PD0332991, Cdk4/Cdk6 inhibitor (ab218118)
- Datasheet
- References
Overview
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Product name
PD0332991, Cdk4/Cdk6 inhibitor -
Description
Potent, highly specific Cdk4/Cdk6 inhibitor -
Alternative names
- Palbociclib
- PD-0332991
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Biological description
Potent, highly specific inhibitor of Cdk4 (IC50 = 11 nM) and Cdk6 (IC50 = 16 nM). Displays selectivity for Cdk4/6 over a panel of 36 additional protein kinases (IC50 values are > 10 μM). Induces G1 cell cycle arrest and senescence in retinoblastoma protein (Rb)-proficient cell lines. Blocks growth of intracranial glioblastoma multiforme xenografts in mice. Blood-brain barrier permeable.
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Purity
> 98% -
CAS Number
571190-30-2 -
Chemical structure
Properties
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Chemical name
6-Acetyl-8-cyclopentyl-5-methyl-2-[[5-(1-piperazinyl)-2-pyridinyl]amino]pyrido[2,3-d]pyrimidin-7(8H)-one -
Molecular weight
447.53 -
Molecular formula
C24H29N7O2 -
PubChem identifier
5330286 -
Storage instructions
Shipped at 4°C. Store at -20°C. Store under desiccating conditions. -
Solubility overview
Soluble in DMSO -
Handling
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
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SMILES
CC1=C(C(=O)N(C2=NC(=NC=C12)NC3=NC=C(C=C3)N4CCNCC4)C5CCCC5)C(=O)C -
Source
Synthetic
References
This product has been referenced in:
- Michaud K et al. Pharmacologic inhibition of cyclin-dependent kinases 4 and 6 arrests the growth of glioblastoma multiforme intracranial xenografts. Cancer Res 70:3228-38 (2010). Read more (PubMed: 20354191) »
- Finn RS et al. 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 Res 11:R77 (2009). Read more (PubMed: 19874578) »
- Toogood PL et al. Discovery of a potent and selective inhibitor of cyclin-dependent kinase 4/6. J Med Chem 48:2388-406 (2005). Read more (PubMed: 15801831) »
- Fry DW et al. Specific inhibition of cyclin-dependent kinase 4/6 by PD 0332991 and associated antitumor activity in human tumor xenografts. Mol Cancer Ther 3:1427-38 (2004). Read more (PubMed: 15542782) »
