Biological Activity
Substance P analog that is a broad spectrum neuropeptide antagonist and antiproliferative agent. Blocks Swiss 3T3 cell growth induced by vasopressin, gastrin-releasing peptide and bradykinin. Inhibits neuropeptide-dependent and -independent proliferation of small cell lung cancer in vitro; activates JNK and stimulates apoptosis. Inhibits growth of SCLC xenografts in mice in vivo.
Technical Data
| M. Wt | 951.2 |
| Formula | C49H66N12O6S |
| Sequence |
RWFWLM (Modifications: Trp-2 = D-Trp, Phe-3 = N-Methyl-Phe, Trp-5 = D-Trp, Met-7 = C-terminal amide) |
| Storage | Desiccate at -20°C |
| CAS Number | 115150-59-9 |
| PubChem ID | 163960 |
| InChI Key | CUCSSYAUKKIDJV-FAXBSAIASA-N |
| Smiles | [H]N[C@@H](CCCNC(N)=N)C(=O)N[C@H](CC1=CNC2=C1C=CC=C2)C(=O)N(C)[C@@H](CC1=CC=CC=C1)C(=O)N[C@H](CC1=CNC2=C1C=CC=C2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(N)=O |
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
| Solubility | Soluble to 1 mg/ml in water |
Preparing Stock Solutions
The following data is based on the product molecular weight 951.2. 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 | 1.05 mL | 5.26 mL | 10.51 mL |
| 5 mM | 0.21 mL | 1.05 mL | 2.1 mL |
| 10 mM | 0.11 mL | 0.53 mL | 1.05 mL |
| 50 mM | 0.02 mL | 0.11 mL | 0.21 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Woll and Rozengurt (1990) A neuropeptide antagonist that inhibits the growth of small cell lung cancer in vitro. Cancer Res. 50 3968 PMID: 1693879
Langdon et al (1992) Broad spectrum neuropeptide antagonists inhibit the growth of small cell lung cancer in vivo. Cancer Res. 52 4554 PMID: 1379515
MacKinnon et al (2000) [Arg6, D-Trp7,9, NmePhe8]-Substance P (6-11) (antagonist G) induces AP-1 transcription and sensitizes cells to chemotherapy. Br.J.Cancer 83 941 PMID: 10970698
Keywords: Antagonist G, supplier, Broad, spectrum, neuropeptide, receptors, antagonists, Tachykinin, Non-Selective, Neurokinin, AntagonistG, neuropeptides, [Arg6,D-Trp7,9,N-MePhe8]-Substance, P(6-11), Other, Tachykinin, Other, Peptide, Receptors, Other, Tachykinin, Tocris Bioscience
