팔보시클립

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팔보시클립 화학적 특성, 용도, 생산

• 개요

  Palbociclib is a cyclin-dependent kinase (CDK) 4 and CDK6 inhibitor approved by the FDA to treat hormone receptor-positive (HR+) human epidural growth factor 2-negative (HER2-) metastatic breast cancer. It is used in combination with letrazole as the first-line hormonal-based therapy in postmenopausal women, or with fulvestrant in women with disease progression following hormonal therapy. Palbociclib was discovered at Warner- Lambert and developed by Pfizer after their merger. Pfizer is also studying the effectiveness of palbociclib in a variety of other cancers at various stages in the clinic.

• 용도

  Palbociclib (also known as compound number PD-0332991) is an experimental drug for the treatment of breast cancer being developed by Pfizer. It is a selective inhibitor of the cyclin-dependent kinases CDK4 and CDK6.

• Indications

  Palbociclib (Ibrane(R), Pfizer), a selective CDK4 and CDK6 inhibitor, received accelerated approval from FDA in 2015 for women with estrogen receptor-positive and HER2-negative breast cancer in combination with letrozole.

• 정의

  ChEBI: A member of the class of pyridopyrimidines that is 2-{[5-(piperazin-1-yl)pyridin-2-yl]amino}pyrido[2,3-d]pyrimidin-7-one bearing additional methyl, acetyl and cyclopentyl substituents at positions 5, 6 and 8 respectively. It is used in combina ion with letrozole for the treatment of metastatic breast cancer.

• 효소 저해제

  This orally active, non-ATP-competitive cyclin kinase-directed inhibitor (FW = 483.99 g/mol (mono-HCl); CASs = 827022-32-2 (mono- hydrochloride, 571190-30-2 (free base); Solubility: 10 mg/mL DMSO; 30 mg/mL Water; Formulation: Dissolved in sodium lactate buffer (50 mM, ® pH 4.0) ), also known as PD-0332991, Ibrance, and 6-acetyl-8-cyclopentyl- 5-methyl-2- (5- (piperazin-1-yl) pyridin-2-ylamino) pyrido[2,3-d]pyrimidin- 7 (8H) -one hydrochloride, targets Cdk-4 (Cyclin D1) and Cdk-6 (Cyclin D2), enzymes that participate in the so-called CDK4/6-retinoblastoma signaling pathway governing the cell-cycle restriction point. Palbociclib induces rapid G1 cell-cycle arrest in primary human myeloma cells. This agent also shows significant efficacy in a broad spectrum of human tumor xenografts in vivo, resulting in complete regression in some tumors with no evidence of acquired resistance or ability to circumvent the growth inhibitory properties of this agent. Ibrance received FDA approval in 2015 for combined use with letrozole to treat postmenopausal women with estrogen receptor- positive, (HER2) -negative advanced breast cancer as an initial endocrine- based therapy for metastatic disease. Cyclin Target Selectivity: Cdk1 (weak, if any), Cdk2 (weak, if any), Cdk3 (weak, if any), Cdk4 (IC50 = 11 nM), Cdk5 (weak, if any), Cdk6 (IC50 = 16 nM), Cdk7 (weak, if any), Cdk8 (weak, if any), Cdk9 (weak, if any), Cdk10 (weak, if any).

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