G-744

Research use only, not for human use.

G-744 is a highly potent, selective inhibitor of BTK with biochemical Ki of 1.28 nM.

G-744 is a highly potent, selective inhibitor of BTK with biochemical Ki of 1.28 nM; demonstrates >1,000-fold selectivity against a panel 285 kinase (exception with EphA7 and Fgr, 400-800 fold); prevents BCR-mediated CD86 induction (EC50=64 nM), also inhibits BCR-stimulated B-cell proliferation in human B-cells (EC50=22 nM), abrogates production of TNFα in human monocytes (EC50=33 nM); demonstrates efficacy in the developing CIA model in rats.

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G-744 (6.25/12.25/25 mg/kg, p.o., b.i.d., daily) protects Lewis rats from collagen-induced arthritis dose-dependently. Animal Model:Female Lewis rat based CIA models.Dosage:6.25, 12.25, 25 mg/kg.Administration:Orally, b.i.d., daily for 17 days.Result:All three doses resulted in a significant dose-dependent inhibition of ankle thickness between day 10 and day 17 (onset of increase in ankle diameter on day 9).

G 744 | G744

Tyrosine Kinase

BTK

BTK

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1346669-54-2

527.643

C29H29N5O3S

>98% (HPLC)

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OCC1=C(N2C(C(SC3=C4CC(C)(C)C3)=C4CC2)=O)C=CC=C1C5=CN(C)C(C(NC6=NC=NC=C6)=C5)=O

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

(-20℃)

With Ice Pack

≥ 2 years