1312691-33-0

1312691-33-0 structure

Name: TAK-659
Chemical Name: 8QR88H79VX
CAS Number: 1312691-33-0
Molecular Formula: C₁₇H₂₁FN₆O
Molecular Weight: 344.387
Catalog: Signaling Pathways Protein Tyrosine Kinase/RTK FLT3
Create Date: 2018-06-19 07:28:58
Modify Date: 2024-01-10 19:55:58
TAK-659 is a highly potent, selective, reversible and orally available inhibitor of spleen tyrosine kinase (SYK) and fms related tyrosine kinase 3 (FLT3), with an IC50 of 3.2 nM for SYK. TAK-659 induces cell death in tumor cells but not in nontumor cells, and with potential for the treatment of chronic lymphocytic leukemia (CLL)[1][2][3][4].

Name	8QR88H79VX
Synonyms	6-{[(1R,2S)-2-Aminocyclohexyl]amino}-7-fluoro-4-(1-methyl-1H-pyrazol-4-yl)-1,2-dihydro-3H-pyrrolo[3,4-c]pyridin-3-one MFCD30829411 8QR88H79VX 3H-Pyrrolo[3,4-c]pyridin-3-one, 6-[[(1R,2S)-2-aminocyclohexyl]amino]-7-fluoro-1,2-dihydro-4-(1-methyl-1H-pyrazol-4-yl)-

Description	TAK-659 is a highly potent, selective, reversible and orally available inhibitor of spleen tyrosine kinase (SYK) and fms related tyrosine kinase 3 (FLT3), with an IC50 of 3.2 nM for SYK. TAK-659 induces cell death in tumor cells but not in nontumor cells, and with potential for the treatment of chronic lymphocytic leukemia (CLL)[1][2][3][4].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Syk Signaling Pathways >> Protein Tyrosine Kinase/RTK >> FLT3
Target	IC50: 3.2 nM (Syk)[1]
References	[1]. Lam B, et al. Discovery of TAK-659 an orally available investigational inhibitor of Spleen Tyrosine Kinase (SYK). Bioorg Med Chem Lett. 2016 Dec 15;26(24):5947-5950. [2]. Purroy N, et al. Inhibition of BCR signaling using the Syk inhibitor TAK-659 prevents stroma-mediated signaling in chronic lymphocytic leukemia cells. Oncotarget. 2017 Jan 3;8(1):742-756. [3]. Jie Yu, et al. Anti-tumor activity of TAK-659, a dual inhibitor of SYK and FLT-3 kinases, in AML models. Journal of Clinical Oncology 34, no. 15_suppl. [4]. Cen O, et al. Spleen Tyrosine Kinase Inhibitor TAK-659 Prevents Splenomegaly and Tumor Development in a Murine Model of Epstein-Barr Virus-Associated Lymphoma. mSphere. 2018 Aug 22;3(4).