All Photos(1)
2-(6-Methyl-pyridin-2-yl)-3-[6-amido-quinolin-4-yl)-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole, 4-(2-(6-Methylpyridin-2-yl)-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl)quinoline-6-carboxamide, 4-[5,6-Dihydro-2-(6-methyl-2-pyridinyl)-4H-pyrrolo[1,2-b]pyrazol-3-yl]-6-quinolinecarboxamide, LY 2157299, LY-2157299, LY2157299
C22H19N5O
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Quality Level
Assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
InChI
1S/C22H19N5O/c1-13-4-2-5-18(25-13)21-20(19-6-3-11-27(19)26-21)15-9-10-24-17-8-7-14(22(23)28)12-16(15)17/h2,4-5,7-10,12H,3,6,11H2,1H3,(H2,23,28)
InChI key
IVRXNBXKWIJUQB-UHFFFAOYSA-N
Biochem/physiol Actions
Galunisertib (LY2157299) is an orally active multikinase inhibitor (IC50 in nM = 80/ALK4, 170/TGFβR1, 210/TGβ?R2, 190/MINK (MAP4K6), 220/RIP2 (RIPK2), 260/CK1α, 280/MEKKK4, 310/GAK, 400/CK1ε, 470/ALK6 (BMPR1B), 500/B-raf, 510/TNIK) mostly cited for its ALK4 & TGFbeta (TGFβ) receptors (TGFβ-RI (ALK5) & TGFβ-RII) inhibitory activity and anticancer efficacy in vitro (0.1-10 μM) and in vivo (20-100 mg/kg p.o.; mice).
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
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Immune network, 18(6), e45-e45 (2019-01-09)
Immune checkpoint inhibitors (ICIs), such as anti-PD-1 and anti-PD-L1 Abs, have shown efficacy for the treatment of various cancers. Although research has actively sought to develop new ICIs and immunomodulators, no efficient in vitro assay system is available to evaluate
Drug design, development and therapy, 9, 4479-4499 (2015-08-27)
Transforming growth factor-beta (TGF-β) signaling regulates a wide range of biological processes. TGF-β plays an important role in tumorigenesis and contributes to the hallmarks of cancer, including tumor proliferation, invasion and metastasis, inflammation, angiogenesis, and escape of immune surveillance. There
Theranostics, 9(14), 4115-4129 (2019-07-10)
Galunisertib (Gal) is a transforming growth factor (TGF-β) blockade which is being investigated as a potential tumor immunotherapy candidate drug in clinical trials. However, primary or acquired resistance is often found in the recruited cancer patients, which limits its clinical
European journal of cancer (Oxford, England : 1990), 44(1), 142-150 (2007-11-28)
Human xenografts Calu6 (non-small cell lung cancer) and MX1 (breast cancer) were implanted subcutaneously in nude mice and LY2157299, a new type I receptor TGF-beta kinase antagonist, was administered orally. Plasma levels of LY2157299, percentage of phosphorylated Smad2,3 (pSmad) in
Cellular oncology (Dordrecht), 38(2), 131-144 (2015-01-13)
The transforming growth factor-beta (TGF-β) signaling pathway is known to play a critical role in promoting tumor growth. Consequently, blocking this pathway has been found to inhibit tumor growth. In order to achieve an optimal anti-tumor effect, however, it remains
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