Thieno[3,2-d]pyriMidin-4-aMine, N-[(1S)-2-[4-[(3,4-dichlorophenyl)sulfonyl]-1-piperazinyl]-1-Methylethyl]-7-Methyl- Chemical Properties

Boiling point:

684.6±65.0 °C(Predicted)

Density 

1.453±0.06 g/cm3(Predicted)

storage temp. 

2-8°C(protect from light)

solubility 

DMF: 30 mg/ml; DMSO: 30 mg/ml; Ethanol: 30 mg/ml; Ethanol:PBS (pH 7.2)(1:2): 0.33 mg/ml

form 

Powder

pka

6.52±0.10(Predicted)

color 

White to off-white

Thieno[3,2-d]pyriMidin-4-aMine, N-[(1S)-2-[4-[(3,4-dichlorophenyl)sulfonyl]-1-piperazinyl]-1-Methylethyl]-7-Methyl- Usage And Synthesis

Description

LPA₂ antagonist 1 is an antagonist of lysophosphatidic acid receptor 2 (LPA₂; IC₅₀ = 17 nM). It is selective for LPA₂ over LPA₁ and LPA₃ (IC₅₀s = >50 μM). LPA₂ antagonist 1 inhibits HGF-induced phosphorylation of ERK and proliferation of HCT116 colon cancer cells in a concentration-dependent manner.

Uses

N-[(2S)-1-[4-(3,4-Dichlorophenyl)sulfonylpiperazin-1-yl]propan-2-yl]-7-methylthieno[3,2-d]pyrimidin-4-amine is a Lpa2 protein antagonists.

References

[1] HILARY P. BECK . Discovery of potent LPA2 (EDG4) antagonists as potential anticancer agents[J]. Bioorganic & Medicinal Chemistry Letters, 2008, 18 3: Pages 1037-1041. DOI: 10.1016/j.bmcl.2007.12.024