2'-THIOADENOSINE

Names

[ Name ]:
2'-THIOADENOSINE

[Synonym ]:
2'-Thioadenosine

Biological Activity

[Description]:

2'-Thioadenosine (PD157432) is a selective and irreversible inhibitor of ErbB-1 and ErbB-2, with an IC50 of 45 µM for ErbB-2. 2'-Thioadenosine covalently inactivates ErbB-1 via modification of a cysteine residue at the active site[1].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> JAK/STAT Signaling >> EGFR

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> EGFR

[Target]

ErbB1

ErbB2:45 μM (IC50)

[In Vitro]

2'-Thioadenosine (50 µM) 对 FGF，PDGF 和胰岛素受体酪氨酸激酶没有活性[1]。 2'-Thioadenosine 使 ErbB-1 共价失活，这种失活可被 1 mM Dithiothreitol 逆转[1]。

[References]

[1]. Singh J, et, al. Structure-based design of a potent, selective, and irreversible inhibitor of the catalytic domain of the erbB receptor subfamily of protein tyrosine kinases. J Med Chem. 1997 Mar 28;40(7):1130-5.

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₀H₁₃N₅O₃S

[ Molecular Weight ]:
283.31

[ Exact Mass ]:
283.07400

[ PSA ]:
158.11000

Related Compounds

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