6-Acetyl-8-cyclopentyl-5-methyl-2-[[5-(1-piperazinyl)-2-pyridinyl]amino]pyrido[2,3-d]pyrimidin-7(8H)-one hydrochloride

Modify Date: 2024-08-10 14:55:08

6-Acetyl-8-cyclopentyl-5-methyl-2-[[5-(1-piperazinyl)-2-pyridinyl]amino]pyrido[2,3-d]pyrimidin-7(8H)-one hydrochloride Structure
6-Acetyl-8-cyclopentyl-5-methyl-2-[[5-(1-piperazinyl)-2-pyridinyl]amino]pyrido[2,3-d]pyrimidin-7(8H)-one hydrochloride structure
Common Name 6-Acetyl-8-cyclopentyl-5-methyl-2-[[5-(1-piperazinyl)-2-pyridinyl]amino]pyrido[2,3-d]pyrimidin-7(8H)-one hydrochloride
CAS Number 571189-11-2 Molecular Weight 520.45500
Density N/A Boiling Point N/A
Molecular Formula C24H31Cl2N7O2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of 6-Acetyl-8-cyclopentyl-5-methyl-2-[[5-(1-piperazinyl)-2-pyridinyl]amino]pyrido[2,3-d]pyrimidin-7(8H)-one hydrochloride


Palbociclib (PD 0332991) hydrochloride is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib hydrochloride has potent anti-proliferative activity and induces cell cycle arrest in cancer cells. Palbociclib hydrochloride can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma[1][3][4].

 Names

Name 6-acetyl-8-cyclopentyl-5-methyl-2-[(5-piperazin-1-ylpyridin-2-yl)amino]pyrido[2,3-d]pyrimidin-7-one,dihydrochloride

  Biological Activity

Description Palbociclib (PD 0332991) hydrochloride is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib hydrochloride has potent anti-proliferative activity and induces cell cycle arrest in cancer cells. Palbociclib hydrochloride can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma[1][3][4].
Related Catalog
Target

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)

In Vitro Palbociclib (0-1 μM, 24 h) hydrochloride inhibits retinoblastoma 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) hydrochloride arrests MDA-MB-453 cells exclusively in G1 phase[1]. Palbociclib (500 nM, 7 days) hydrochloride 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) hydrochloride 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) hydrochloride 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]. 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: 0-1 μM Incubation Time: 6 days Result: Inhibited growth of luminal ER-positive as well as HER2-amplified breast cancer cell lines. Cell Cycle Analysissup>[1] Cell Line: MDA-MB-453 cells Concentration: 0-1 μM Incubation Time: 24 h Result: Arrested MDA-MB-453 cells in G1.
In Vivo Palbociclib (oral adminstration, 75 or 150 mg/kg, daily for 14 days) hydrochloride produces rapid tumor regressions and delays tumor growth[1]. Palbociclib (oral adminstration, 90 mg/kg, daily for 12 days) hydrochloride 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) hydrochloride has potent antitumour effects in genetically engineered mosaic mouse model of liver cancer[4]. Animal Model: Mice bearing Colo-205 colon carcinoma xenografts (p16 deleted)[1] Dosage: 75, 150 mg/kg Administration: Oral administration; daily for 14 days 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 Administration: Oral administration; daily for 12 days 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 Administration: Oral administration; daily for 1 week Result: Decreased the luminescence signal in liver and delayed tumour growth.

 Chemical & Physical Properties

Molecular Formula C24H31Cl2N7O2
Molecular Weight 520.45500
Exact Mass 519.19200
PSA 105.04000
LogP 5.03660