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SML2851

Sigma-Aldrich

Galunisertib

≥98% (HPLC)

Synonym(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

Empirical Formula (Hill Notation):
C22H19N5O
CAS Number:
700874-72-2
Molecular Weight:
369.42
MDL number:
MFCD12923319
UNSPSC Code:
12352200
NACRES:
NA.77
Pricing and availability is not currently available.

Quality Level

100

Assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

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

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.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

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Certificates of Analysis (COA)

Lot/Batch Number
0000427091
0000427091
0000418875
0000418876
0000418876

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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
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
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
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
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