PD0332991, Cdk4/Cdk6 inhibitor (ab218118)
- Datasheet
- References
Overview
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Product namePD0332991, Cdk4/Cdk6 inhibitor
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DescriptionPotent, highly specific Cdk4/Cdk6 inhibitor
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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%
Properties
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Chemical name6-Acetyl-8-cyclopentyl-5-methyl-2-[[5-(1-piperazinyl)-2-pyridinyl]amino]pyrido[2,3-d]pyrimidin-7(8H)-one
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Molecular weight447.53
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Chemical structure
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Molecular formulaC24H29N7O2
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CAS Number571190-30-2
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PubChem identifier5330286
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Storage instructionsShipped at 4°C. Store at -20°C. Store under desiccating conditions.
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Solubility overviewSoluble in DMSO
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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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SMILESCC1=C(C(=O)N(C2=NC(=NC=C12)NC3=NC=C(C=C3)N4CCNCC4)C5CCCC5)C(=O)C
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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) »
