164640

Sigma-Aldrich

Aminopurvalanol A - CAS 220792-57-4 - Calbiochem

A cell-permeable 2,6,9-trisubstituted purine analog that displays anti-mitotic as well as anti-tumor properties.

Synonym(s):
(2R)-2-((6-((3-Amino-5-chlorophenyl)amino)-9-(1-methylethyl)-9H-purin-2-yl)amino)-3-methyl-1-butanol, NG-97, Aminopurvalanol A - CAS 220792-57-4 - Calbiochem
Empirical Formula (Hill Notation):
C19H26ClN7O
CAS Number:
Molecular Weight:
403.91
Pricing and availability is not currently available.

storage conditions

+2C to +8C

Quality Level

assay

≥98% (HPLC)

form

solid

mfr. no.

Calbiochem®

storage condition

OK to freeze
protect from light

color

pale yellow

solubility

DMSO: 40 mg/mL

shipped in

ambient

General description

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). Acts as a reversible and ATP-competitive inhibitor of Cdks (IC50 = 33 nM for 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). Shown to induce cell differentiation by preferentially targeting the G2/M-phase and act intracellularly by inhibiting both Cdks and MAPKs.
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). Acts as a reversible and ATP-competitive inhibitor of Cdks (IC50 = 33 nM for 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). Shown to induce cell differentiation by preferentially targeting the G2/M-phase and act intracellularly by inhibiting both Cdks and MAPKs.

Packaging

5 mg in Plastic ampoule
Packaged under inert gas

Biochem/physiol Actions

Reversible: yes
Primary Target
Cdk1/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E, and Cdk5/p35
Cell permeable: yes
Product competes with ATP.
Target IC50: 33 nM for Cdk1/cyclin B and Cdk2/cyclin A, 28 nM for Cdk2/cyclin E, and 20 nM for Cdk5/p35

Warning

Toxicity: Irritant (B)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Breton, M.L., et al. 2003. Biochem. Biophys. Res. Commun.306, 880.
Knockaert, M., et al. 2002.Oncogene21, 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. USA96, 4797.
Chang, Y.T., et al. 1999. Chem. Biol.6, 361.

Legal Information

Sold under license of U.S. Patent 6,255,485 and 6,617,331.
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