TC-S 7003

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Cat.No. 3567 - TC-S 7003 | C31H30N8O | CAS No. 847950-09-8
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% (HPLC)
Datasheet
Citations
Reviews
Literature

Biological Activity

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.

Compound Libraries

TC-S 7003 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox I. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 530.62
Formula C31H30N8O
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 847950-09-8
PubChem ID 11785878
InChI Key BHJJWVDKNXABFS-UHFFFAOYSA-N
Smiles O=C3N(C4=C(C)C=CC=C4C)C1=NC7=C(C=CC=C7)N1C2=NC(NC5=CC=C(N6CCN(C)CC6)C=C5)=NC=C23

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 53.06 100
ethanol 5.31 10 with gentle warming

Preparing Stock Solutions

The following data is based on the product molecular weight 530.62. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.88 mL 9.42 mL 18.85 mL
5 mM 0.38 mL 1.88 mL 3.77 mL
10 mM 0.19 mL 0.94 mL 1.88 mL
50 mM 0.04 mL 0.19 mL 0.38 mL

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References

References are publications that support the biological activity of the product.

Martin et al (2008) 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 J.Med.Chem. 51 1637 PMID: 18278858


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Keywords: TC-S 7003, TC-S 7003 supplier, Lck, kinases, inhibitors, inhibits, lymphocyte, specific, Src, Kinases, 3567, Tocris Bioscience

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