Orelabrutinib
- CAS NO.:1655504-04-3
- Empirical Formula: C26H25N3O3
- Molecular Weight: 427.49
- MDL number: MFCD32184857
- Update Date: 2024-11-18 17:01:59
What is Orelabrutinib ?
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.
The Uses of Orelabrutinib
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.
Properties of Orelabrutinib
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 |
Safety information for Orelabrutinib
Signal word | Warning |
Pictogram(s) |
Exclamation Mark Irritant GHS07 |
GHS Hazard Statements |
H302:Acute toxicity,oral H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation H335:Specific target organ toxicity, single exposure;Respiratory tract irritation |
Precautionary Statement Codes |
P261:Avoid breathing dust/fume/gas/mist/vapours/spray. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing. |
Computed Descriptors for Orelabrutinib
New Products
4-Aminotetrahydropyran-4-carbonitrile Hydrochloride (R)-3-Aminobutanenitrile Hydrochloride 4-AMINO-TETRAHYDRO-PYRAN-4-CARBOXYLIC ACID HCL 4-(Dimethylamino)tetrahydro-2H-pyran-4-carbonitrile 3-((Dimethylamino)methyl)-5-methylhexan-2-one oxalate 1,4-Dioxa-8-azaspiro[4.5]decane 5-Bromo-2-nitropyridine Nimesulide BP Aceclofenac IP/BP/EP Diclofenac Sodium IP/BP/EP/USP Mefenamic Acid IP/BP/EP/USP Ornidazole IP Diclofenac Potassium SODIUM AAS SOLUTION ZINC AAS SOLUTION BUFFER SOLUTION PH 10.0(BORATE) GOOCH CRUCIBLE SINTERED AQUANIL 5 BERYLLIUM AAS SOLUTION 2-Bromo-1-(bromomethyl)-3-chloro-5-nitrobenzene 2-Bromo-3-nitroaniline N-(3-Hydroxypropyl)-N-methylacetamide 3-Bromo-6-chloropyridazine 4-ethyl-3-nitrobenzoic acidRelated products of tetrahydrofuran
You may like
-
1-Methyl-6-oxo-1,6-dihydropyridazine-3-carbonitrile 98%View Details
99903-60-3 -
88491-46-7 98%View Details
88491-46-7 -
1823368-42-8 98%View Details
1823368-42-8 -
2-(3-(tert-butyl)phenoxy)-2-methylpropanoic acid 1307449-08-6 98%View Details
1307449-08-6 -
Ethyl 3-(furan-2-yl)-3-hydroxypropanoate 25408-95-1 98%View Details
25408-95-1 -
2-Chloro-5-fluoro-1-methoxy-3-methylbenzene 98%View Details
1805639-70-6 -
1784294-80-9 98%View Details
1784294-80-9 -
Lithium ClavulanateView Details
61177-44-4