[CAS NO. 212844-53-6] PurvalanolA
PRODUCTS SPECIFICATIONS [212844-53-6]
DESCRIPTION [212844-53-6]
Overview
| MDL | MFCD02179211 |
|---|---|
| Molecular Weight | 388.89 |
| Molecular Formula | C19H25ClN6O |
| SMILES | CC([C@@H](NC1=NC(NC2=CC=CC(Cl)=C2)=C3N=CN(C(C)C)C3=N1)CO)C |
2 Publications Citing Use of MCE
Summary
Purvalanol A is a potent CDK inhibitor, which inhibits cdc2-cyclin B, cdk2-cyclin A, cdk2-cyclin E, cdk4-cyclin D1, and cdk5-p35 with IC 50 s of 4, 70, 35, 850, 75 nM, resepctively.
IC50 & Target
|
cdc2-cyclin B 4 nM (IC 50 ) |
cdk2-cyclin E 35 nM (IC 50 ) |
cdk2-cyclin A 70 nM (IC 50 ) |
cdk4-cyclin D1 850 nM (IC 50 ) |
cdk5-p35 75 nM (IC 50 ) |
erk1 9000 nM (IC 50 ) |
In Vitro
Purvalanol A inhibits cdc28 (S. cerevisiae) and erk1 with IC 50 s of 80 and 9000 nM. Purvalanol A shows inhibitory activities against the NCI panel of 60 human tumor cell lines, with average GI50 of 2 μM; two cell lines show an -20-fold increase in sensitivity to purvalanol A: the KM12 colon cancer cell line with a GI 50 of 76 nM and the NCI-H522 non–small cell lung cancer cell line with a GI 50 of 347 nM [1] . Purvalanol A is a 2.5-fold more potent inhibitor of CDK2, but also inhibits DYRK1A potently and a number of other protein kinases in the low micromolar range. Purvalanol A inhibits MKK1, MAPK2/ERK2, JNK/SAPK1c with IC 50 s of 80, 26, 84 μM [2] . Purvalanol A selectively inhibits the phosphorylation of cellular proteins. Purvalanol A prevents the increases of the contents of cyclins D and E during serum-induced G1 phase progression. Purvalanol A does not inhibit transcription under cell-free conditions [3] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 50 mg/mL ( 128.57 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.5714 mL | 12.8571 mL | 25.7142 mL |
| 5 mM | 0.5143 mL | 2.5714 mL | 5.1428 mL |
| 10 mM | 0.2571 mL | 1.2857 mL | 2.5714 mL |
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1.
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2.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (6.43 mM); Clear solution
References
- [1] Gray NS, et al. Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors. Science. 1998 Jul 24;281(5376):533-8.
- [2] Bain J, et al. The specificities of protein kinase inhibitors: an update. Biochem J. 2003 Apr 1;371(Pt 1):199-204.
- [3] Villerbu N, et al. Cellular effects of purvalanol A: a specific inhibitor of cyclin-dependent kinase activities. Int J Cancer. 2002 Feb 20;97(6):761-9.
Synonyms