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;PD 0332991 hydrochloride;PD-0332991 (Palbociclib);PD 0332991 HCl USP/EP/BP;Palbociclib (hydrochloride)
- 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
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
-
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
- $142
- Updated
- 2024/03/01
- 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
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
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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 $50.00/kg
- Min. Order
- 1kg
- Purity
- 99%
- Supply Ability
- 1
- Release date
- 2022-10-18
- 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