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ONO-4059 analogue
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
ONO-4059 analogue图片
CAS NO:1351635-67-0
规格:≥98%
包装与价格:
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

产品介绍
理化性质和储存条件
Molecular Weight (MW)456.50
FormulaC25H24N6O3
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 infoChemical 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
SynonymsONO 4059-Analog; ONO-4059-Analog; ONO-WG-307; ONO4059-Analog; GS 4059-Analog; GS-4059-Analog; GS4059-Analog.
实验参考方法
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 VivoFor 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 modelMouse tumor and CIA models
Formulation & DosageONO-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
ReferencesBlood. 2016 Jan 28;127(4):411-9.
生物活性


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.