Purvalanol A
| Code | Size | Price |
|---|
| AG-CR1-2903-M001 | 1 mg | £60.00 |
Quantity:
| AG-CR1-2903-M005 | 5 mg | £105.00 |
Quantity:
| AG-CR1-2903-M025 | 25 mg | £325.00 |
Quantity:
Prices exclude any Taxes / VAT
Overview
Regulatory Status: RUO
Shipping:
-20°C
Storage:
Short Term: +4°C. Long Term: -20°C
Documents
Further Information
Alternate Names/Synonyms:
2-(1R-Isopropyl-2-hydroxyethylamino)-6-(3-chloroanilino)-9-isopropylpurine; NG 60
Appearance:
Off-white powder.
CAS:
212844-53-6
EClass:
32160000
Form (Short):
liquid
InChi:
InChI=1S/C19H25ClN6O/c1-11(2)15(9-27)23-19-24-17(22-14-7-5-6-13(20)8-14)16-18(25-19)26(10-21-16)12(3)4/h5-8,10-12,15,27H,9H2,1-4H3,(H2,22,23,24,25)/t15-/m0/s1
InChiKey:
PMXCMJLOPOFPBT-HNNXBMFYSA-N
Long Description:
Chemical. CAS: 212844-53-6. Formula: C19H25ClN6O. MW: 388.9. Synthetic. 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.
MDL:
MFCD02179211
Molecular Formula:
C19H25ClN6O
Molecular Weight:
388.9
Package Type:
Plastic Vial
Product 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.
Purity:
>98% (HPLC)
SMILES:
ClC1=CC=CC(NC2=C3C(N(C(C)C)C=N3)=NC(N[C@@H](CO)C(C)C)=N2)=C1
Solubility Chemicals:
Soluble in DMSO (30mg/ml), ethanol (10mg/ml), DMF (50mg/ml), methanol or dichloromethane.
Transportation:
Non-hazardous
UNSPSC Category:
Protein Kinase Modulators
UNSPSC Number:
12352200
Use & Stability:
Stable for at least 2 years after receipt when stored at -20°C.
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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