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ONO-4059

Catalog No.
B5941
Btk抑制剂
组合的产品项目
规格价格库存 数量
5mg
¥ 1,320.00
Ship with 10-15 days
10mg
¥ 2,160.00
Ship with 10-15 days
25mg
¥ 3,840.00
Ship with 10-15 days
50mg
¥ 6,600.00
Ship with 10-15 days
100mg
¥ 9,528.00
Ship with 10-15 days

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邮箱: sales@apexbio.cn

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Background

Description:

IC50: 2.2 nM for Btk kinase activity

Bruton’s tyrosine kinase (Btk) is a key regulator of the B-cell receptor (BCR) pathway and abberant BCR signaling has been implicated in the survival of malignant B-cells. Previous studies indicate that targeting Btk is effective in the treatment of B-cell malignancies. ONO-4059 is a highly potent and selective oral Btk inhibitor.

In vitro: 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 [1].

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 [2].

Clinical trial: ONO-4059 is a highly potent and selective oral Btk inhibitor that shows a favourable safety profile along with promising efficacy in this difficult-to-treat patient population with relapsed/refractory B-Cell lymphoma [3].

Reference:
[1] Tomoko Yasuhiro, Toshio Yoshizawa, Joseph TP Birkett, and Kazuhito Kawabata.  ONO-4059, A Novel Bruton’s Tyrosine Kinase (Btk) Inhibitor: Synergistic Activity In Combination With Chemotherapy In a ABC-DLBCL Cell Line. 2013; Blood: 122 (21): 5151 - 5151
[2] Toshio Yoshizawa, Tomoko Yasuhiro, Hideyuki Honda, and Kazuhito Kawabata.  ONO-4059—a Potent and Selective Reversible Bruton’s Tyrosine Kinase (Btk) Inhibitor: Single Agent, Twice Daily (BD) Dosing and Dosing with Food Results in Sustained, High Trough Levels of ONO-4059, Translating into 100% Tumour Remission in a TMD-8 Xenograft Model. 2014; Blood: 124 (21) 4502 - 4502
[3] Simon Rule, Nimish Shah, Gilles Andre Salles et al.  A Phase I Study Of The Oral Btk Inhibitor ONO-4059 In Patients With Relapsed/Refractory B-Cell Lymphoma. Blood. 2013 122 (21): 4397 – 4397.

Chemical Properties

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt456.5
Cas No.1351635-67-0
FormulaC25H24N6O3
SolubilitySoluble in DMSO
Chemical Name(S)-9-(1-acryloylpiperidin-3-yl)-6-amino-7-(4-phenoxyphenyl)-7H-purin-8(9H)-one
SDFDownload SDF
Canonical SMILESNC1=C(N(C(N2[C@@H]3CN(C(C=C)=O)CCC3)=O)C(C=C4)=CC=C4OC5=CC=CC=C5)C2=NC=N1
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

质量控制

质量控制和MSDS

批次:

化学结构

ONO-4059