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Purity: ≥98%
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.
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References |
Blood.2016Jan 28;127(4):411-9.
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Molecular Formula |
C25H24N6O3
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Molecular Weight |
456.50
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CAS # |
1351635-67-0
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Related CAS # |
Tirabrutinib;1351636-18-4;Tirabrutinib hydrochloride;1439901-97-9
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SMILES |
O=C1N([C@H]2CCCN(C(C=C)=O)C2)C3=NC=NC(N)=C3N1C4=CC=C(OC5=CC=CC=C5)C=C4
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InChi Key |
KSUDUUBCXJUFRL-SFHVURJKSA-N
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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
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Chemical Name |
(S)-9-(1-acryloylpiperidin-3-yl)-6-amino-7-(4-phenoxyphenyl)-7,9-dihydro-8H-purin-8-one
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Synonyms |
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(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.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT03100942 | Completed | Drug: Lanraplenib Drug: Filgotinib |
Sjogren's Syndrome | Gilead Sciences | May 1, 2017 | Phase 2 |
NCT02626026 | Completed | Drug: Tirabrutinib Drug: Placebo |
Rheumatoid Arthritis | Gilead Sciences | January 26, 2016 | Phase 1 |
PFS curves for CLL, MCL, and DLBCL patients. Results are shown for CLL, MCL, and DLBCL patients as separate curves. Estimated mean PFS for each cohort: CLL = 874 days, MCL = 341 days, and DLBCL = 54 days. Blood.2016Jan 28;127(4):411-9. td> |
Efficacy of ONO/GS-4059 in patients with CLL. (A) Duration on treatment for all CLL patients (n = 28) according to dose cohort. *Ongoing patients. (B) Waterfall plot for all CLL patients by dose cohort (n = 25), showing response evaluated by CT imaging. Changes from baseline scan (sum of the largest diameter of each target lesion) are shown. Negative values indicate tumor response. **Patients with TP53/17p deletion; @patients with ATM/11q deletion. (C) Rate of response of lymph nodes in CLL patients up to cycle 7 (n = 23). Measured by the percentage change in tumor SPD. (D) Mean blood concentrations of hemoglobin (g/dL) and platelet count (×109/L) showing recovery of normal hemopoiesis in CLL patients up to cycle 31. (E) Case example: CT axial images from a CLL patient. (i) Pretreatment CT imaging showing large volume intra-abdominal lymphadenopathy. (ii) CT imaging during cycle 3 following treatment with ONO/GS-4059 600 mg once daily shows considerable reduction in lymphadenopathy. SPD, sum of perpendicular dimensions. Blood.2016Jan 28;127(4):411-9. td> |
Efficacy of ONO/GS-4059 in patients with DLBCL. (A) Waterfall plot for all DLBCL patients by dose cohort (n = 17), showing response evaluated by CT imaging. Changes from baseline scan (sum of the largest diameter of each target lesion) are shown. Negative values indicate tumor response. (B) Duration on treatment for all DLBCL patients (n = 35) according to dose cohort. *Ongoing patients. Blood.2016Jan 28;127(4):411-9. td> |