Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C37H44N8O4 |
Molecular Weight | 664.7965 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
C[C@H]1CN(CCN1C2=CN=C(NC3=CC(=CN(C)C3=O)C4=CC=NC(N5CCN6C(=CC7=C6CC(C)(C)C7)C5=O)=C4CO)C=C2)C8COC8
InChI
InChIKey=WNEODWDFDXWOLU-QHCPKHFHSA-N
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/s1
Molecular Formula | C37H44N8O4 |
Molecular Weight | 664.7965 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
G-0853 (also GDC-0853, or Fenebrutinib) is a potent, selective, orally administered, and noncovalent Bruton's tyrosine kinase (Btk) inhibitor currently in clinical development. Upon administration, G-0853 inhibits the activity of Btk and prevents the activation of the B-cell antigen receptor (BCR) signaling pathway. This prevents both B-cell activation and Btk-mediated activation of downstream survival pathways, which leads to the inhibition of the growth of malignant B-cells that overexpress BTK. BTK is overexpressed in B-cell malignancies, and plays an important role in B-lymphocyte development, activation, signaling, proliferation and survival. G-0853 suppresses B cell- and myeloid cell-mediated components of disease and demonstrates dose-dependent activity in an in vivo rat model of inflammatory arthritis. G-0853 demonstrates highly favorable safety, pharmacokinetic (PK), and pharmacodynamic (PD) profiles in preclinical and Phase 2 studies ongoing in patients with rheumatoid arthritis, lupus, and chronic spontaneous urticaria.
Approval Year
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 08:26:24 GMT 2023
by
admin
on
Sat Dec 16 08:26:24 GMT 2023
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Record UNII |
E9L2885WUL
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Record Status |
Validated (UNII)
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Record Version |
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NCI_THESAURUS |
C129825
Created by
admin on Sat Dec 16 08:26:24 GMT 2023 , Edited by admin on Sat Dec 16 08:26:24 GMT 2023
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NCI_THESAURUS |
C124801
Created by
admin on Sat Dec 16 08:26:24 GMT 2023 , Edited by admin on Sat Dec 16 08:26:24 GMT 2023
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EF-62
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1434048-34-6
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10603
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DB14785
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E9L2885WUL
Created by
admin on Sat Dec 16 08:26:24 GMT 2023 , Edited by admin on Sat Dec 16 08:26:24 GMT 2023
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100000175821
Created by
admin on Sat Dec 16 08:26:24 GMT 2023 , Edited by admin on Sat Dec 16 08:26:24 GMT 2023
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C116844
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admin on Sat Dec 16 08:26:24 GMT 2023 , Edited by admin on Sat Dec 16 08:26:24 GMT 2023
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86567195
Created by
admin on Sat Dec 16 08:26:24 GMT 2023 , Edited by admin on Sat Dec 16 08:26:24 GMT 2023
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PRIMARY |
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ACTIVE MOIETY |
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