368836-72-0
Chemical Structure
LS-104
Synonym(s): Tyrene CR-4
- CAS No.: 368836-72-0
- Formula:C19H16N2O3
- Molecular Weight:320.34
IUPAC Name: (2E,4E)-N-benzyl-2-cyano-5-(3,4-dihydroxyphenyl)penta-2,4-dienamide
InChIKey: DTCCYSMPUUYHOF-LHQXNBGVSA-N
SMILES: OC1=C(O)C=CC(/C=C/C=C(C#N)/C(NCC2=CC=CC=C2)=O)=C1
Biological Activity: LS-104 (Tyrene CR-4) is a non-ATP-competitive kinase inhibitor against JAK2, Bcr-Abl and FLT3. LS-104 potently induces apoptosis in JAK2V617F-positive cells and inhibits JAK2 autophosphorylation and downstream signal transduction. LS-104 also inhibits proliferation and induces potent cytotoxic effects in FLT3 expressing leukemic cells. LS-104 is a hydroxystyryl-acrylonitrile compound, which is promising for research of myeloproliferative disorders and refractory/relapsed hematologic malignancies[1][2].
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LS-104 | LS-104 (Tyrene CR-4) is a non-ATP-competitive kinase inhibitor against JAK2, Bcr-Abl and FLT3. LS-104 potently induces apoptosis in JAK2V617F-positive cells and inhibits JAK2 autophosphorylation and downstream signal transduction. LS-104 also inhibits proliferation and induces potent cytotoxic effects in FLT3 expressing leukemic cells. LS-104 is a hydroxystyryl-acrylonitrile compound, which is promising for research of myeloproliferative disorders and refractory/relapsed hematologic malignancies. | |||||||||||||||||||||
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- [1]. Lipka DB, et al. LS104, a non-ATP-competitive small-molecule inhibitor of JAK2, is potently inducing apoptosis in JAK2V617F-positive cells. Mol Cancer Ther. 2008 May;7(5):1176-84. [Content Brief]
- [2]. Kasper S, et al. The kinase inhibitor LS104 induces apoptosis, enhances cytotoxic effects of chemotherapeutic drugs and is targeting the receptor tyrosine kinase FLT3 in acute myeloid leukemia. Leuk Res. 2008 Nov;32(11):1698-708. [Content Brief]
Keywords
