GW441756

Names

[ Name ]:
GW441756

[Synonym ]:
(3E)-3-[(1-Methyl-1H-indol-3-yl)methylene]-1,3-dihydro-2H-pyrrolo[3,2-b]pyridin-2-one
2H-Pyrrolo[3,2-b]pyridin-2-one, 1,3-dihydro-3-[(1-methyl-1H-indol-3-yl)methylene]-, (3Z)-
(3Z)-3-[(1-Methyl-1H-indol-3-yl)methylene]-1,3-dihydro-2H-pyrrolo[3,2-b]pyridin-2-one
2H-Pyrrolo[3,2-b]pyridin-2-one, 1,3-dihydro-3-[(1-methyl-1H-indol-3-yl)methylene]-, (3E)-
(3Z)-3-[(1-methyl-1H-indol-3-yl)methylidene]-1,3-dihydro-2H-pyrrolo[3,2-b]pyridin-2-one
GW 441756
GW441756

Biological Activity

[Description]:

GW 441756 is a specific Tropomyosin-related kinase A (TrkA) inhibitor with an IC50 value of 2 nM; little activity to c-Raf1 and CDK2.IC50 Value: 2 nM [1]Target: TrkAin vitro: GW441756 specifically blocked TrkA-induced cell death in a dose-dependent manner, but there was no effect in uninduced cells. TrkA ability to induce γH2AX production was significantly downregulated by both K-252a and GW441756 in the absence of DNA damage inducer. In addition, it was also suppressed by K-252a during DNA damage by doxorubicin treatment, but not by GW441756 [2].

[Related Catalog]:

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Trk Receptor

Research Areas >> Cancer

[References]

[1]. Wood ER, Kuyper L, Petrov KG, Discovery and in vitro evaluation of potent TrkA kinase inhibitors: oxindole and aza-oxindoles. Bioorg Med Chem Lett. 2004 Feb 23;14(4):953-7.

[2]. Eun Joo Jung, Choong Won Kim, Deok Ryong Kim. Cytosolic accumulation of γH2AX is associated with tropomyosin-related kinase A-induced cell death in U2OS cells. Exp Mol Med. 2008 June 30; 40(3): 276-285.

[Related Small Molecules]

Entrectinib | LOXO-101 | ANA-12 | LM22B 10 | Repotrectinib | GNF-5837 | Altiratinib | LM22A-4 | Selitrectinib (LOXO-195) | Tyrphostin AG 879 | Belizatinib | Tavilermide | AZ-23 | CH7057288 | CE-245677

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
568.0±50.0 °C at 760 mmHg

[ Molecular Formula ]:
C₁₇H₁₃N₃O

[ Molecular Weight ]:
275.305

[ Flash Point ]:
297.3±30.1 °C

[ Exact Mass ]:
275.105865

[ PSA ]:
46.92000

[ LogP ]:
2.90

[ Appearance of Characters ]:
light yellow solid

[ Vapour Pressure ]:
0.0±1.6 mmHg at 25°C

[ Index of Refraction ]:
1.708

[ Storage condition ]:
Store at RT

Related Compounds

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