An LPA2 antagonist
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LPA2 Antagonist 1

Item No. 22051

Technical Information
Formal Name
N-[(1S)-2-[4-[(3,4-dichlorophenyl)sulfonyl]-1-piperazinyl]-1-methylethyl]-7-methyl-thieno[3,2-d]pyrimidin-4-amine
CAS Number
1017606-66-4
Synonyms
  • LPA2-IN-1
Molecular Formula
C20H23Cl2N5O2S2
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 30 mg/mlEthanol:PBS (pH 7.2)(1:2): 0.33 mg/ml
λmax
242, 302 nm
SMILES
ClC1=CC=C(S(N2CCN(C[C@H](C)NC3=NC=NC4=C3SC=C4C)CC2)(=O)=O)C=C1Cl
InChi Code
InChI=1S/C20H23Cl2N5O2S2/c1-13-11-30-19-18(13)23-12-24-20(19)25-14(2)10-26-5-7-27(8-6-26)31(28,29)15-3-4-16(21)17(22)9-15/h3-4,9,11-12,14H,5-8,10H2,1-2H3,(H,23,24,25)/t14-/m0/s1
InChi Key
BPRNMVDTWIHULJ-AWEZNQCLSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    LPA2 antagonist 1 is an antagonist of lysophosphatidic acid receptor 2 (LPA2; IC50 = 17 nM).1 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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Beck, H.P., Kohn, T., Rubenstein, S., et alDiscovery of potent LPA2 (EDG4) antagonists as potential anticancer agents. Bioorg. Med. Chem. Lett. 18(3), 1037-1041 (2008).