PURVALANOL A

PURVALANOL A Basic information
Product Name:PURVALANOL A
Synonyms:PURVALANOL A;NG-60;6-(3-CHLOROANILINO)-2(1R)-ISOPROPYL-2-HYDROXYETHYLAMINO-9-ISOPROPYLPURINE;(2R)-2-[[6-[(3-CHLOROPHENYL)AMINO]-9-(1-METHYLETHYL)-9H-PURIN-2-YL]AMINO]-3-METHYL-1-BUTANOL;2-(1R-ISOPROPOYL-2-HYDROXYETHYLAMINO)-6-(3-CHLOROANILINO)-9-ISOPROPYLPURINE;2-(1R-ISOPROPYL-2-HYDROXYETHYLAMINO)-6-(3-CHLOROANILINO)-9-ISOPROPYL-PURINE;CH61386;2R)-2-[[6-[(3-Chlorophenyl)amino]-9-(1-methylethyl)-9H-purin-2-yl]amino]-3-methyl-1-butanolCDKinhibitor.
CAS:212844-53-6
MF:C19H25ClN6O
MW:388.89
EINECS:
Product Categories:Inhibitors;Signalling
Mol File:212844-53-6.mol
PURVALANOL A Structure
PURVALANOL A Chemical Properties
Boiling point 590.5±60.0 °C(Predicted)
density 1.33±0.1 g/cm3(Predicted)
storage temp. Keep in dark place,Inert atmosphere,Store in freezer, under -20°C
solubility methylene chloride: 50 mg/mL, clear, colorless
form powder
pka14.51±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.
Safety Information
WGK Germany 3
HS Code 2933599590
MSDS Information
ProviderLanguage
SigmaAldrich English
PURVALANOL A Usage And Synthesis
DescriptionPurvalanol 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.
UsesPurvalanol A acts as a potent, cell-permeable CDK inhibitor used in the treatment of cell proliferative disorders. Anti-cancer.
DefinitionChEBI: Purvalanol A is a purvalanol.
Biological ActivityCyclin-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.
storageStore at +4°C
References1) 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
PURVALANOL A Preparation Products And Raw materials
OLOMOUCINE ROSCOVITINE NU6102 PURVALANOL B SU 9516 AMINOPURVALANOL A OLOMOUCINE II 2(BIS-(HYDROXYETHYL)AMINO)-6-(4-METHOXYBENZYLAMINO)-9-ISOPROPYL-PURINE ARCYRIAFLAVIN A 3-amino-10H-acridine-9-thione NU6140 (S)-ROSCOVITINE QNZ (EVP4593) N9-ISOPROPYL-OLOMOUCINE Ro 3306 6-ANILINOPURINE 2-Aminopurine PURVALANOL A

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