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Principaux documents

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SML2851

Sigma-Aldrich

Galunisertib

≥98% (HPLC)

Synonyme(s) :

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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About This Item

Formule empirique (notation de Hill) :
C22H19N5O
Numéro CAS:
700874-72-2
Poids moléculaire :
369.42
Numéro MDL:
MFCD12923319
Code UNSPSC :
12352200
Nomenclature NACRES :
NA.77

Niveau de qualité

100

Essai

≥98% (HPLC)

Forme

powder

Couleur

white to beige

Solubilité

DMSO: 2 mg/mL, clear

Température de stockage

2-8°C

Chaîne SMILES 

[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)

Clé InChI

IVRXNBXKWIJUQB-UHFFFAOYSA-N

Actions biochimiques/physiologiques

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.

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 3

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

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Certificats d'analyse (COA)

Lot/Batch Number
0000427091
0000427091
0000418875
0000418876
0000418876

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Retrouvez la documentation relative aux produits que vous avez récemment achetés dans la Bibliothèque de documents.

Consulter la Bibliothèque de documents

Mariafrancesca Cascione et al.
International journal of molecular sciences, 20(1) (2019-01-02)
The epithelial mesenchymal transition (EMT) is a physiological multistep process involving epithelial cells acquiring a mesenchymal-like phenotype. It is widely demonstrated that EMT is linked to tumor progression and metastasis. The transforming growth factor (TGF)-β pathways have been widely investigated
Wan He et al.
Cancer cell international, 19, 160-160 (2019-06-15)
Our previous studies revealed that Jagged 2 (JAG2) is involved in the regulation of migration and invasion of colon cancer cells without affecting cell proliferation. This study further explored the specific mechanism by which JAG2 promotes migration and invasion of
Wenlong Li et al.
International journal of cancer, 146(6), 1631-1642 (2019-07-16)
Galunisertib (LY2157299), a promising small-molecule inhibitor of the transforming growth factor-beta (TGF-β) receptor, is currently in mono- and combination therapy trials for various cancers including glioblastoma, hepatocellular carcinoma and breast cancer. Using genetically modified mouse models, we investigated the roles
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
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