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Spebrutinib

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Chemical Structure| 1202757-89-8 同义名 : -
CAS号 : 1202757-89-8
货号 : A537377
分子式 : C22H22FN5O3
纯度 : 98+%
分子量 : 423.44
MDL号 : MFCD25976876
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 45 mg/mL(106.27 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • BTK

    BTK, IC50:<0.5 nM
描述 Bruton’s tyrosine kinase (Btk) plays a crucial role in B cell development and activation through the B cell receptor (BCR) signaling pathway and represents a new target for diseases characterized by inappropriate B cell activity[3]. AVL-292 is a highly selective, covalent Btk inhibitor with IC50 less than 0.5 nM. In Ramos cells which express an intact BCR signaling pathway, AVL-292 (0.1 nM-3 μM) potently inhibited Btk autophosphorylation on Tyr223 (EC50 = 8 nM), phosphorylation of the Btk substrate, PLCγ2, as well as activation of the downstream kinase. In the collagen-induced arthritis (CIA) model of arthritis, AVL-292 (3-30 mg/kg, p.o.) dose-dependently suppressed the clinical signs of inflammatory disease including reduction in joint and paw swelling and visible redness of the affected paws. Reduction of clinical signs of disease was measured at 95%, 85% and 50% for 30, 10 and 3mg/kg treatment respectively[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.36mL

0.47mL

0.24mL

11.81mL

2.36mL

1.18mL

23.62mL

4.72mL

2.36mL
参考文献

[1]Eda H, Santo L, et al. A novel Bruton's tyrosine kinase inhibitor CC-292 in combination with the proteasome inhibitor carfilzomib impacts the bone microenvironment in a multiple myeloma model with resultant antimyeloma activity. Leukemia. 2014 Sep;28(9):1892-901.

[2]Evans EK, Tester R, 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.

[3]Evans EK, Tester R, Aslanian S, Karp R, Sheets M, Labenski MT, Witowski SR, Lounsbury H, Chaturvedi P, Mazdiyasni H, Zhu Z, Nacht M, Freed MI, Petter RC, Dubrovskiy A, Singh J, Westlin WF. 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. doi: 10.1124/jpet.113.203489. Epub 2013 May 24. PMID: 23709115.