For research use only. Not for therapeutic Use.
GDC-0853(CAT: I001677)is an orally available, potent inhibitor of Bruton’s tyrosine kinase (BTK) with IC₅₀ values ranging from 2–9 nM for basophil activation, B-cell receptor (BCR) activation, and constitutive p-BTK activity in whole blood lysates. By targeting BTK, GDC-0853 effectively disrupts the BCR signaling pathway, inhibiting both B-cell activation and BTK-mediated downstream survival pathways. This mechanism leads to the suppression of malignant B-cell proliferation in conditions where BTK is overexpressed. Currently in Phase II development for the treatment of rheumatoid arthritis, GDC-0853 is a critical tool for exploring therapeutic strategies in autoimmune diseases and B-cell malignancies.
Catalog Number | I001677 |
CAS Number | 1434048-34-6 |
Synonyms | RG-7845;GDC-0853;GDC0853;GDC 0853 |
Molecular Formula | C37H44N8O4 |
Purity | ≥95% |
Target | Btk |
Solubility | DMSO ≥ 25 mg/mL |
Storage | -20°C |
IUPAC Name | 10-[3-(hydroxymethyl)-4-[1-methyl-5-[[5-[(2S)-2-methyl-4-(oxetan-3-yl)piperazin-1-yl]pyridin-2-yl]amino]-6-oxopyridin-3-yl]pyridin-2-yl]-4,4-dimethyl-1,10-diazatricyclo[6.4.0.02,6]dodeca-2(6),7-dien-9-one |
InChI | InChI=1S/C37H44N8O4/c1-23-18-42(27-21-49-22-27)9-10-43(23)26-5-6-33(39-17-26)40-30-13-25(19-41(4)35(30)47)28-7-8-38-34(29(28)20-46)45-12-11-44-31(36(45)48)14-24-15-37(2,3)16-32(24)44/h5-8,13-14,17,19,23,27,46H,9-12,15-16,18,20-22H2,1-4H3,(H,39,40)/t23-/m0 |
InChIKey | WNEODWDFDXWOLU-QHCPKHFHSA-N |
SMILES | O=C1N(C)C=C(C2=CC=NC(N3CCN4C(C3=O)=CC5=C4CC(C)(C)C5)=C2CO)C=C1NC(N=C6)=CC=C6N7CCN(C8COC8)C[C@@H]7C |