Size | Price | |
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100mg | ||
250mg | ||
500mg | ||
Other Sizes |
Targets |
DYRK1A 2000 nM (IC50) MAPK 8000 nM (IC50) Cdk4/cyclin D3 9 nM (IC50) Cdk4/cyclin D1 11 nM (IC50) Cdk6/cyclin D2 16 nM (IC50)
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ln Vitro |
With an IC50 value of 0.063 μM, palbociclib (0-1 μM, 24 h) orotate suppresses the phosphorylation of Ser795 in retinoblastoma in MDA-MB-435 cells. It also has comparable effects on the phosphorylation of Ser780 and Ser795 in colon cancer Colo-205[1]. Only MDA-MB-453 cells in the G1 phase are arrested by palbociclib (0–10 μM, 24 h) orotate[1]. In MDA-MB-453 and MDA-MB-361 cells, palbociclib (500 nM, 7 days) orotate enhances the expression of homologous genes (H2d1, H2k1, and B2m)[2]. The growth of several luminal ER-positive and HER2-amplified breast cancer cell lines is inhibited by palbociclib (0-1 μM, 6 days) orotate, with IC50 values ranging from 0.01 μM to 3.49 μM. Additionally, palbociclib (0-1 μM, 3 days) orotate inhibits the proliferation of human liver cancer cell lines, causing a reversible cell cycle arrest[4].
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ln Vivo |
Palbociclib, when administered orally for 14 days at a dose of 75 or 150 mg/kg, causes tumors to develop more slowly and to rapidly recede[1]. Tumor-free animals treated with palbociclib (oral administration, 90 mg/kg, daily for 12 days) have decreased Treg counts and the Treg:CD8 ratio in the spleen and lymph nodes, indicating tumor-independent effects[2]. Palbociclib, orotate (oral treatment, 100 mg/kg, daily for 1 week) exhibits strong antitumor effects in a mosaic mouse model of genetically altered liver cancer[4].
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Cell Assay |
Cell Proliferation Assay[3]
Cell Types: ER-positive as well as HER2-amplified breast cancer cell lines (MDA-MB-175, ZR-75-30, CAMA-1, etc.) Tested Tested Concentrations: 0-1 μM Incubation Duration: 6 days Experimental Results: Inhibited growth of luminal ER-positive as well as HER2-amplified breast cancer cell lines. Cell Cycle Analysissup>[1] Cell Types: MDA-MB-453 cells Tested Tested Concentrations: 0-1 μM Incubation Duration:: 24 h Experimental Results: Arrested MDA-MB-453 cells in G1. |
Animal Protocol |
Animal/Disease Models: Mice bearing Colo-205 colon carcinoma xenografts (p16 deleted)[1]
Doses: 75, 150 mg/kg Route of Administration: Oral administration; daily for 14 days Experimental Results: Produced rapid tumor regressions and a corresponding tumor growth delay of ~50 days. Animal/Disease Models: Tumor-free female FVB mice[2] Doses: 90 mg/kg Route of Administration: Oral administration; daily for 12 days Experimental Results: decreased total thymic mass and immature CD4+ and CD8+ double-positive thymocytes, and increased the fractions of CD4+ and CD8+ single-positive thymocytes. Animal/Disease Models: Genetically engineered mosaic mouse model of liver cancer (Myc;p53-sgRNA)[4] Doses: 100 mg/kg Route of Administration: Oral administration; daily for 1 week Experimental Results: diminished the luminescence signal in liver and delayed tumor growth. |
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 Nov;3(11):1427-38.
[2]. Goel S, et al. CDK4/6 inhibition triggers anti-tumour immunity. Nature. 2017 Aug 24;548(7668):471-475. [3]. Richard S Finn, 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. [4]. Bollard J, et al. Palbociclib (PD-0332991), a selective CDK4/6 inhibitor, restricts tumour growth in preclinical models of hepatocellular carcinoma. Gut. 2017 Jul;66(7):1286-1296. |
Molecular Formula |
C29H33N9O6
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Molecular Weight |
603.63
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CAS # |
2757498-64-7
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Related CAS # |
Palbociclib;571190-30-2;Palbociclib monohydrochloride;827022-32-2;Palbociclib hydrochloride;571189-11-2;Palbociclib dihydrochloride
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.6566 mL | 8.2832 mL | 16.5664 mL | |
5 mM | 0.3313 mL | 1.6566 mL | 3.3133 mL | |
10 mM | 0.1657 mL | 0.8283 mL | 1.6566 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.