AVL-292

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

AVL-292 (Spebrutinib, CC-292) 是一种高选择性、共价 Btk 抑制剂，IC50 <1 nM；对 Yes、c-Src、Brk、Lyn 和 Fyn 的抑制作用也较弱，IC50 分别为 723 nM、1.729 uM、2.43 uM、4.4 uM 和 7.15 uM。

AVL-292 (Spebrutinib, CC-292) is a highly selective, covalent Btk inhibitor with IC50 of <1 nM; also less potently inhibits Yes, c-Src, Brk, Lyn, and Fyn with IC50s of 723 nM, 1.729 uM, 2.43 uM, 4.4 uM, and 7.15 uM, rspectively; shows anti-inflammatory activity in the collagen-induced arthritis model of autoimmune disease; also prevents NRG- and EGF-dependent growth factor-driven resistance to lapatinib in HER2(+) breast cancer cells.Rheumatoid Arthritis Phase 2 Clinical.(In Vitro):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.

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Spebrutinib | CC-292

Tyrosine Kinase

BTK

BRK|BTK|c-Src|Lyn|Yes

Inflammation/Immunology

Rheumatoid Arthritis

1202757-89-8

423.4402

C22H22FN5O3

>98% (HPLC)

DMSO: ≥ 45 mg/mL

C=CC(NC1=CC=CC(NC2=NC(NC3=CC=C(OCCOC)C=C3)=NC=C2F)=C1)=O

2-Propenamide, N-[3-[[5-fluoro-2-[[4-(2-methoxyethoxy)phenyl]amino]-4-pyrimidinyl]amino]phenyl]-

(-20℃)

With Ice Pack

≥ 2 years