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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Other Sizes |
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Purity: ≥98%
Spebrutinib (formerly AVL-292; CC-292; SBT) is a covalent/irreversible, orally bioactive, and highly selective inhibitor of Bruton's agammaglobulinemia tyrosine kinase/BTK inhibitor with potential antitumor activity. It inhibits BTK with an IC50 of<0.5 nM, and exhibits > 1400-fold higher selectivity for BTK over the other kinases.
ln Vitro |
Spebrutinib (CC-292) is an oral Btk inhibitor that is covalent, highly selective, and has an IC50 of 0.5 nM. Moreover, spebrutinib exhibits mild inhibitory effects on Yes, c-Src, Brk, Lyn, and Fyn, with corresponding IC50s of 723 nM, 1.729 μM, 2.43 μM, 4.4 μM, and 7.15 μM. A further investigation revealed a close correlation between the cellular EC50 of Spebrutinib inhibition of Btk kinase (EC50=8 nM) and the EC50 of Btk occupancy in Ramos cells in response to the drug's dosage response (EC50=6 nM). Moreover, 35 nM of spebrutinib is the concentration that suppresses 90% of Btk activity in Ramos cells, whereas 39 nM is the concentration needed for 90% Btk occupancy [1].
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ln Vivo |
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Animal Protocol |
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References |
[1]. Evans EK, et al. Inhibition of Btk with CC-292 provides early pharmacodynamic assessment of activity in mice and humans. J Pharmacol Exp Ther. 2013 Aug;346(2):219-28
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Molecular Formula |
C22H22FN5O3
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Molecular Weight |
423.44
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CAS # |
1202757-89-8
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Related CAS # |
Spebrutinib besylate;1360053-81-1
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SMILES |
FC1=C([H])N=C(N=C1N([H])C1C([H])=C([H])C([H])=C(C=1[H])N([H])C(C([H])=C([H])[H])=O)N([H])C1C([H])=C([H])C(=C([H])C=1[H])OC([H])([H])C([H])([H])OC([H])([H])[H]
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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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Solubility (In Vivo) |
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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 |
*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 |
NCT01975610 | Completed | Drug: CC-292 Drug: CC-292 |
Rheumatoid Arthritis | Celgene | October 2013 | Phase 2 |
NCT02031419 | Terminated | Drug: CC-122 Drug: CC-223 |
Lymphoma, Large B-Cell, Diffuse |
Celgene | December 18, 2013 | Phase 1 |
Btk occupancy and Btk protein resynthesis can be detected in mice in vivo. Mice were treated orally once with 50 mg/kg CC-292 to inhibit all Btk protein.J Pharmacol Exp Ther.2013 Aug;346(2):219-28. td> |
CC-292 is efficacious in an established collagen-induced arthritis model.J Pharmacol Exp Ther.2013 Aug;346(2):219-28. td> |