TP-5801(TP 5801, TP5801) CAS No.: 2574474-81-8

Chemical Structure : TP-5801

CAS No.: 2574474-81-8

 

TP-5801(TP 5801, TP5801)

Catalog No.: URK-V2472 Only Used For Lab.

TP-5801 is a selective and potent small molecule inhibitor of the receptor tyrosine kinase Axl.

Biological Activity

TP-5801 is a new selective and potent small molecule inhibitor of the receptor tyrosine kinase Axl. Axl is a transmembrane receptor and a member of the TAM (Tyro3, Axl, Mer) family of receptor tyrosine kinases. It plays a key role in a variety of biological processes such as cell growth, differentiation, migration, and apoptosis. However, Axl overexpression has been associated with tumor progression, metastasis, and resistance to chemotherapy, making it an attractive target for cancer therapy.
TP-5801 is identified as a highly potent Axl inhibitor in a high-throughput screening of a library of small molecule candidates. It selectively inhibits Axl kinase activity with an IC50 of 13 nM and displays excellent kinome-wide selectivity and minimal off-target effects. In preclinical studies, TP-5801 has shown efficacy in inhibiting tumor growth and metastasis in several cancer models, including triple-negative breast cancer, ovarian cancer, and lung cancer.
The mechanism of TP-5801 involves binding to the kinase domain of Axl and inhibiting its phosphorylation, thereby suppressing downstream signaling pathways such as PI3K/AKT and MAPK/ERK. This leads to decreased cell proliferation, migration, and invasion, and increased apoptosis in cancer cells.

Physicochemical Properties

References

1. Holland SJ, Pan A, Franci C, et al. R428, a selective small molecule inhibitor of Axl kinase, blocks tumor spread and prolongs survival in models of metastatic breast cancer. Cancer Res. 2010;70(4):1544-1554. doi:10.1158/0008-5472.CAN-09-4019

2. Gay CM, Balaji K, Byers LA. Giving AXL the axe: targeting AXL in human malignancy. Br J Cancer. 2017;116(4):415-423. doi:10.1038/bjc.2016.421.

URK-V2472_COA

URK-V2472_SDS

URK-V2472_TDS

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