[CAS NO. 1202757-89-8] Spebrutinib (CC-292)
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PRODUCTS SPECIFICATIONS [1202757-89-8]
Store
Catalog
SLK-S7173
Brand
Selleck
CAS
1202757-89-8
DESCRIPTION [1202757-89-8]
Overview
| MDL | MFCD25976876 |
|---|---|
| Molecular Weight | 423.44 |
| Molecular Formula | C22H22FN5O3 |
| SMILES | C=CC(NC1=CC=CC(NC2=NC(NC3=CC=C(OCCOC)C=C3)=NC=C2F)=C1)=O |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3616 mL | 11.8080 mL | 23.6161 mL |
| 5 mM | 0.4723 mL | 2.3616 mL | 4.7232 mL |
| 10 mM | 0.2362 mL | 1.1808 mL | 2.3616 mL |
| 50 mM | 0.0472 mL | 0.2362 mL | 0.4723 mL |
Description
Spebrutinib (CC-292, AVL-292) is a covalent, orally active, and highly selective inhibitor with of <0.5 nM, displaying at least 1400-fold selectivity over the other kinases assayed. Phase 1.
Features
Orally bioavailable BTK-selective inhibitor that has been tested in Phase I clinical trials for treatment of relapsed or refractory B-NHL, CLL and WM.
Targets
| BTK [1] (Cell-free assay) |
| <0.5 nM |
In vitro
AVL-292 exhibits dose-dependent inhibition of Btk with EC50 of 8 nM and downstream BCR signaling components in Ramos cells. AVL-292, by inhibiting BTK activities, further inhibits B cell proliferation with EC50 of 3 nM.
In vivo
In a collagen-induced arthritis mouse model, AVL-292 (3- 30 mg/kg, p.o.) dose-dependently inhibits the clinical signs of inflammatory disease, including reduction in joint and paw swelling and visible redness of the affected paws.
References
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