WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 530642
Description: G-744 is a highly potent, selective for Btk inhibitor. G-774 is metabolically stable, well tolerated, and efficacious in an animal model of arthritis. G-744 prevents cellular functions in murine B-cells such as B-cell receptor (BCR)-mediated CD86 induction with an EC50 of 64nM. G-744 also inhibited BCR-stimulated B-cell proliferation in human B-cells (EC50 = 22 nM). In human monocytes, production of the inflammatory cytokine TNFα following activation with immune complexes was abrogated by G-744 (EC50 = 33 nM). In human whole blood, G-744 demonstrated potent inhibition of BCR-stimulated CD69 expression on Bcells with an EC50 of 87 nM.
MedKoo Cat#: 530642
Chemical Formula: C29H29N5O3S
Exact Mass: 527.1991
Molecular Weight: 527.643
Elemental Analysis: C, 66.01; H, 5.54; N, 13.27; O, 9.10; S, 6.08
This product is not in stock, which may be available by custom synthesis.
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Synonym: G-744; G 744; G744.
IUPAC/Chemical Name: 2-(2-(hydroxymethyl)-3-(1-methyl-6-oxo-5-(pyrimidin-4-ylamino)-1,6-dihydropyridin-3-yl)phenyl)-6,6-dimethyl-3,4,6,7-tetrahydro-2H-cyclopenta[4,5]thieno[2,3-c]pyridin-1(5H)-one
InChi Key: QAESSIFTPVEYRY-UHFFFAOYSA-N
InChi Code: InChI=1S/C29H29N5O3S/c1-29(2)12-20-19-8-10-34(28(37)26(19)38-24(20)13-29)23-6-4-5-18(21(23)15-35)17-11-22(27(36)33(3)14-17)32-25-7-9-30-16-31-25/h4-7,9,11,14,16,35H,8,10,12-13,15H2,1-3H3,(H,30,31,32)
SMILES Code: OCC1=C(N2C(C(SC3=C4CC(C)(C)C3)=C4CC2)=O)C=CC=C1C5=CN(C)C(C(NC6=NC=NC=C6)=C5)=O
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 527.643 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.15 mL||5.76 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|
1: Katewa A, Wang Y, Hackney JA, Huang T, Suto E, Ramamoorthi N, Austin CD, Bremer M, Chen JZ, Crawford JJ, Currie KS, Blomgren P, DeVoss J, DiPaolo JA, Hau J, Johnson A, Lesch J, DeForge LE, Lin Z, Liimatta M, Lubach JW, McVay S, Modrusan Z, Nguyen A, Poon C, Wang J, Liu L, Lee WP, Wong H, Young WB, Townsend MJ, Reif K. Btk-specific inhibition blocks pathogenic plasma cell signatures and myeloid cell-associated damage in IFNα-driven lupus nephritis. JCI Insight. 2017 Apr 6;2(7):e90111. doi: 10.1172/jci.insight.90111. PubMed PMID: 28405610; PubMed
Central PMCID: PMC5374071.
2. Discovery of Potent and Selective Tricyclic Inhibitors of Bruton’s Tyrosine Kinase with Improved Druglike Properties Xiaojing Wang, James Barbosa, Peter Blomgren, Meire C. Bremer, Jacob Chen, James J. Crawford, Wei Deng, Liming Dong, Charles igenbrot, Steve allion, Jonathon Hau, Huiyong Hu, Adam R. Johnson, Arna Katewa, Jeffrey E. Kropf, Seung H. Lee, Lichuan Liu, Joseph W. Lubach, Jen Macaluso, Pat Maciejewski, Scott A. Mitchell, Daniel F. Ortwine, Julie DiPaolo, Karin Reif, Heleen Scheerens, Aaron chmitt, Harvey Wong, Jin-Ming Xiong, Jianjun Xu, Zhongdong Zhao, Fusheng Zhou, Kevin S. Currie, and Wendy B. Young Publication Date (Web): May 3, 2017 (Letter) DOI: 10.1021/acsmedchemlett.7b00103