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Palbociclib

CAS NO.: 571190-30-2 Purity: 99%
Item Code: BOZ-API-001
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Product Name: Palbociclib

Other Name: 6-acetyl-8-cyclopentyl-5-methyl-2-{[5-(piperazin-1-yl)pyridin-2yl]

           amino}pyrido[2,3-d]pyrimidin-7-(8H)-one

CAS NO.: 571190-30-2

Molecular Formula: C24H29N7O2

Molecular Weight: 447.53

Appearance: Light Yellow to Yellow Powder

Purity: 99%

Density: 1.313g/cm3

Melting Point: 200ºC

Boiling Point: 711.5ºC at 760 mmHg

Flash Point: 384.1ºC

Refractive Index: 1.647

Package: 1kg/Foil Bag; 25kg/Drum or as Required

Product Description: 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].

 

Palbociclib (codenamed PD-0332991, trade name Ibrance) is a drug for the treatment of ER-positive and HER2-negative breast cancer developed by . It is a selective inhibitor of the cyclin-dependent kinases CDK4 and CDK6. 

 

The drug IBRANCE was reviewed and approved under the Food and Drug Administration's (FDA) accelerated Priority Review and Breakthrough Therapy designation programs on February 3, 2015 as a treatment (in combination with letrozole) for patients with estrogen receptor-positive advanced breast cancer. A potentially confirmatory phase 3 trial, PALOMA-2, has fully enrolled patients. The PALOMA-3 trial announced in April 2015 that the addition of palbociclib was superior to fulvestrant alone for progression-free survival.

 

Palbociclib (PD-0332991) is an orally available pyridopyrimidine-derived cyclin-dependent kinase (CDK) inhibitor with potential antineoplastic activity. Palbociclib is a highly specific inhibitor of cyclindependent kinase 4 (Cdk4) (IC50, 0.011 μmol/L) and Cdk6 (IC50, 0.016 μmol/L), having no activity against a panel of 36 additional protein kinases.

 Breast Cancer New Drugs: Prabhu past Lieb (palbociclib) by developed new drugs to treat breast cancer, the trade name IBRANCE, IBRANCE an oral cyclin-dependent kinases (CDKs) 4 and 6 inhibitor for the United States FDA Approves first cyclin-dependent kinase 4/6 (CDK4 / 6) inhibitors. CDKs4 and 6 are a key factor in regulating the cell cycle, which can trigger cell cycle progression. IBRANCE indications in the United States for the joint letrozole for the treatment of estrogen receptor positive, human epidermal growth factor receptor 2-negative (ER + / HER2-) advanced breast cancer in postmenopausal patients as initial endocrine therapy based programs treatment of metastatic disease.

Storage: 3years in -20ºC


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