GDC-0853 - CAS 1434048-34-6
Catalog number: 1434048-34-6
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
Molecular Weight:
Ser/Thr Protease
GDC-0853 is a Bruton's tyrosine kinase (BTK) inhibitor originated by Genentech. GDC-0853 can inhibit the activity of BTK and prevent the activation of the B-cell antigen receptor (BCR) signaling pathway. This leads to the inhibition of the growth of malignant B-cells that overexpress BTK. Phase I clinical trials for the treatment of Autoimmune disorders and Phase II clinical trials for the treatment of Rheumatoid arthritis are on-going.
RG 7845; GDC-0853; RG7845; GDC0853; RG-7845; GDC 0853; (S)-2-(3'-(hydroxymethyl)-1-methyl-5-((5-(2-methyl-4-(oxetan-3-yl)piperazin-1-yl)pyridin-2-yl)amino)-6-oxo-1,6-dihydro-[3,4'-bipyridin]-2'-yl)-7,7-dimethyl-3,4,7,8-tetrahydro-2H-cyclopenta[4,5]pyrrolo[1,2-a]pyrazin-1(6H)-one
DMSO ≥ 25 mg/mL
-20°C Freezer
Rheumatoid arthritis;Autoimmune disorders
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Canonical SMILES:
Current Developer:
Originator Genentech
1.Bruton's Tyrosine Kinase Small Molecule Inhibitors Induce a Distinct Pancreatic Toxicity in Rats.
Erickson RI;Schutt LK;Tarrant JM;McDowell M;Liu L;Johnson AR;Lewin-Koh SC;Hedehus M;Ross J;Carano RA;Staflin K;Zhong F;Crawford JJ;Zhong S;Reif K;Katewa A;Wong H;Young WB;Dambach DM;Misner DL J Pharmacol Exp Ther. 2017 Jan;360(1):226-238. Epub 2016 Nov 7.
Bruton's tyrosine kinase (BTK) is a member of the Tec family of cytoplasmic tyrosine kinases involved in B-cell and myeloid cell signaling. Small molecule inhibitors of BTK are being investigated for treatment of several hematologic cancers and autoimmune diseases. GDC-0853 ((S)-2-(3'-(hydroxymethyl)-1-methyl-5-((5-(2-methyl-4-(oxetan-3-yl)piperazin-1-yl)pyridin-2-yl)amino)-6-oxo-1,6-dihydro-[3,4'-bipyridin]-2'-yl)-7,7-dimethyl-3,4,7,8-tetrahydro-2H-cyclopenta[4,5]pyrrolo[1,2-a]pyrazin-1(6H)-one) is a selective and reversible oral small-molecule BTK inhibitor in development for the treatment of rheumatoid arthritis and systemic lupus erythematosus. In Sprague-Dawley (SD) rats, administration of GDC-0853 and other structurally diverse BTK inhibitors for 7 days or longer caused pancreatic lesions consisting of multifocal islet-centered hemorrhage, inflammation, fibrosis, and pigment-laden macrophages with adjacent lobular exocrine acinar cell atrophy, degeneration, and inflammation. Similar findings were not observed in mice or dogs at much higher exposures. Hemorrhage in the peri-islet vasculature emerged between four and seven daily doses of GDC-0853 and was histologically similar to spontaneously occurring changes in aging SD rats.
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