VU 0364849

Names

[ CAS No. ]:
1206711-14-9

[ Name ]:
VU 0364849

[Synonym ]:
DMH2
4-(6-{4-[2-(4-Morpholinyl)ethoxy]phenyl}pyrazolo[1,5-a]pyrimidin-3-yl)quinoline
VU0364849
4-[6-[4-[2-(4-Morpholinyl)ethoxy]phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]-quinoline
Quinoline, 4-[6-[4-[2-(4-morpholinyl)ethoxy]phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]-

Biological Activity

[Description]:

A potent, specific BMP receptor activin receptor-like kinase 3 (ALK3) antaognist with Ki of 5.4 nM; also inhibits ALK6 (Ki<1 nM) and ALK2 (Ki=42.77 nM), little to no affinity for ALK4/5, BMPR2, AMPK etc.; blocks SMAD phosphorylation in vitro and in vivo, and enhances liver regeneration after partial hepatectomy.

[References]

References 1. Tsugawa D, et al. J Pharmacol Exp Ther. 2014 Dec;351(3):549-58. 2. Langenfeld E, et al. Mol Cancer. 2013 Oct 26;12(1):129. 3. Langenfeld E, et al. PLoS One. 2013 Apr 12;8(4):e61256. View Related Products by Target TGF beta Receptor (TGFBR)

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Molecular Formula ]:
C₂₇H₂₅N₅O₂

[ Molecular Weight ]:
451.520

[ Exact Mass ]:
451.200836

[ LogP ]:
2.09

[ Index of Refraction ]:
1.689

Safety Information

[ RIDADR ]:
NONH for all modes of transport

Articles

Small molecule antagonist of the bone morphogenetic protein type I receptors suppresses growth and expression of Id1 and Id3 in lung cancer cells expressing Oct4 or nestin.

Mol. Cancer 12(1) , 129, (2013)

Bone morphogenetic proteins (BMP) are embryonic morphogens that are aberrantly expressed in lung cancer. BMPs mediate cell fate decisions and self-renewal of stem cells, through transcription regulati...

Related Compounds

The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.