Purvalanol A (NG60)

Alias:
Cat No.:V1540 Purity: ≥98%
Purvalanol A (NG60; NG-60; NG 60) is a potent and cell-permeable CDK (cyclin-dependent kinase) inhibitor with potential antitumor activity.
Purvalanol A (NG60) Chemical Structure CAS No.: 212844-53-6
Product category: CDK
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
25mg
50mg
100mg
250mg
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1g
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Other Forms of Purvalanol A (NG60):

  • Purvalanol B (NG 95)
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Purvalanol A (NG60; NG-60; NG 60) is a potent and cell-permeable CDK (cyclin-dependent kinase) inhibitor with potential antitumor activity. It has IC50 values of 4 nM, 70 nM, 35 nM, and 850 nM for cdc2-cyclin B, cdk2-cyclin A, cdk2-cyclin E, and cdk4-cyclin D1 inhibition, respectively. Purvalanol A (30 μM) caused apoptosis in MKN45 cells by downregulating the expression of the antiapoptotic proteins survivin, Bcl-XL, and Bcl-2. Additionally, purvalanol A inhibited the expression and phosphorylation of RNA polymerase II, which was involved in transcriptional regulation, as well as the phosphorylation of STAT3 by Janus kinase 2 (JAK2).

Biological Activity I Assay Protocols (From Reference)
Targets
cdc2-cyclin B (IC50 = 4 nM); cdk2-cyclin E (IC50 = 35 nM); cdk2-cyclin A (IC50 = 70 nM); cdk4-cyclin D1 (IC50 = 850 nM); cdk5-p35 (IC50 = 75 nM); erk1 (IC50 = 9000 nM)
ln Vitro

Purvalanol A has IC50s of 80 and 9000 nM for inhibiting cdc28 (S. cerevisiae) and erk1. Purvalanol A exhibits inhibitory activities against the NCI panel of 60 human tumor cell lines, with an average GI50 of 2 μM. Two cell lines, the NCI-H522 non-small cell lung cancer cell line with a GI50 of 347 nM and the KM12 colon cancer cell line with a GI50 of 76 nM, exhibit a -20-fold increase in sensitivity to purvalanol A[1]. In addition to being a 2.5-fold more potent inhibitor of CDK2, purvalanol A also exhibits potent low-micromolar inhibitory effects on DYRK1A and several other protein kinases. Purvalanol A inhibits JNK/SAPK1c, MKK1, MAPK2/ERK2, and has IC50 values of 80, 26, and 84 μM[2]. The phosphorylation of cellular proteins is specifically inhibited by purvalanol A. When the G1 phase is induced by serum, purvalanol A stops the contents of cyclins D and E from increasing. In cell-free environments, purvalanol A does not impede transcription[3].

ln Vivo
Purvalanol A (40 nmol/3 μl) dramatically increased the number of BrdU-positive cells in the dentate gyrus (DG) of the rat hippocampal region in a concentration- and time-dependent manner.
Enzyme Assay
Purvalanol A is a potent CDK inhibitor, inhibiting cdc2-cyclin B, cdk2-cyclin A, cdk2-cyclin E, cdk4-cyclin D1, and cdk5-p35 with IC50s of 4, 70, 35, 850, 75 nM, resepctively.
Cell Assay
In 96-well plates, cells are seeded at a density of 10,000 and exposed to different concentrations of Purvalanol A (0-100 μM) for a duration of 24 hours. For four hours, cells are incubated at 37°C after being exposed to 10 μL of 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide dye (5 mg/mL). 100 μL of DMSO is added to the formazan crystals to help them dissolve. The absorbance is measured spectrophotometrically at 570 nm.
Animal Protocol
40 nmol/3 μl
Rats
References

[1]. Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors. Science. 1998 Jul 24;281(5376):533-8.

[2]. The specificities of protein kinase inhibitors: an update. Biochem J. 2003 Apr 1;371(Pt 1):199-204.

[3]. Cellular effects of purvalanol A: a specific inhibitor of cyclin-dependent kinase activities. Int J Cancer. 2002 Feb 20;97(6):761-9.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C19H25CLN6O
Molecular Weight
388.89
Exact Mass
388.18
Elemental Analysis
C, 58.68; H, 6.48; Cl, 9.12; N, 21.61; O, 4.11
CAS #
212844-53-6
Appearance
Grey to green solid powder
SMILES
CC(C)[C@H](CO)NC1=NC(=C2C(=N1)N(C=N2)C(C)C)NC3=CC(=CC=C3)Cl
InChi Key
PMXCMJLOPOFPBT-HNNXBMFYSA-N
InChi Code
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
Chemical Name
(2R)-2-[[6-(3-chloroanilino)-9-propan-2-ylpurin-2-yl]amino]-3-methylbutan-1-ol
Synonyms

NG60; NG-60; NG 60

HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~60 mg/mL (~154.3 mM)
Water: <1 mg/mL
Ethanol: ~13 mg/mL (~33.4 mM)
Preparing Stock Solutions 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

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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Biological Data
  • Entry of BP-A31 cells into S-phase: effects of purvalanol A and B. Int J Cancer . 2002 Feb 20;97(6):761-9.
  • Effect of purvalanol A on cell cycle progression. Int J Cancer . 2002 Feb 20;97(6):761-9.
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