Orelabrutinib
- Product Name
- Orelabrutinib
- CAS No.
- 1655504-04-3
- Chemical Name
- Orelabrutinib
- Synonyms
- ICP-022;Orelabrutinib;Orelabrutinib USP/EP/BP;Orelabrutinib (ICP-022);6-(1-Acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)nicotinamide;:6-[1-(1-oxo-2-propen-1-yl)-4-piperidinyl]-2-(4-phenoxyphenyl)-3-Pyridinecarboxamide;3-Pyridinecarboxamide, 6-[1-(1-oxo-2-propen-1-yl)-4-piperidinyl]-2-(4-phenoxyphenyl)-;Malignancies,Btk,ICP 022,inhibit,antineoplastic,Inhibitor,chronic,small,Bruton tyrosine kinase,lymphocytic leukemia,cell,Orelabrutinib,ICP022
- CBNumber
- CB03369553
- Molecular Formula
- C26H25N3O3
- Formula Weight
- 427.49
- MOL File
- 1655504-04-3.mol
Orelabrutinib Property
- Boiling point:
- 646.3±55.0 °C(Predicted)
- Density
- 1.213±0.06 g/cm3(Predicted)
- form
- Solid
- pka
- 14.80±0.50(Predicted)
- color
- White to off-white
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- CS-0105163
- Product name
- Orelabrutinib
- Purity
- 98.93%
- Packaging
- 5mg
- Price
- $300
- Updated
- 2021/12/16
- Product number
- CS-0105163
- Product name
- Orelabrutinib
- Purity
- 98.93%
- Packaging
- 10mg
- Price
- $450
- Updated
- 2021/12/16
- Product number
- CS-0105163
- Product name
- Orelabrutinib
- Purity
- 98.93%
- Packaging
- 50mg
- Price
- $1200
- Updated
- 2021/12/16
- Product number
- CS-0105163
- Product name
- Orelabrutinib
- Purity
- 98.93%
- Packaging
- 100mg
- Price
- $1800
- Updated
- 2021/12/16
Orelabrutinib Chemical Properties,Usage,Production
Description
Orelabrutinib is a small molecule inhibitor of Bruton's tyrosine kinase with potential antineoplastic activity.
Description
In December 2020, orelabrutinib was approved by the China National Medical Products Administration for treating patients with relapsed/refractory MCL, CLL, and SLL. This compound is also being evaluated for the treatment of multiple sclerosis. Orelabrutinib, which has a unique pyridylcarboxamide hinge binder, showed an IC50 value of 1.6 nM in the BTK enzymatic assay. When tested against a panel of 456 kinases at 1 μM, orelabrutinib only inhibited BTK (>90%), while ibrutinib also targeted several other kinases, including EGFR, TEC, and BMX. Orelabrutinib has a favorable half-life of 4 h in healthy volunteers.1,2 It is administered orally at a daily dose of 150 mg.
Uses
Orelabrutinib has been previously approved to treat patients with relapsed or refractory (R/R) mantle cell lymphoma and R/R chronic lymphocytic leukemia/small lymphocytic lymphoma.
brand name
InnobrukaTM
General Description
Class: non-receptor tyrosine kinase
Treatment: CLL, SLL, MCL
Elimination half-life = 4 h
Protein binding = not reported
Biological Activity
Orelabrutinib (ICP-022) is a potent, orally active and irreversible inhibitor of Bruton's tyrosine kinase (BTK).
Mechanism of action
Upon administration, orelabrutinib binds to and inhibits the activity of BTK. This prevents both the activation of the B-cell antigen receptor (BCR) signaling pathway and BTK-mediated activation of downstream survival pathways, inhibiting the growth of malignant B-cells that overexpress BTK.
target
| Target | Value |
| BTK () |