product name ONO-4059 analogue
Description: ONO-4059 analogue is an novel analogue of ONO-4059, which is a highly potent and selective oral BTK inhibitor with IC50 of 23.9 nM. ONO-4059 inhibited the TMD-8 cell growth and Btk phosphorylation in a concentration-dependent manner. Furthermore, the decrease in Btk phosphorylation subsequently down-regulated Erk phosphorylation. After the combination of ONO-4059 with doxorubicin, etoposide, vincristine and dexamethasone, increased apoptosis ratio was observed, 25, 20, 17 and 29%, respectively.
References: Blood. 2016 Jan 28;127(4):411-9.
456.50
Formula
C25H24N6O3
CAS No.
1351635-67-0
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 20 mg/mL (43.8 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
ONO-WG-307
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19401416
| In Vitro |
In vitro activity: In TMD-8 cells, ONO-4059 inhibits cell growth with IC50 of 3.59 nM, and induces cell apoptosis. The combination of of ONO-4059 with doxorubicin, etoposide, vincristine or dexamethasone causes the increased apoptosis ratio. Kinase Assay: Cell Assay: ONO-4059 inhibited the TMD-8 cell growth and Btk phosphorylation in a concentration-dependent manner. Furthermore, the decrease in Btk phosphorylation subsequently down-regulated Erk phosphorylation. After the combination of ONO-4059 with doxorubicin, etoposide, vincristine and dexamethasone, increased apoptosis ratio was observed, 25, 20, 17 and 29%, respectively. |
|---|---|
| In Vivo | For the 100-200 mm3 tumour groups, tumour growth inhibition at the final treatment day was 23% in QD, 72.9% in BD and 100% in dose mixed in food, groups respectively. For the 400-450 mm3 tumour groups, no growth inhibition was observed in the QD group and, growth inhibitions of 27.5% in BD and 100% in dose mixed in food were observed. The PK concentration and phosphorylated Btk inhibition levels of those animals whose dose was mixed in with food were higher than that of other treatment groups. |
| Animal model | |
| Formulation & Dosage | |
| References | Blood. 2016 Jan 28;127(4):411-9. |
Related Posts
product name ONO-4059 analogue
Description: ONO-4059 analogue is an novel analogue of ONO-4059, which is a highly potent and selective oral BTK inhibitor with IC50 of 23.9 nM. ONO-4059 inhibited the TMD-8 cell growth and Btk phosphorylation in a concentration-dependent manner. Furthermore, the decrease in Btk phosphorylation subsequently down-regulated Erk phosphorylation. After the combination of ONO-4059 with doxorubicin, etoposide, vincristine and dexamethasone, increased apoptosis ratio was observed, 25, 20, 17 and 29%, respectively.
References: Blood. 2016 Jan 28;127(4):411-9.
456.50
Formula
C25H24N6O3
CAS No.
1351635-67-0
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 20 mg/mL (43.8 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
ONO-WG-307
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19401416
| In Vitro |
In vitro activity: In TMD-8 cells, ONO-4059 inhibits cell growth with IC50 of 3.59 nM, and induces cell apoptosis. The combination of of ONO-4059 with doxorubicin, etoposide, vincristine or dexamethasone causes the increased apoptosis ratio. Kinase Assay: Cell Assay: ONO-4059 inhibited the TMD-8 cell growth and Btk phosphorylation in a concentration-dependent manner. Furthermore, the decrease in Btk phosphorylation subsequently down-regulated Erk phosphorylation. After the combination of ONO-4059 with doxorubicin, etoposide, vincristine and dexamethasone, increased apoptosis ratio was observed, 25, 20, 17 and 29%, respectively. |
|---|---|
| In Vivo | For the 100-200 mm3 tumour groups, tumour growth inhibition at the final treatment day was 23% in QD, 72.9% in BD and 100% in dose mixed in food, groups respectively. For the 400-450 mm3 tumour groups, no growth inhibition was observed in the QD group and, growth inhibitions of 27.5% in BD and 100% in dose mixed in food were observed. The PK concentration and phosphorylated Btk inhibition levels of those animals whose dose was mixed in with food were higher than that of other treatment groups. |
| Animal model | |
| Formulation & Dosage | |
| References | Blood. 2016 Jan 28;127(4):411-9. |