Aminopurvalanol A CAS: 220792-57-4
MF: C19H26ClN7O
MW: 403.91
A reversible and ATP-competitive inhibitor of Cdks.

Aminopurvalanol A (CAS 220792-57-4)

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Aminopurvalanol A is rated 5.0 out of 5 by 1.
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Alternate Names: (2R)-2-((6-((3-Amino-5-chlorophenyl)amino)-9-(1-methylethyl)-9H-purin-2-yl)amino)-3-methyl-1-butanol; NG-97
Application Aminopurvalanol A is a reversible and ATP-competitive inhibitor of Cdks
CAS 등록번호: 220792-57-4
분자량: 403.91
분자식: C19H26ClN7O
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* 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
용해도 :
Soluble in DMSO (100 mM), and methanol.
저장 :
Store at 4° C
녹는점 :
263.62° C (Predicted)
비등점 :
~639.0° C at 760 mmHg (Predicted)
밀도 :
1.41 g/cm3 (Predicted)
굴절률 :
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 :
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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