Size | Price | Stock |
---|---|---|
5mg | $60 | In-stock |
10mg | $84 | In-stock |
50mg | $108 | In-stock |
100mg | $132 | In-stock |
500mg | $312 | In-stock |
1g | $480 | In-stock |
5 g | Get quote | |
10 g | Get quote | |
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Cat. No. : | HY-50767 |
M.Wt: | 447.53 |
Formula: | C24H29N7O2 |
Purity: | >98 % |
Solubility: | H2O : 0.1 mg/mL (0.22 mM; Need ultrasonic); DMSO : 25 mg/mL (55.86 mM; ultrasonic and warming and adjust pH to 5 with HCl and heat to 60°C); 0.1 M HCL : 25 mg/mL (55.86 mM; ultrasonic and adjust pH to 4 with 0.1 M HCL) |
Palbociclib (PD 0332991) is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib 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].
In Vitro: Palbociclib (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 (0-10 μM, 24 h) arrests MDA-MB-453 cells exclusively in G1 phase[1].
Palbociclib (500 nM, 7 days) increases expression of homologous genes (H2d1, H2k1, and B2m) in MDA-MB-453 and MDA-MB-361 cells[2].
Palbociclib (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 (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].
In Vivo: Palbociclib (oral adminstration, 75 or 150 mg/kg, daily for 14 days) produces rapid tumor regressions and delays tumor growth[1].
Palbociclib (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 (oral administration, 100 mg/kg, daily for 1 week) has potent antitumour effects in genetically engineered mosaic mouse model of liver cancer[4].
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