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PD 0332991 HCl

CAS No.
827022-32-2
Chemical Name:
PD 0332991 HCl
Synonyms
CS-365;PD 0332991 HCl;Palbociclib HCl;Palbociclib-025;Palbociclib-019-HCl;PD 0332991;PD-0332991;StemSelect PD 0332991;PD 0332991 hydrochloride;PD-0332991 (Palbociclib);PD 0332991 HCl USP/EP/BP
CBNumber:
CB22593007
Molecular Formula:
C24H30ClN7O2
Molecular Weight:
484
MDL Number:
MFCD22420809
MOL File:
827022-32-2.mol
MSDS File:
SDS
Last updated:2025-07-24 18:13:49

PD 0332991 HCl Properties

storage temp. = -70C
solubility ≥14.48 mg/mL in H2O; ≥2.42 mg/mL in DMSO; ≥2.79 mg/mL in EtOH with gentle warming and ultrasonic
form Yellow liquid
color Light yellow to yellow
Water Solubility water: 10mg/mL
InChIKey STEQOHNDWONVIF-UHFFFAOYSA-N
SMILES O=C1C(=C(C)C2=CN=C(NC3N=CC(N4CCNCC4)=CC=3)N=C2N1C1CCCC1)C(=O)C.Cl
FDA UNII BKC4F3Q5XL
UNSPSC Code 12352200
NACRES NA.77

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictograms
GHS07
Signal word  Warning
Hazard statements  H315-H319
Precautionary statements  P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313
HS Code  29399990

PD 0332991 HCl price More Price(28)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich 5.30487 StemSelect PD 0332991 - CAS 827022-32-2 - Calbiochem 827022-32-2 5mg $146 2025-07-31 Buy
Cayman Chemical 16273 PD 0332991 (hydrochloride) ≥95% 827022-32-2 1mg $37 2024-03-01 Buy
Cayman Chemical 16273 PD 0332991 (hydrochloride) ≥95% 827022-32-2 5mg $108 2024-03-01 Buy
Cayman Chemical 16273 PD 0332991 (hydrochloride) ≥95% 827022-32-2 10mg $195 2024-03-01 Buy
Cayman Chemical 16273 PD 0332991 (hydrochloride) ≥95% 827022-32-2 25mg $353 2024-03-01 Buy
Product number Packaging Price Buy
5.30487 5mg $146 Buy
16273 1mg $37 Buy
16273 5mg $108 Buy
16273 10mg $195 Buy
16273 25mg $353 Buy

PD 0332991 HCl Chemical Properties,Uses,Production

Description

PD 0332991 is an orally active, selective inhibitor of the cyclin D kinases Cdk4 (IC50 = 11 nM) and Cdk6 (IC50= 16 nM) with no activity against a panel of 36 additional protein kinases. It has been reported to have antiproliferative activity against retinoblastoma-positive tumor cells, blocking retinoblastoma phosphorylation and inducing G1 arrest at nanomolar concentrations. PD 0332991 can inhibit the growth of certain ER-positive or HER2-amplified breast cancer cells (IC50s as low as 4 nM) and demonstrates synergy with tamoxifen and trastuzumab, respectively. PD 0332991 inhibition of Cdk4 activity has been used to demonstrate a role for insulin-activated cyclinD1-Cdk4 signaling in the control of glucose metabolism that is independent of cell cycle progression.

General Description

A cell-permeable, orally available and brain permeant, non-toxic pyridopyrimidinone compound that acts as a potent, selective, reversible, ATP competitive inhibitor of Cdk4 and Cdk6 (IC50 = 11, 9, and 15 nM for Cdk4/D1, Cdk4/D3 and Cdk6/D2, respectively). Hence, it reduces retinoblastoma protein phosphorylation at Ser780/Ser795 (IC50 = 66 nM in MDA-435 cells) and arrests cell cycle at G1 phase. Acts as a cytostatic agent, but does induce apoptotic cell death when used alone. However, it potentiates the cytotoxicity of dexamethasone (>Cat. No. 265005), bortezomib (>Cat. No. 504314), and tamoxifen (Cat. No. 579000) in estrogen receptor (ER)-positive cell lines. Exhibits only a trivial inhibitory activity towards Cdk2/E2, Cdk2/A, Cdk1/B and Cdk5/p25 in a 36-kinase panel (IC50 >10 μM). Improves endoderm differentiation of late G1-human embryonic stem cells expressing Smad2 or Smad3 (~ 750 nM) and further enhances endoderm differentiation into hepatic and pancreatic progenitor cells. Shown to regress the growth of human breast tumor xenografts in murine models (~150 mg/kg, p.o., daily).

Biochem/physiol Actions

Cell permeable: yes

Synthesis

4-{6-[8-CYCLOPENTYL-6-(1-ETHOXY-VINYL)-5-METHYL-7-OXO-7,8-DIHYDRO-PYRIDO[2,3-D]PYRIMIDIN-2-YLAMINO]-PYRIDIN-3-YL}-PIPERAZINE-1-CARBOXYLIC ACID TERT-BUTYL ESTER

571189-10-1

PD 0332991 HCl

827022-32-2

Synthesis of 6-acetyl-8-cyclopentyl-5-methyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one hydrochloride from tert-butyl 4-[6-[[8-cyclopentyl-6-(1-ethoxyethenyl)-5-methyl-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino]pyridin-3-yl]piperazin-1-carboxylate. [2,3-d]pyrimidin-7(8H)-one hydrochloride was prepared in the following general procedure: to tert-butyl 4-[6-[[8-cyclopentyl-6-(1-ethoxyvinyl)-5-methyl-7-oxo-7,8-dihydropyrido[2,3-D]pyrimidin-2-yl]amino]pyridin-3-yl]piperazine-1-carboxylate under ice-bath cooling conditions (4.50 g. 0.00783 mol, as prepared in Example 2) in a solution of dichloromethane (100 mL) was bubbled with hydrogen chloride gas. The resulting suspension was sealed and stirred overnight at room temperature and subsequently diluted with ether (200 mL). The solid was collected by filtration, washed with ether and dried to afford 6-acetyl-8-cyclopentyl-5-methyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one hydrochloride as a yellow solid (4.01 g, 92% yield).

target

CDK4/cyclin D1

References

[1] ivan diaz-padilla, lillian l. siu and ignacio duran. cyclin-dependent kinase inhibitors as potential targeted anticancer agents. invest new drugs. 2009, 27: 586–594.
[2] richard s finn, judy dering, dylan conklin, ondrej kalous, david j cohen, amrita j desai, charles ginther, mohammad atefi, isan chen, camilla fowst, gerret los and dennis j slamon. pd 0332991, a selective cyclin d kinase 4/6 inhibitor, preferentially inhibits proliferation of luminal estrogen receptor-positive human breast cancer cell lines in vitro. breast cancer research. 2009, 11: r77.

571189-10-1
827022-32-2
Synthesis of PD 0332991 HCl from 4-{6-[8-CYCLOPENTYL-6-(1-ETHOXY-VINYL)-5-METHYL-7-OXO-7,8-DIHYDRO-PYRIDO[2,3-D]PYRIMIDIN-2-YLAMINO]-PYRIDIN-3-YL}-PIPERAZINE-1-CARBOXYLIC ACID TERT-BUTYL ESTER
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View Lastest Price from PD 0332991 HCl manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
PD 0332991 HCl pictures 2024-03-25 PD 0332991 HCl
827022-32-2
US $31.00-1.20 / kg 1kg 99% g-kg-tons, free sample is available Henan Fengda Chemical Co., Ltd
PD 0332991 HCl USP/EP/BP pictures 2021-08-18 PD 0332991 HCl USP/EP/BP
827022-32-2
US $1.10 / g 1g 99.9% 100 Tons min Dideu Industries Group Limited
PD 0332991 HCl pictures 2019-07-06 PD 0332991 HCl
827022-32-2
US $2.00 / kg 1kg 99% ask Career Henan Chemical Co
  • PD 0332991 HCl pictures
  • PD 0332991 HCl
    827022-32-2
  • US $31.00-1.20 / kg
  • 99%
  • Henan Fengda Chemical Co., Ltd

PD 0332991 HCl Spectrum

PD 0332991 HCl PALBOCICLIB HCL; PD0332991 HCL 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) HCl Palbociclib hydrochloride, >=98% PD-0332991 (Palbociclib) PD 0332991 hydrochloride Palbociclib HCl Palbociclib (hydrochloride) Palbociclib (PD-0332991) HCl 6-acetyl-8-cyclopentyl-5-Methyl-2-(5-(piperazin-1-yl)pyridin-2-ylaMino)pyrido[2,3-d]pyriMidin-7(8H)-one hydrochloride 6-Acetyl-8-cyclopentyl-5-methyl-2-[[5-(1-piperazinyl)-2-pyridyl]amino]pyrido[2,3-d]pyrimidin-7(8H)-one Hydrochloride PD 0332991 HCl (Palbociclib) Palbociclib-025 PD 0332991 (Palbociclib) HCl CS-365 Palbociclib-019-HCl PD 0332991;PD-0332991 Pyrido[2,3-d]pyrimidin-7(8H)-one,6-acetyl-8-cyclopentyl-5-methyl-2-[[5-(1-piperazinyl)-2-pyridinyl]amino]-,monohydrochloride Palbociclib (PD-0332991) hydrochloride 6-acetyl-8-cyclopentyl-5-methyl-2-[(5-piperazin-1-ylpyridin-2-yl)amino]pyrido[2,3-d]pyrimidin-7-one hydrochloride 6-Acetyl-8-cyclopentyl-5-methyl-2-(5-(piperazin-1-yl)pyridin-2-ylamino)pyrido[2,3-d]pyrimidin- Palbociclib hydrochloride, 99%, a highly selective CDK4/6 inhibitor PALBOCICLIB;PD-0332991 HYDROCHLORIDE;PD0332991 HYDROCHLORIDE;PD 0332991 HYDROCHLORIDE Palbociclib, brand name: Ibrance PD 0332991; PD-0332991; PD0332991; PD0332991; PD332991; PD-332991; PD 332991; PALBOCICLIB, BRAND NAME: IBRANCE PD 0332991 HCl USP/EP/BP Pyrido[2,3-d]pyrimidin-7(8H)-one,6-acetyl-8-cyclopentyl-5-me... Palbociclib (monohydrochloride) TIANFU-CHEM CAS:827022-32-2 PD 0332991 HCl 6-Acetyl-8-cyclopentyl-5-methyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one hydrochloride1 PALBOCICLIB (PD-0332991) (HCL SALT) Palbociclib Impurity 22 HCl Palbociclib Impurity 20 HCl PD 0332991 hydrochloride(1:1) StemSelect PD 0332991 PD-0332991 HCl (Palbociclib HCl) Pyrido[2,3-d]pyrimidin-7(8H)-one, 6-acetyl-8- cyclopentyl-5-methyl-2-[[5-(1-piperazinyl)-2- pyridinyl]amino]-, hydrochloride (1:1) Palbociclib hydrochloride (PD-0332991 hydrochloride 827022-32-2 C24H29N7O2HCl C24H30ClN7O2 C24H29N7O2ClH Inhibitors