Palbociclib; CAS 571190-30-2

Colour
White
Samples
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Purity
99%
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5-7 Working Days
Shelf Life
2-3 Years
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MOQ
10g
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Yunbang
Origin
China
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Product Description

Palbociclib;CAS 571190-30-2
 
Palbociclib; CAS 571190-30-2
 
Palbociclib Chemical Properties
Melting point  200 ºC
Boiling point  711.5±70.0 °C(Predicted)
density  1.313±0.06 g/cm3(Predicted)
storage temp.  room temp
pka 8.66±0.10(Predicted)
form  powder
color  white to beige
 
Safety Information
 
MSDS Information
 
 
Palbociclib Usage And Synthesis
Description 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 fu lvestrant 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.
Definition 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 letro zole for the treatment of metastatic breast cancer.
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 letro zole.
Chemical Synthesis Numerous syntheses of palbociclib have been reported,149,150 and the commercial scale process published by scientists at Pfizer is described herein. The amino-pyridylpiper azine fragment 212 was prepared in two steps. Commercial pip erazine 209 was added to 5-bromo-2-nitropyridine (210) to give nitro-pyridine 211 in 93% yield. Hydrogenation of the nitro group using catalytic palladium on carbon provided the amino-pyridylpipe razine 212 in 96% yield.
As such, cyclopent ylamine (214) was added to 5-bromo-2,4-dichloropyrimidine (213) to give 5-bromo-2-chloro-6-cyclopentylaminopyrimidine (215) in 84% yield. Heck reaction with croto nic acid followed by treating the resulting product with acetic anh ydride formed the mixed anhydride under elevated temperatures, and this resulted in cyclization to give pyrimidinone 214 in 81% yield. Bromination using N-bromosuccinimide (NBS) provided coupling partner 217 in 88% yield. Next, aminopyridine 212 was treated with cyclohexylmagnesium chloride and then reacted with 217 to give the SNAr product 218 in 88% yield. A second Heck reaction between bromide 218 and butyl vinyl ether (219) using palladium acetate/bis(2- diphenylphosphinophenyl)ether (DPEPhos) as the catalyst provided enol ether 220 in 84% yield. Exposure of 220 to acidic conditions removed the Boc group from the pipe razine while converting the enol ether to the corresponding ketone, providing palbociclib (XXVII) in 90% yield.
Enzyme inhibitor 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 letro zole 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).
 
 
Palbociclib; CAS 571190-30-2 Palbociclib; CAS 571190-30-2 Palbociclib; CAS 571190-30-2 Palbociclib; CAS 571190-30-2
Company Informations:

Hunan Yunbang Pharmaceutical Co., Ltd. ( Yunbangpharm) located in Changsha High-tech Industrial Park, Hunan. It is a high-tech enterprise specializing in the research and development, production and sales of Pharmaceutical raw materials, Pharmaceutical intermediates(API) and Fine chemicals. Based in China, Yunbangpharm has been providing suitable solutions for many domestic,foreign pharmaceutical companies and traders. Excellent quality, good reputation and authentic price have won the praise of the majority of customers.
The company adheres to the corporate tenet of "We do not produce medicines, but help pharmaceutical companies make good medicines".

We can provide customers with customized processing, research and development services;
We can develop high-end Pharmaceutical and chemical products with high technical difficulties,high barriers and unique production processes;
We can provide 100 grams Grade, kilograms, and hundred kilograms of raw material pharmaceutical intermediates and other products.
We can perform -100°C to 300°C reaction.

R&D strength is the company's core competitiveness.Yunbangpharm has maintains a good cooperation relationship with many Universities and Research institutes locally, which can quickly transform R&D results into industrial production.

Our goal : To achieve the integrated upgrade of P harmaceutical intermediates, raw materials and high-end chemical products, adhere to "serving pharmaceutical companies, creating our brands" to provide customers with high-quality and low-cost pharmaceutical and chemical products, realizing Win-win cooperation and common development.

 

Organic Intermediate