1743 mL 0.3486 mL 0.4358 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Palbociclib (PD0332991) Isethionate

IC50: Palbociclib is an orally active, potent and highly selective inhibitor of CDK4 and CDK6, with IC50 values for CDK4/cyclinD1, CDK4/cyclinD3 and CDK6/cyclinD2 of 11, 9 and 15 nmol/l, respectively.

Cyclin-dependent kinases (CDKs) are a family of protein kinases first discovered for their role in regulating the cell cycle. They are also involved in regulating transcription, mRNA processing, and the differentiation of nerve cells. A cyclin-dependent kinase inhibitor (CKI) is a protein that interacts with a cyclin-CDK complex to block kinase activity, usually during G1 or in response to signals from the environment or from damaged DNA. Palbociclib is an experimental drug for the treatment of breast cancer being developed by Pfizer. It is a selective inhibitor of the cyclin-dependent kinases CDK4 and CDK6.

In vitro: Half-maximal inhibitory concentrations (IC50) of PD-0332991 were determined with cell line proliferation assays. Resutls showed that IC50 values for PD-0332991 ranged from 25.0 nM to 700 nM, and the agent demonstrated G0/G1 cell-cycle arrest, induction of late apoptosis, and blockade of RB phosphorylation. Through genotype and expression data p16, p15 and E2F1 were identified as having significant association between loss and sensitivity to PD-0332991: p16 (p=0.021), p15 (p=0.047), and E2F1 (p=0.041) [1].

In vivo: Oral administration of PD 0332991 to mice bearing the Colo-205 human colon carcinoma produces marked tumor regression. Therapeutic doses of PD 0332991 cause elimination of phospho-Rb and the proliferative marker Ki-67 in tumor tissue and down-regulation of genes under the transcriptional control of E2F. The results indicate that inhibition of Cdk4/6 alone is sufficient to cause tumor regression and a net reduction in tumor burden in some tumors [2].

Clinical trial: In a phase 2 trial reported at the April 2014 annual meeting of the American Association for Cancer Research, the addition of palbociclib to letrozole was shown to significantly slow the progression of advanced cancer (median progression-free survival increased from 10.2 months to 20.2 months), but was not shown to have a statistically significant effect on increasing patients' overall survival times. A potentially confirmatory phase 3 trial, PALOMA-2, has fully enrolled patients. The drug received an accelerated approval from the Food and Drug Administration on February 3, 2015, as a treatment (in combination with letrozole) for patients with estrogen receptor-positive advanced breast cancer (http://en.wikipedia.org/wiki/Palbociclib).

References:
[1] Logan JE, Mostofizadeh N, Desai AJ, VON Euw E, Conklin D, Konkankit V, Hamidi H, Eckardt M, Anderson L, Chen HW, Ginther C, Taschereau E, Bui PH, Christensen JG, Belldegrun AS, Slamon DJ, Kabbinavar FF.  PD-0332991, a potent and selective inhibitor of cyclin-dependent kinase 4/6, demonstrates inhibition of proliferation in renal cell carcinoma at nanomolar concentrations and molecular markers predict for sensitivity. Anticancer Res. 2013;33(8):2997-3004.
[2] Fry DW, Harvey PJ, Keller PR, Elliott WL, Meade M, Trachet E, Albassam M, Zheng X, Leopold WR, Pryer NK, Toogood PL.  Specific inhibition of cyclin-dependent kinase 4/6 by PD 0332991 and associated antitumor activity in human tumor xenografts. Mol Cancer Ther. 2004;3(11):1427-38.

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Description

Palbociclib isethionate is a highly selective inhibitor of CDK4/6 with IC50s of 11 nM/16 nM, respectively.

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