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...