| Identification | Back Directory | [Name]
PURVALANOL A | [CAS]
212844-53-6 | [Synonyms]
NG-60
PurvaL
CH61386
CS-1631
CDKinhibitor
PURVALANOL A
(R)-Purvalanol A
NG 60;NG60;NG-60
PURVALANOLA, >98%
PurvalanolA/CH61386
Purvalanol A(NG 60)
PURVALANOL A USP/EP/BP
PurvalanolA,CDKinhibitor
Purvalanol A - CAS 212844-53-6 - Calbiochem
6-(3-CHLOROANILINO)-2(1R)-ISOPROPYL-2-HYDROXYETHYLAMINO-9-ISOPROPYLPURINE
2-(1R-ISOPROPOYL-2-HYDROXYETHYLAMINO)-6-(3-CHLOROANILINO)-9-ISOPROPYLPURINE
2-(1R-ISOPROPYL-2-HYDROXYETHYLAMINO)-6-(3-CHLOROANILINO)-9-ISOPROPYL-PURINE
(2R)-2-[[6-(3-chloroanilino)-9-propan-2-ylpurin-2-yl]amino]-3-methylbutan-1-ol
(R)-2-(6-(3-chlorophenylamino)-9-isopropyl-9H-purin-2-ylamino)-3-methylbutan-1-ol
NG-60, 2-(1R-Isopropyl-2-hydroxyethylamino)-6-(3-chloroanilino)-9-isopropylpurine
(2R)-2-[[6-[(3-CHLOROPHENYL)AMINO]-9-(1-METHYLETHYL)-9H-PURIN-2-YL]AMINO]-3-METHYL-1-BUTANOL
1-Butanol, 2-[[6-[(3-chlorophenyl)amino]-9-(1-methylethyl)-9H-purin-2-yl]amino]-3-methyl-, (2R)-
2R)-2-[[6-[(3-Chlorophenyl)amino]-9-(1-methylethyl)-9H-purin-2-yl]amino]-3-methyl-1-butanolCDKinhibitor. | [Molecular Formula]
C19H25ClN6O | [MDL Number]
MFCD02179211 | [MOL File]
212844-53-6.mol | [Molecular Weight]
388.89 |
| Chemical Properties | Back Directory | [Boiling point ]
590.5±60.0 °C(Predicted) | [density ]
1.33±0.1 g/cm3(Predicted) | [storage temp. ]
−20°C
| [solubility ]
methylene chloride: 50 mg/mL, clear, colorless
| [form ]
powder
| [pka]
14.51±0.10(Predicted) | [color ]
off-white
| [Stability:]
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months. |
| Hazard Information | Back Directory | [Description]
Purvalanol A (212844-53-6) is a cyclin-dependent kinase inhibitor. IC50s= 4, 70, 35, 75 and 850 nM for cdc2/cyclin B, cdk2/cyclin A, cdk2/cyclin E, cdk5/p35 and cdk4/cyclin D1 and respectively.1?Reversibly arrests synchronized cells in G1 and G2 phase.2?Induces ER stress-mediated apoptosis and autophagy in colon cancer cells.3?Suppresses Src-mediated transformation by inhibiting both CDKs and c-Src.4?In cells transformed with MYC, purvalanol A rapidly down-regulates survivin expression and induces MYC-dependent apoptosis.5?Cell permeable. | [Uses]
Inhibitor of human CDK1 (IC50=4nM), CDK2/cyclin A (IC50=70nM), Cdc2/cyclin B, CDK2/cyclin E (IC50=35nM), CDK4/cyclin D1 (IC50=850nM) as well as CDK5/p35 (IC50=75nM). More membrane permeable than purvalanol B. | [Definition]
ChEBI: Purvalanol A is a purvalanol. | [Biological Activity]
Cyclin-dependent kinase inhibitor. IC 50 values are 4, 70, 35, 850 and 75 nM for cdc2/cyclin B, cdk2/cyclin A, cdk2/cyclin E, cdk4/cyclin D1 and cdk5-p35 respectively. Reversibly arrests synchronised cells in G1 and G2, and inhibits cell proliferation and cell death. | [storage]
Store at +4°C | [References]
1) Gray?et al.?(1998),?Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors; Science,?281?533
2) Villerbu?et al.?(2002),?Cellular effects of purvalanol A: a specific inhibitor of cyclin-dependent kinase activities; Int. J. Cancer,?97?761
3) Coker-Gurkan?et al.?(2015),?Purvalanol induces endoplasmic reticulum stress-mediated apoptosis and autophagy in a time dependent manner in HCT116 colon cancer cells; Oncol. Rep.,?33?2761
4) Hikita?et al.?(2010),?Purvalanol A, a CDK inhibitor, effectively suppresses Src-mediated transformation by inhibiting both CDKs and c-Src; Genes Cells,?15?1051
5) Goga?et al.?(2007),?Inhibition of CDK1 as a potential therapy for tumors over-expressing MYC; Nat. Med.,?13?820 |
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