PD 0332991 HCl
- Product Name
- 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
- Formula Weight
- 484
- MOL File
- 827022-32-2.mol
PD 0332991 HCl Property
- 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
Safety
- HS Code
- 29399990
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H315Causes skin irritation
H319Causes serious eye irritation
- Precautionary statements
-
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P332+P313IF SKIN irritation occurs: Get medical advice/attention.
P337+P313IF eye irritation persists: Get medical advice/attention.
N-Bromosuccinimide Price
- Product number
- 5.30487
- Product name
- StemSelect PD 0332991 - CAS 827022-32-2 - Calbiochem
- Packaging
- 5mg
- Price
- $146
- Updated
- 2025/07/31
- Product number
- 16273
- Product name
- PD 0332991 (hydrochloride)
- Purity
- ≥95%
- Packaging
- 1mg
- Price
- $37
- Updated
- 2024/03/01
- Product number
- 16273
- Product name
- PD 0332991 (hydrochloride)
- Purity
- ≥95%
- Packaging
- 5mg
- Price
- $108
- Updated
- 2024/03/01
- Product number
- 16273
- Product name
- PD 0332991 (hydrochloride)
- Purity
- ≥95%
- Packaging
- 10mg
- Price
- $195
- Updated
- 2024/03/01
- Product number
- 16273
- Product name
- PD 0332991 (hydrochloride)
- Purity
- ≥95%
- Packaging
- 25mg
- Price
- $353
- Updated
- 2024/03/01
PD 0332991 HCl Chemical Properties,Usage,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
571189-10-1
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.
PD 0332991 HCl Preparation Products And Raw materials
Raw materials
Preparation Products
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View Lastest Price from PD 0332991 HCl manufacturers
- Product
- PD 0332991 HCl 827022-32-2
- Price
- US $31.00-1.20/kg
- Min. Order
- 1kg
- Purity
- 99%
- Supply Ability
- g-kg-tons, free sample is available
- Release date
- 2024-03-25
- Product
- PD 0332991 HCl 827022-32-2
- Price
- US $1.10/g
- Min. Order
- 1g
- Purity
- 99.9%
- Supply Ability
- 100 Tons min
- Release date
- 2021-08-17
- Product
- PD 0332991 HCl 827022-32-2
- Price
- US $2.00/kg
- Min. Order
- 1kg
- Purity
- 99%
- Supply Ability
- ask
- Release date
- 2018-12-23