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| Size | Price | Stock |
|---|---|---|
| 250mg | $1200 | Check With Us |
| 500mg | $1800 | Check With Us |
| 1g | $2700 | Check With Us |
: Cat #: V0649 CAS #: 1351635-67-0 Purity ≥ 98%
Description: ONO-4059 analogue, an analogue of ONO-4059, is a novel, covalent, selective and orally bioavailable BTK inhibitor with potential anticancer and anti-inflammatory activity. It inhibits BTK with IC50 of 23.9 nM. ONO-4059 has demonstrated high antitumor activity in several pre-clinical models. It potently and dose-dependently reverse clinical arthritis and prevented bone damage in the CIA model. 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: [1]. Simon Rule,A Phase I Study Of The Oral Btk Inhibitor ONO-4059 In Patients With Relapsed/Refractory B-Cell Lymphoma. November 15, 2013; Blood: 122 (21)
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- Physicochemical and Storage Information
- Protocol
- Related Biological Data
- Stock Solution Preparation
- Quality Control Documentation
| Molecular Weight (MW) | 456.50 |
|---|---|
| Molecular Formula | C25H24N6O3 |
| CAS No. | 1351635-67-0 |
| Storage | -20℃ for 3 years in powder formrr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 20 mg/mL (43.8 mM)rr |
| Water: <1 mg/mLrr | |
| Ethanol: <1 mg/mL | |
| 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 |
| Protocol | 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. |
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| 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 |
| Related Biological Data |
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| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 2.1906 mL | 10.9529 mL | 21.9058 mL | 43.8116 mL |
| 5mM | 0.4381 mL | 2.1906 mL | 4.3812 mL | 8.7623 mL |
| 10mM | 0.2191 mL | 1.0953 mL | 2.1906 mL | 4.3812 mL |
| 20mM | 0.1095 mL | 0.5476 mL | 1.0953 mL | 2.1906 mL |
This equation is commonly abbreviated as: C1 V1 = C2 V2
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.