Fenebrutinib

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

一种口服生物可利用的、选择性的、非共价的、可逆的 BTK 抑制剂，IC50 为 2-9 nM。

An orally bioavailable, selective, non-covalent and reversible BTK inhibitor with IC50 of 2-9 nM; has demonstrated efficacy in pre-clinical autoimmune disease models and is being developed for the treatment of rheumatoid arthritis and lupus, with future development for other autoimmune indications.RheumatoId Arthritis Phase 2 Clinical(In Vitro):Fenebrutinib (GDC-0853) inhibits CD69 expression on CD19+ B cells in human whole blood with an IC50 of 8.4±5.6 nM. Fenebrutinib inhibits CD63 expression on basophils with an IC50 of 30.7±4.1 nM.Fenebrutinib suppresses anti-IgM induced Btk Y223 autophosphorylation in human whole blood (IC50=11 nM).(In Vivo):Fenebrutinib (GDC-0853) dose-dependently reduces ankle thickness following once (0.06, 0.25, 1, 4, and 16 mg/kg QD; orally) or twice (0.125, 0.5, and 2 mg/kg BID; orally) daily in female Lewis rats with developing collagen-induced arthritis.Fenebrutinib (0.2 mg/kg IV and 1.0 mg/kg PO; for rats) and (0.2 mg/kg IV and 0.5 mg/kg PO for dogs) demonstrates the half-lives (t1/2s) of 2.2 and 3.8 h In rats, and dogs, respectively.

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Animal Model:Female Lewis rats with developing collagen-induced arthritis (CIA) Dosage:0.06, 0.25, 1, 4, and 16 mg/kg once daily (QD); 0.125, 0.5, and 2 mg/kg twice daily (BID) Administration:Dosed orally; for 16 days Result:Dose-dependently reduced ankle thickness following QD and BID dosing regimens.

RG-7845 | GDC-0853

Tyrosine Kinase

BTK

BTK

Inflammation/Immunology

Rheumatoid Arthritis

1434048-34-6

664.7964

C37H44N8O4

>98% (HPLC)

DMSO: ≥ 23 mg/mL

CC1CN(CCN1C2=CN=C(C=C2)NC3=CC(=CN(C3=O)C)C4=C(C(=NC=C4)N5CCN6C7=C(CC(C7)(C)C)C=C6C5=O)CO)C8COC8

2H-Cyclopenta[4,5]pyrrolo[1,2-a]pyrazin-1(6H)-one, 2-[1,6-dihydro-3'-(hydroxymethyl)-1-methyl-5-[[5-[(2S)-2-methyl-4-(3-oxetanyl)-1-piperazinyl]-2-pyridinyl]amino]-6-oxo[3,4'-bipyridin]-2'-yl]-3,4,7,8-tetrahydro-7,7-dimethyl-

(-20℃)

With Ice Pack

≥ 2 years