SML2851
Galunisertib
≥98% (HPLC), multikinase inhibitor , powder
别名:
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
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关于此项目
经验公式（希尔记法）:
C22H19N5O
化学文摘社编号:
分子量:
369.42
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
产品名称
Galunisertib, ≥98% (HPLC)
SMILES string
[n]21nc(c(c2CCC1)c4c5c(ncc4)ccc(c5)C(=O)N)c3nc(ccc3)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
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
Quality Level
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).
Orally active multikinase inhibitor best known for its ALK4, TGFbeta receptors TGFβ-RI (ALK5) & TGFβ-RII activity and anticancer efficacy in vitro and in vivo.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Linlin Shi et al.
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
Lorea Bueno et al.
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
Armin Maier et al.
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
Minsuk Kwon et al.
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
Stephan Herbertz et al.
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
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