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Galunisertib

Galunisertib structure

CAS No:
700874-72-2
Formula:
C22H19N5O
Chemical Name:
Galunisertib
Synonyms:
6-Quinolinecarboxamide,4-[5,6-dihydro-2-(6-methyl-2-pyridinyl)-4H-pyrrolo[1,2-b]pyrazol-3-yl]-;4-[5,6-Dihydro-2-(6-methyl-2-pyridinyl)-4H-pyrrolo[1,2-b]pyrazol-3-yl]-6-quinolinecarboxamide;LY 2157299;Galunisertib;912477-03-3
Categories:
Biochemical Engineering > Inhibitors

Description

LY-2157299 is a pyrrolopyrazole that is 5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole which is substituted at positions 2 and 3 by 6-methylpyridin-2-yl and 6-(aminocarbonyl)quinolin-4-yl groups, respectively. A Transforming growth factor-betaRI (TGF-betaRI) kinase inhibitor, it blocks TGF-beta-mediated tumor growth in glioblastoma. It has a role as a TGFbeta receptor antagonist and an antineoplastic agent. It is a member of quinolines, a pyrrolopyrazole, a member of methylpyridines, an aromatic amide and a monocarboxylic acid amide.|Galunisertib has been used in trials studying the basic science and treatment of Glioma, Neoplasms, Solid Tumor, GLIOBLASTOMA, and Prostate Cancer, among others.|Galunisertib is an orally available, small molecule antagonist of the tyrosine kinase transforming growth factor-beta (TGF-b) receptor type 1 (TGFBR1), with potential antineoplastic activity. Upon administration, galunisertib specifically targets and binds to the kinase domain of TGFBR1, thereby preventing the activation of TGF-b-mediated signaling pathways. This may inhibit the proliferation of TGF-b-overexpressing tumor cells. Dysregulation of the TGF-b signaling pathway is seen in a number of cancers and is associated with increased cancer cell proliferation, migration, invasion and tumor progression.

Galunisertib Basic Attributes

Molecular Weight：

369.43

Exact Mass：

369.42

UNII：

3OKH1W5LZE

DSSTox ID：

DTXSID00220362

NCI Thesaurus Code：

C116891

HScode：

29334900

Characteristics

PSA：

86.7

XLogP3：

2.4

Density：

1.40

Boiling Point：

619.004ºC at 760 mmHg

Flash Point：

328.162ºC

Safety Information

safety instructions：

Marks：

Drug Information

MeSH Entry Terms：

4-(2-(6-methylpyridin-2-yl)-5,6-dihydro-4H-pyrrolo(1,2-b)pyrazol-3-yl)quinoline-6-carboxylic acid amide

Galunisertib Use and Manufacturing

LY2157299 is a small molecule inhibitor of the TGF-β receptor type 1 kinase (IC50 = 56 nM). It has been used to study the role of TGF-β signaling in chemotherapy-induced expansion of cancer stem-like cells in triple negative breast cancer cell lines and xenografts. LY2157299 has also been shown to inhibit the migration and tumor growth of hepatocellular carcinoma cell lines by disrupting Smad-2 phosphorylation.[Cayman Chemical]

Computed Properties

Molecular Weight:369.4
XLogP3:2.4
Hydrogen Bond Donor Count:1
Hydrogen Bond Acceptor Count:4
Rotatable Bond Count:3
Exact Mass:369.15896025
Monoisotopic Mass:369.15896025
Topological Polar Surface Area:86.7
Heavy Atom Count:28
Complexity:585
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

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Galunisertib cas 700874-72-2

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