Aminopurvalanol AA reversible and ATP-competitive inhibitor of Cdks

Aminopurvalanol A (CAS 220792-57-4)

Aminopurvalanol A | CAS 220792-57-4 is rated 5.0 out of 5 by 1.
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Synonym: (2R)-2-((6-((3-Amino-5-chlorophenyl)amino)-9-(1-methylethyl)-9H-purin-2-yl)amino)-3-methyl-1-butanol; NG-97
Application: A reversible and ATP-competitive inhibitor of Cdks
CAS Number: 220792-57-4
Molecular Weight: 403.91
Molecular Formula: C19H26ClN7O
* Refer to Certificate of Analysis for lot specific data (including water content).
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Aminopurvalanol A is a cell-permeable 2,6,9-trisubstituted purine analog that displays anti-mitotic as well as anti-tumor properties (GI50 ~ 1.8 μM in the NCI 60-cell panel in vitro activity screen; potently inhibits the growth of KM12 colon cancer cells with a GI50 of 30 nM) Aminopurvalanol A acts as a reversible and ATP-competitive inhibitor of Cdks (IC50 = 33 nM for cdc2 (Cdk1)/cyclin B and Cdk2/cyclin A, 28 nM for Cdk2/cyclin E, and 20 nM for Cdk5/p35), and displays ~ 100-fold greater selectivity over a panel of kinases tested (IC50 ≥ 2.4 μM). Aminopurvalanol A has been shown to induce cell differentiation by preferentially targeting the G2/M-phase and act intracellularly by inhibiting both Cdks and MAPKs.


References

Breton, M.L., et al. 2003. Biochem. Biophys. Res. Commun. 306, 880. Knockaert, M., et al. 2002.Oncogene 21, 6413. Adachi, S., et al. 2001. Mol. Cell. Biol. 21, 4929. Knockaert, M., et al. 2000. Chem. Biol. 7, 411. Rosiana, G.R., et al. 1999. Proc. Natl. Acad. Sci. USA 96, 4797. Chang, Y.T., et al. 1999. Chem. Biol. 6, 361

Physical State :
Solid
Solubility :
Soluble in DMSO (100 mM), and methanol.
Storage :
Store at 4° C
Melting Point :
263.62° C (Predicted)
Boiling Point :
~639.0° C at 760 mmHg (Predicted)
Density :
1.41 g/cm3 (Predicted)
Refractive Index :
n20D 1.68 (Predicted)
IC50 :
CDK5/p35: IC50 = 20 nM; CDK2/cyclin E: IC50 = 28 nM; CDK1/cyclin B: IC50 = 33 nM; CDK2/cyclin A: IC50 = 33 nM; ERK 2: IC50 = 3.1 µM
pK Values :
pKb: 4.2 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
6604931
Beilstein Registry :
9293320
SMILES :
CC(C)C(CO)NC1=NC2=C(C(=N1)NC3=CC(=CC(=C3)N)Cl)N=CN2C(C)C

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Certificate of Analysis

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Rated 5 out of 5 by from Dobrikov et al Dobrikov et al. (PubMed ID 2428602) used aminopurvalanol A to inhibit Cdk1 and release HeLa cells from mitotic arrest. -SCBT Publication Review
Date published: 2015-05-06
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