Biological Activity
Orally active Ca2+ channel blocker; inhibits K+- and carbachol-stimulated Ca2+ influx (IC50 values are 500 and 935 nM respectively). Exhibits antiproliferative, antiangiogenic and antimetastatic activity in vivo and displays selectivity towards numerous mismatch repair-deficient tumor cell lines in vitro.
Technical Data
| M. Wt | 424.67 |
| Formula | C17H12Cl3N5O2 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 99519-84-3 |
| PubChem ID | 108144 |
| InChI Key | WNRZHQBJSXRYJK-UHFFFAOYSA-N |
| Smiles | ClC1=CC=C(C(C2=C(Cl)C=C(CN3N=NC(C(N)=O)=C3N)C=C2Cl)=O)C=C1 |
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 | 42.47 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 424.67. 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 | 2.35 mL | 11.77 mL | 23.55 mL |
| 5 mM | 0.47 mL | 2.35 mL | 4.71 mL |
| 10 mM | 0.24 mL | 1.18 mL | 2.35 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.47 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Hupe et al (1991) The inhibition of receptor-mediated and voltage-dependent calcium entry by the antiproliferative L-651,582 J.Biol.Chem. 266 10136 PMID: 1645340
Yang et al (2008) Selective sensitivity to carboxyamidotriazole by human tumor cell lines with DNA mismatch repair deficiency. Int.J.Cancer. 123 258 PMID: 18464258
Felder et al (1991) The antiproliferative and antimetastatic compound L651582 inhibits muscarinic acetylcholine receptor-stimulated calcium influx and arachidonic acid release. J.Pharm.Exp.Ther. 257 967 PMID:
Keywords: L-651,582, supplier, Ca2+, channel, blockers, Calcium, CaV, Channels, voltage-gated, voltage-dependent, L651582, Carboxyamidotriazole, Voltage-gated, Calcium, Channels, Voltage-gated, Calcium, Channels, Tocris Bioscience
