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Palbociclib

Palbociclib
Palbociclib structure
CAS No.
571190-30-2
Chemical Name:
Palbociclib
Synonyms
bocicL;Pab Xilib;palboclib;PD0332991;albociclib;Pabuxilibu;Palbociclib; 571190-30-2;API-Anti-Tumer;albociclib API
CBNumber:
CB62464897
Molecular Formula:
C24H29N7O2
Formula Weight:
447.53
MOL File:
571190-30-2.mol

Palbociclib 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
FDA UNII
G9ZF61LE7G
NCI Dictionary of Cancer Terms
palbociclib
NCI Drug Dictionary
palbociclib
ATC code
L01EF01

Palbociclib price More Price(36)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
TRC P139900 Palbociclib 571190-30-2 100mg $95 2021-12-16 Buy
TRC P139900 Palbociclib 571190-30-2 500mg $340 2021-12-16 Buy
ApexBio Technology B7798 PD0332991(Palbociclib) 571190-30-2 25mg $90 2021-12-16 Buy
Biorbyt Ltd orb546251 Palbociclib >98% 571190-30-2 25 mg $307.7 2021-12-16 Buy
American Custom Chemicals Corporation API0028131 PALBOCICLIB 95.00% 571190-30-2 5MG $459.22 2021-12-16 Buy

Palbociclib Chemical Properties,Uses,Production

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 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.

Uses

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.

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 letrozole 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 letrozole.

Biochem/physiol Actions

PF-00080665 (Palbociclib; PD 0332991) is an orally active and highly specific inhibitor against cyclin-dependent kinase 4 & 6 (IC50 = 9, 11, 15 nM, respectively, using CDK4/cycD3, CDK4/cycD1, CDK6/cycD2; IC50 >10 μM against 36 other kinases) that potently suppresses Cdk4/6-dependent cellular Rb phosphorylation (IC50 = 66 nM/pSer780 & 63 nM/pSer795; MDA-MB-435). PF-00080665 exhibits selective antiproliferation activity against Rb-positive human breast/colon/lung/leukemia cancer cultures (IC50 = 40-400 nM; IC50 >3 μM/Rb-negative MDA-MB-468 & H2009) and displays in vivo efficacy against various advanced stage human tumor xenografts in mice (12.5-150 mg/kg/day p.o.).

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-pyridylpiperazine fragment 212 was prepared in two steps. Commercial piperazine 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-pyridylpiperazine 212 in 96% yield.
As such, cyclopentylamine (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 crotonic acid followed by treating the resulting product with acetic anhydride 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 piperazine 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 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).

Palbociclib Preparation Products And Raw materials

Raw materials

Preparation Products


Palbociclib Suppliers

Global( 344)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
TianYuan Pharmaceutical CO.,LTD
+86-755-23284190 13684996853
+86-755-23284190 sales@tianpharm.com CHINA 305 58
Capot Chemical Co.,Ltd.
+86(0)13336195806 +86-571-85586718
+86-571-85864795 sales@capotchem.com China 20012 60
Henan DaKen Chemical CO.,LTD.
+86-371-66670886
info@dakenchem.com China 15426 58
Beijing Cooperate Pharmaceutical Co.,Ltd
010-60279497
010-60279497 sales01@cooperate-pharm.com CHINA 1817 55
Shanghai Bojing Chemical Co.,Ltd.
+86-21-37122233
+86-21-37127788 Candy@bj-chem.com CHINA 497 55
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com China 22607 55
Hangzhou FandaChem Co.,Ltd.
008615858145714
+86-571-56059825 fandachem@gmail.com CHINA 9115 55
Nanjing ChemLin Chemical Industry Co., Ltd.
025-83697070
product@chemlin.com.cn CHINA 3013 60
Nanjing Finetech Chemical Co., Ltd.
025-85710122 17714198479
025-85710122 sales@fine-chemtech.com CHINA 890 55
ATK CHEMICAL COMPANY LIMITED
+86 21 5161 9050/ 5187 7795
+86 21 5161 9052/ 5187 7796 ivan@atkchemical.com CHINA 26782 60

View Lastest Price from Palbociclib manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2021-03-17 Palbociclib
571190-30-2
US $0.00 / KG 1g 99.9% 1 ton Hebei shuoxi biotechnology co. LTD
2020-11-16 Palbociclib
571190-30-2
US $20.00 / KG 1KG 99% 1000kg Longyan Tianhua Biological Technology Co., Ltd
2020-07-22 Palbociclib
571190-30-2
US $0.00-0.00 / KG 1g 99% 100kg/month Beijing Yibai Biotechnology Co., Ltd

571190-30-2(Palbociclib)Related Search:


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