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- Reiko Watanabe, .et al. Development of an In Silico Prediction Model for P-glycoprotein Efflux Potential in Brain Capillary Endothelial Cells toward the Prediction of Brain Penetration, J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
- Vimal Pandey, .et al. Roscovitine effectively enhances antitumor activity of temozolomide in vitro and in vivo mediated by increased autophagy and Caspase-3 dependent apoptosis, Scientific Reports, 2019, 9, Article number: 5012 PMID: 30899038
Biological Activity
Roscovitine (Seliciclib) is a CDK inhibitor that preferentially inhibit multiple enzyme targets including CDK2, CDK7 and CDK9.
Targets
Target | Value |
---|---|
CDK5/p35 | IC50: 0.16μM |
Cdc2/CyclinB | IC50: 0.65μM |
CDK2/CyclinA | IC50: 0.7μM |
CDK2/CyclinE | IC50: 0.7μM |
ERK2 | IC50: 14μM |
GST-ERK1 | IC50: 30μM |
ERK1 | IC50: 34μM |
CDK4/CyclinD1 | IC50: >100μM |
CDK6/CyclinD3 | IC50: >100μM |
PKCα | IC50: >100μM |
PKCβ1 | IC50: >100μM |
PKCβ2 | IC50: >100μM |
PKCγ | IC50: 100μM |
PKCε | IC50: >100μM |
PKCη | IC50: >100μM |
c-Src | IC50: 250μM |
PKCδ | IC50: >1000μM |
PKCζ | IC50: >1000μM |
v-Abl | IC50: >1000μM |
In vitro (25°C) | DMSO | 69 mg/mL (194.67 mM) | |
Water | Insoluble | ||
Ethanol | 6 mg/mL (16.92 mM) | ||
In vivo | 1% DMSO+10% Tween 80+20% N-N-dimethylacetamide+69% PEG 400 | 4 mg/mL | |
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
0.1 mM | 28.21 mL | 141.04 mL | 282.09 mL |
0.5 mM | 5.64 mL | 28.21 mL | 56.42 mL |
1 mM | 2.82 mL | 14.1 mL | 28.21 mL |
5 mM | 0.56 mL | 2.82 mL | 5.64 mL |
*The above data is based on the productmolecular weight 354.5 . Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
Catalog Num | A10806 |
---|---|
Actions | Inhibitor |
CAS No. | 186692-46-6 |
Formula | C19H26N6O |
M. Wt | 354.5 |
Purity | >98% |
Synonyms | CYC202, Seliciclib |
SMILES | CC[C@H](CO)NC1=NC2=C(C(=N1)NCC3=CC=CC=C3)N=CN2C(C)C |
Storage | Store lyophilized at -20ºC, keep desiccated. |
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