| CAS NO: | 1351635-67-0 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| Molecular Weight (MW) | 456.50 |
|---|---|
| Formula | C25H24N6O3 |
| CAS No. | 1351635-67-0 (ONO-4059-analog); |
| 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 | |
| Other info | Chemical Name: (S)-9-(1-acryloylpiperidin-3-yl)-6-amino-7-(4-phenoxyphenyl)-7,9-dihydro-8H-purin-8-one InChi Key: KSUDUUBCXJUFRL-SFHVURJKSA-N InChi Code: InChI=1S/C25H24N6O3/c1-2-21(32)29-14-6-7-18(15-29)31-24-22(23(26)27-16-28-24)30(25(31)33)17-10-12-20(13-11-17)34-19-8-4-3-5-9-19/h2-5,8-13,16,18H,1,6-7,14-15H2,(H2,26,27,28)/t18-/m0/s1 SMILES Code: O=C1N(C2=CC=C(C=C2)OC3=CC=CC=C3)C4=C(N)N=CN=C4N1[C@@H]5CN(C(C=C)=O)CCC5 |
| Synonyms | ONO 4059-Analog; ONO-4059-Analog; ONO-WG-307; ONO4059-Analog; GS 4059-Analog; GS-4059-Analog; GS4059-Analog. |
| 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: ONO-4059 analog is the analog of ONO-4059, ONO-4059 is a highly potent and selective Btk inhibitor. IC50 value: sub-nM range. 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 | Mouse tumor and CIA models |
| Formulation & Dosage | ONO-4059 has demonstrated anti-tumour activity in several pre-clinical models. ONO-4059 potently and dose-dependently reverse clinical arthritis and prevented bone damage in the CIA model |
| References | Blood. 2016 Jan 28;127(4):411-9. |
Efficacy of ONO/GS-4059 in patients with DLBCL. Blood. 2016 Jan 28;127(4):411-9. |
Efficacy of ONO/GS-4059 in patients with CLL. Blood. 2016 Jan 28;127(4):411-9. |
Efficacy of ONO/GS-4059 in patients with MCL. Blood. 2016 Jan 28;127(4):411-9. |
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