PD 0332991 (Palbociclib) HClCDK4/6 inhibitor,highly selective CAS# 827022-32-2 |
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Quality Control & MSDS
3D structure
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| Cas No. | 827022-32-2 | SDF | Download SDF |
| PubChem ID | 11431660 | Appearance | Powder |
| Formula | C24H30ClN7O2 | M.Wt | 483.99 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | PD 0332991 hydrochloride | ||
| Solubility | DMSO : 5.4 mg/mL (11.16 mM; Need ultrasonic) H2O : 4.9 mg/mL (10.12 mM; Need ultrasonic and warming) | ||
| Chemical Name | 6-acetyl-8-cyclopentyl-5-methyl-2-[(5-piperazin-1-ylpyridin-2-yl)amino]pyrido[2,3-d]pyrimidin-7-one;hydrochloride | ||
| SMILES | CC1=C(C(=O)N(C2=NC(=NC=C12)NC3=NC=C(C=C3)N4CCNCC4)C5CCCC5)C(=O)C.Cl | ||
| Standard InChIKey | STEQOHNDWONVIF-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C24H29N7O2.ClH/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;/h7-8,13-14,17,25H,3-6,9-12H2,1-2H3,(H,26,27,28,29);1H | ||
| 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. |
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| 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. |
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| 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. | ||
| Description | Palbociclib (PD-0332991) HCl is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM. | |||||
| Targets | CDK4/cyclin D1 | CDK6/cyclin D2 | ||||
| IC50 | 11 nM | 16 nM | ||||
| Cell experiment: [1] | |
| Cell lines | MDA-MB-453 cells |
| Preparation method | The solubility of this compound in DMSO is <10 mm. general tips for obtaining a higher concentration: please warm the tube at 37 °c 10 minutes and> |
| Reacting condition | 80 nM, 24 hours |
| Applications | MDA-MB-453 breast carcinoma cells exposed to varying concentrations of PD 0332991 for 24 hours showed a significant increase in the percentage of cells in G1 in the presence of as little as 0.04 μmol/L PD 0332991 with a concomitant decline in other phases of the cell cycle. Maximum effects were attained at 0.08 μmol/L and an exclusive G1 arrest was maintained even at concentrations as high as 10 μmol/L, consistent with the complete absence of any other effects on the cell cycle. |
| Animal experiment: [1] | |
| Animal models | Mice bearing Colo-205 colon carcinoma xenografts |
| Dosage form | Oral administration, 150 or 75 mg/kg, daily for 14 days |
| Application | Administration of PD 0332991 produced rapid tumor regressions and a corresponding tumor growth delay of about 50 days with >1 log of tumor cell kill at the highest dose tested. At 37.5 mg/kg, the tumor slowly regressed during treatment. Even at doses as low as 12.5 mg/kg, a 13-day growth delay was obtained indicating a 90% inhibition of tumor growth rate. |
| Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
| References: [1] Fry D W, Harvey P J, Keller P R, et al. Specific inhibition of cyclin-dependent kinase 4/6 by PD 0332991 and associated antitumor activity in human tumor xenografts. Molecular cancer therapeutics, 2004, 3(11): 1427-1438. | |
PD 0332991 (Palbociclib) HCl Dilution Calculator
PD 0332991 (Palbociclib) HCl Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.0662 mL | 10.3308 mL | 20.6616 mL | 41.3232 mL | 51.654 mL |
| 5 mM | 0.4132 mL | 2.0662 mL | 4.1323 mL | 8.2646 mL | 10.3308 mL |
| 10 mM | 0.2066 mL | 1.0331 mL | 2.0662 mL | 4.1323 mL | 5.1654 mL |
| 50 mM | 0.0413 mL | 0.2066 mL | 0.4132 mL | 0.8265 mL | 1.0331 mL |
| 100 mM | 0.0207 mL | 0.1033 mL | 0.2066 mL | 0.4132 mL | 0.5165 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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PD-0332991 is selective and oral inhibitor of cyclin-dependent kinase 4/6 with IC50 values of 11nM and 16nM, respectively for CDK4 and CDK6 [1].
PD-0332991 is a highly specific inhibitor of CDK4/6. It is a potent anti-proliferative agent against Rb-positive tumor cells in vitro, subsequently inducing an exclusive G1 arrest. It has been reported to prevent tumor growth in disseminated human myeloma xenografts and induce G1 arrest in primary bone marrow cells [2].
PD-0332991 is also studied in breast cancer. It causes growth inhibition of ER-positive cell lines and 10/16 HER2-amplified cell lines. 100nM PD-0332991 can inhibit the phosphorylation of Rb in three more sensitive cell lines, resulting in prevention of cell cycle progression [2].
References:
[1] Ivan Diaz-Padilla, Lillian L. Siu and Ignacio Duran. Cyclin-dependent kinase inhibitors as potential targeted anticancer agents. Invest New Drugs. 2009, 27: 586–594.
[2] Richard S Finn, Judy Dering, Dylan Conklin, Ondrej Kalous, David J Cohen, Amrita J Desai, Charles Ginther, Mohammad Atefi, Isan Chen, Camilla Fowst, Gerret Los and Dennis J Slamon. 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 Research. 2009, 11: R77.
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