Spebrutinib besylate (Synonyms: AVL-292 benzenesulfonate; CC-292 besylate) |
| رقم الكتالوجGC37672 |
Spebrutinib besylate (AVL-292 benzenesulfonate ؛ CC-292 besylate) هو مثبط قوي لنشاط Btk كيناز (IC50 <0.5 نانومتر ، Kinact / Ki = 7.69 × 104 M-1s-1s) في فحوصات الكيمياء الحيوية
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Cas No.: 1360053-81-1
Sample solution is provided at 25 µL, 10mM.
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Spebrutinib besylate (AVL-292 benzenesulfonate; CC-292 besylate) is a potent inhibitor of Btk kinase activity (IC50<0.5 nM, Kinact/Ki=7.69×104 M-1s-1s) in biochemical assays. IC50: <0.5 nM (Btk)[1]
Spebrutinib (CC-292) is a covalent, highly selective, orally active inhibitor of Btk with IC50 value of 0.5 nM. Spebrutinib also less potently inhibits Yes, c-Src, Brk, Lyn, and Fyn with IC50s of 723 nM, 1.729 μM, 2.43 μM, 4.4 μM, and 7.15 μM, rspectively. Extensive analysis has revealed that the EC50 of Btk occupancy from a Spebrutinib dose-response in Ramos cells (EC50=6 nM) correlated directly with the cellular EC50 of Btk kinase inhibition with Spebrutinib (EC50=8 nM). Furthermore, the concentration at which Spebrutinib inhibits 90% of Btk activity in Ramos cells is 35 nM while the concentration of Spebrutinib required for 90% occupancy of Btk is 39 nM[1].
[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.
Cell experiment: | Cells are incubated in serum-free RPMI media for 1-1.5 hours. Isolated human B cells are incubated with Spebrutinib at a final concentration of 0.001, 0.01, 0.1 and 1 μM. Ramos cells are incubated with 0.1 nM-3 μM Spebrutinib. Cells are then incubated in the presence of compound for 1 hour at 37°C. Following incubation, cells are centrifuged and resuspended in 100 μL of serum-free RPMI and BCR is stimulated with addition of 5 μg/mL α-human IgM. Samples are centrifuged, washed in phosphate-buffered saline (PBS), and lysed in 100 μL of Cell Extraction Buffer plus 1:10 (v/v) PhosSTOP Phosphatase Inhibitor and 1:10 (v/v) Complete Protease Inhibitor. Antibodies used for immunoblot analysis include P-PLCγ2, PLCγ2 (3871; CST), Syk (2712; CST), P-Syk (2710; CST), Btk, P-Btk, and Tubulin. Membranes are scanned on a Li-Cor Odyssey scanner using infrared fluorescence detection[1]. |
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. | |
| Cas No. | 1360053-81-1 | SDF | |
| المرادفات | AVL-292 benzenesulfonate; CC-292 besylate | ||
| Canonical SMILES | COCCOC1=CC=C(NC2=NC=C(F)C(NC3=CC=CC(NC(C=C)=O)=C3)=N2)C=C1.O=S(C4=CC=CC=C4)(O)=O | ||
| Formula | C28H28FN5O6S | M.Wt | 581.62 |
| الذوبان | Soluble in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7193 mL | 8.5967 mL | 17.1934 mL |
| 5 mM | 0.3439 mL | 1.7193 mL | 3.4387 mL |
| 10 mM | 0.1719 mL | 0.8597 mL | 1.7193 mL |
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- Purity: >98.00%
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