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Submit ReviewTC-S 7003
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)
Biological Activity for TC-S 7003
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.
Compound Libraries for TC-S 7003
TC-S 7003 is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library and Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.
Technical Data for TC-S 7003
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for TC-S 7003
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 53.06 | 100 | |
| ethanol | 5.31 | 10 with gentle warming |
Preparing Stock Solutions for TC-S 7003
The following data is based on the product molecular weight 530.62. Batch specific molecular weights may vary from batch to batch due to the degree 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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Product Datasheets for TC-S 7003
References for TC-S 7003
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
If you know of a relevant reference for TC-S 7003, please let us know.
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Keywords: TC-S 7003, TC-S 7003 supplier, Lck, kinases, inhibitors, inhibits, lymphocyte, specific, Src, Kinases, 3567, Tocris Bioscience
Citations for TC-S 7003
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