TC-S 7003

Catalog #: 3567 Datasheet / COA / SDS

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TC-S 7003 | CAS No. 847950-09-8 | Src Family Kinase Inhibitors

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Description: Potent Lck inhibitor

Chemical Name: 6-(2,6-Dimethylphenyl)-2-[[4-(4-methyl-1-pyrimido[5',4':5,6]pyrimido[1,2-a]benzimidazol-5(6H)-one

Purity: ≥98%

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Biological Activity

TC-S 7003 is a potent inhibitor of lymphocyte specific kinase (Lck). IC₅₀ values are 0.007, 0.021, 0.042 and 0.20 μM for Lck, Lyn, Src and Syk kinases respectively. Displays >1000-fold selectivity for Lck over MAPK, CDK and RSK family representatives. Inhibits T cell proliferation in vitro and inhibits arthritis in two in vivo models. Orally active.

Technical Data

M.Wt:

530.62

Formula:

C₃₁H₃₀N₈O

Solubility:

Soluble to 100 mM in DMSO and to 10 mM in ethanol with gentle warming

Purity:

≥98%

Storage:

Store at -20°C

CAS No:

847950-09-8

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

Structure-based design of novel 2-amino-6-phenyl-pyrimido[5',4':5,6]pyrimido[1,2-a]benzimidazol-5(6H)-ones as potent and orally active inhibitors of lymphocyte specific kinase (Lck): synthesis, SAR, and in vivo anti-inflammatory
Martin et al.
J.Med.Chem., 2008;51:1637

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