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AdipoGen Life Sciences
Purvalanol A
60
CHF
CHF 60.00
In stock
AG-CR1-2903-M0011 mgCHF 60.00
AG-CR1-2903-M0055 mgCHF 120.00
AG-CR1-2903-M02525 mgCHF 360.00
| Product Details | |
|---|---|
| Synonyms | 2-(1R-Isopropyl-2-hydroxyethylamino)-6-(3-chloroanilino)-9-isopropylpurine; NG 60 |
| Product Type | Chemical |
| Properties | |
| Formula |
C19H25ClN6O |
| MW | 388.9 |
| CAS | 212844-53-6 |
| Purity Chemicals | ≥98% (HPLC) |
| Appearance | Off-white powder. |
| Solubility | Soluble in DMSO (30mg/ml), ethanol (10mg/ml), DMF (50mg/ml), methanol or dichloromethane. |
| Identity | Determined by 1H-NMR. |
| InChi Key | PMXCMJLOPOFPBT-HNNXBMFYSA-N |
| Smiles | ClC1=CC=CC(NC2=C3C(N(C(C)C)C=N3)=NC(N[C@@H](CO)C(C)C)=N2)=C1 |
| Shipping and Handling | |
| Shipping | AMBIENT |
| Short Term Storage | +4°C |
| Long Term Storage | -20°C |
| Use/Stability | Stable for at least 2 years after receipt when stored at -20°C. |
| Documents | |
| MSDS |
 Download PDF |
| Product Specification Sheet | |
| Datasheet |
Download PDF |
Description
- Potent, cell permeable cyclin-dependent protein kinase (cdk) inhibitor. Inhibits human CDK1 (IC50=4nM), CDK2/cyclin A (IC50=70nM), Cdc2/cyclin B, CDK2/cyclin E (IC50=35nM), CDK4/cyclin D1 (IC50=850nM) as well as CDK5/p35 (IC50=75nM).
- DYRK1A inhibitor (IC50=300nM).
- Anticancer agent. Strong apoptotic and autophagy inducer which causes cell cycle arrest in the G1 and G2 phase in various cancer cell lines.
- More membrane permeable than purvalanol B.
- Shown to inhibit ABCB1 and ABCB2 transporters and useful in co-treatment with selected anticancer drugs.
Product References
- Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors: N.S. Gray, et al.; Science 281, 533 (1998)
- The specificities of protein kinase inhibitors: An update: J. Bain, et al.; Biochem. J. 371, 199 (2003)
- Cellular effects of purvalanol A: A specific inhibitor of cyclin-dependent kinase activities: N. Villerbu, et al.; Int. J. Cancer 97, 761 (2002)
- Purvalanol A induces apoptosis and downregulation of antiapoptotic proteins through abrogation of phosphorylation of JAK2/STAT3 and RNA polymerase II: D. Iizuka, et al.; Anticancer Drugs 19, 565 (2008)
- Purvalanol A, a CDK inhibitor, effectively suppresses Src-mediated transformation by inhibiting both CDKs and c-Src: T. Hikita, et al.; Genes to Cells 15, 1051 (2010)
- Olomoucine II and purvalanol A inhibit ABCG2 transporter in vitro and in situ and synergistically potentiate cytostatic effect of mitoxantrone: J. Hofman, et al.; Pharmacol. Res. 65, 312 (2012)
- Purvalanol A, olomoucine II and roscovitine inhibit ABCB1 transporter and synergistically potentiate cytotoxic effects of daunorubicin in vitro: D. Cihalova, et al.; PLoS One 8, e83467 (2013)
- Purvalanol induces endoplasmic reticulum stress-mediated apoptosis and autophagy in a time-dependent manner in HCT116 colon cancer cells: A. Coker-Gurkan, et al.; Oncol. Rep. 33, 2761 (2015)
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