Btk Kinase inhibitor
- CAS No.
- 1351636-18-4
- Chemical Name:
- Btk Kinase inhibitor
- Synonyms
- ONO-BKT;ONO BTK;Tirabrutinib;TIRABRUTINIB;GS-4059;Btk Kinase inhibitor;ONO-4059(Tirabrutinib);Tirabrutinib free base;Isoleucine Impurity 18;Tirabrutinib (ONO-4059);ONO-4059;ONO 4059;ONO4059
- CBNumber:
- CB02716154
- Molecular Formula:
- C25H22N6O3
- Molecular Weight:
- 454.48
- MOL File:
- 1351636-18-4.mol
- Modify Date:
- 2024/11/19 15:53:33
| Boiling point | 672.0±65.0 °C(Predicted) |
|---|---|
| Density | 1.412±0.06 g/cm3(Predicted) |
| storage temp. | Store at -20°C |
| solubility |
DMSO:65.0(Max Conc. mg/mL);143.02(Max Conc. mM) DMSO:PBS (pH 7.2) (1:2):0.3(Max Conc. mg/mL);0.66(Max Conc. mM) DMF:30.0(Max Conc. mg/mL);66.01(Max Conc. mM) Ethanol:1.0(Max Conc. mg/mL);2.2(Max Conc. mM) |
| form | A crystalline solid |
| pka | 3.16±0.20(Predicted) |
| color | White to yellow |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Warning | |||||||||
| Hazard statements | H302-H315-H319-H335 | |||||||||
| Precautionary statements | P261-P264-P270-P271-P280-P301+P312-P330-P302+P352-P321-P304+P340-P305+P351+P338-P332+P313-P362+P364-P337+P313-P403+P233-P405-P501 | |||||||||
| NFPA 704 |
|
Btk Kinase inhibitor Chemical Properties,Uses,Production
Description
Btk Kinase inhibitor is highly potent and selective orally administered, small molecule, and also named tirabrutinib, Brutons tyrosine kinase (BTK) inhibitor being developed by Ono pharmaceutical and its licensee Gilead Sciences for the treatment of autoimmune disorders and haematological malignancies.
brand name
VelexbruTM
Biological Functions
In March 2020, tirabrutinib was approved in Japan to treat primary central nervous system lymphoma (PCNSL). Tirabrutinib shows excellent selectivity against all kinases with cysteines in the ATP-binding site corresponding to Cys481 in BTK with the exception of BMX, TXK, and TEC? However, it displays weaker BTK inhibition than ibrutinib (IC50 = 6.8 nM vs. 0.47 nM).
General Description
Class: non-receptor tyrosine kinase
Treatment: PCNSL
Elimination half-life = 6.5–8 h
Protein binding = 91%
Mechanism of action
The selective inhibition of cell growth by Btk Kinase inhibitor was due to blocking of BTK-mediated signaling through AKT and cellular protein kinase D. It can inhibit autophosphorylation of the BTK at the Tyr223 position through the ERK, AKT and PKD signaling pathways.
Side effects
Adverse effects of the Btk Kinase inhibitor that occurred in some patients were rash, vomiting, neutropenia, arthralgia, and malaise, and drug-related Grade 3–4 Adverse effects were neutropenia, leukopenia, anemia, hypophosphatemia, PT-INR increased, pneumonitis, and acute myeloid leukemia. in prior Japanese studies, rash, hematologic adverse effects, erythema multiforme, and constipation were frequent adverse effects in a Phase I/II study of some patients with PCNSL, and rash, hematologic adverse effects, and stomatitis were the most common adverse effects in a Phase II study of some patients with WM.
target
BTK
Btk Kinase inhibitor Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | Inquiry |
|---|---|---|---|---|---|
| A.J Chemicals | 91-9810153283 | New Delhi, India | 6100 | 58 | Inquiry |
| Amadis Chemical Company Limited | 571-89925085 | China | 131957 | 58 | Inquiry |
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | China | 33024 | 60 | Inquiry |
| Zhejiang ZETian Fine Chemicals Co. LTD | +8618957127338 | China | 2136 | 58 | Inquiry |
| BOC Sciences | +1-631-485-4226 | United States | 19552 | 58 | Inquiry |
| career henan chemical co | +86-0371-86658258 +8613203830695 | China | 29808 | 58 | Inquiry |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | China | 10473 | 58 | Inquiry |
| InvivoChem | +1-708-310-1919 +1-13798911105 | United States | 6391 | 58 | Inquiry |
| TargetMol Chemicals Inc. | United States | 38636 | 58 | Inquiry | |
| ShenZhen Trendseen Biological Technology Co.,Ltd. | 13417589054 | China | 11681 | 58 | Inquiry |
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