PURVALANOL A
Synonym(s):2-(1R-Isopropyl-2-hydroxyethylamino)-6-(3-chloroanilino)-9-isopropylpurine;2-(1R-Isopropyl-2-hydroxyethylamino)-6-(3-chloroanilino)-9-isopropyl-purine;NG-60;Purvalanol A - CAS 212844-53-6 - Calbiochem
- CAS NO.:212844-53-6
- Empirical Formula: C19H25ClN6O
- Molecular Weight: 388.89
- MDL number: MFCD02179211
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-11-19 23:02:33
What is PURVALANOL A?
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.
The Uses of PURVALANOL A
Purvalanol A acts as a potent, cell-permeable CDK inhibitor used in the treatment of cell proliferative disorders. Anti-cancer.
What are the applications of Application
Purvalanol A is a selective inhibitor of cyclin-dependent kinases
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
Properties of PURVALANOL A
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 |
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. |
Safety information for PURVALANOL A
Signal word | Warning |
Pictogram(s) |
Exclamation Mark Irritant GHS07 |
GHS Hazard Statements |
H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation H335:Specific target organ toxicity, single exposure;Respiratory tract irritation |
Precautionary Statement Codes |
P261:Avoid breathing dust/fume/gas/mist/vapours/spray. P271:Use only outdoors or in a well-ventilated area. P280:Wear protective gloves/protective clothing/eye protection/face protection. |
Computed Descriptors for PURVALANOL A
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