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ONO-4059 (Synonyms: GS-4059 analog)

Catalog No.GC13219

ONO-4059 is the analog of ONO-4059, ONO-4059 is a highly potent and selective Btk inhibitor.

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ONO-4059 Chemical Structure

Cas No.: 1351635-67-0

Size Price Stock Qty
10mM (in 1mL DMSO)
$109.00
In stock
5mg
$99.00
In stock
10mg
$162.00
In stock
25mg
$288.00
In stock
50mg
$495.00
In stock
100mg
$715.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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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

Cas No. 1351635-67-0 SDF
Synonyms GS-4059 analog
Chemical Name (S)-9-(1-acryloylpiperidin-3-yl)-6-amino-7-(4-phenoxyphenyl)-7H-purin-8(9H)-one
Canonical SMILES NC1=C(N(C(N2[C@@H]3CN(C(C=C)=O)CCC3)=O)C(C=C4)=CC=C4OC5=CC=CC=C5)C2=NC=N1
Formula C25H24N6O3 M.Wt 456.5
Solubility DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:2): 0.3 mg/ml,Ethanol: 1 mg/ml Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.1906 mL 10.9529 mL 21.9058 mL
5 mM 0.4381 mL 2.1906 mL 4.3812 mL
10 mM 0.2191 mL 1.0953 mL 2.1906 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 19 reference(s) in Google Scholar.)

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