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:
C37H44N8O4
Molecular Weight:
664.81
COA:
Inquire
Targets:
Ser/Thr Protease
Description:
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.
Purity:
98%
Appearance:
Powder
Synonyms:
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
Solubility:
DMSO ≥ 25 mg/mL
Storage:
-20°C Freezer
MSDS:
Inquire
Application:
Rheumatoid arthritis;Autoimmune disorders
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Milligrams-Grams
InChIKey:
WNEODWDFDXWOLU-QHCPKHFHSA-N
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
Canonical SMILES:
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
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.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related Ser/Thr Protease Products


BAY-1217389
(CAS: 1554458-53-5)

BAY-1217389, an imidazopyridazin derivative, has been found to be a TTK protein inhibitor that could probably be effective as an antineoplastic agent and also b...

CAS 256476-36-5 UK-371804 HCl

UK-371804 HCl
(CAS: 256476-36-5)

UK-371804 is a potent and selective urokinase-type plasmogen activator (uPA) inhibitor. Study in vitro showed that it inhibited exogenous uPA in human chronic w...

CAS 625110-37-4 DPP-IV-IN-1

DPP-IV-IN-1
(CAS: 625110-37-4)

A potent inhibitor of dipeptidyl peptidase IV (DPP-IV)

CFI-401870
(CAS: 1430741-35-7)

CFI-401870 is a TTK (tyrosine threonine kinase) Inhibitor with IC50 value < 10 nM. CFI-401870 showed low off-target activity (>500×) and microsomal stability (T...

CAS 82956-11-4 Nafamostat Mesylate

Nafamostat Mesylate
(CAS: 82956-11-4)

Nafamostat Mesylate is a synthetic serine protease inhibitor and an anticoagulant. It is a fast-acting proteolytic inhibitor and used during hemodialysis to pre...

Ono 3403
(CAS: 181586-07-2)

Ono 3403, a derivative of camostat mesilate and has a higher protease-inhibitory activity, is a synthetic serine protease inhibitor that inhibits lipopolysaccha...

LCH7749944 HCl
(CAS: 1049788-58-0)

LCH7749944 HCl is a novel and potent PAK4 inhibitor. It could effectively suppress the proliferation of human gastric cancer cells through downregulation of PAK...

CAS 1346547-00-9 GSK583

GSK583
(CAS: 1346547-00-9)

GSK583 is a selective receptor-interacting serine/threonine-protein kinase 2 (RIP2 Kinase) inhibitor and the RIP2K binding IC50 is 5 nM. GSK583 can inhibit both...

Quick Inquiry

Verification code

Featured Items