Biological Activity
ATP-competitive inhibitor of IGF1R (IC50 in the range of 0.1-0.2 μM). Also inhibits c-Kit kinase activity (IC50 in the range of 3-5 μM). Exhibits a synergistic effect with Imatinib, enhancing the sensitivity of multiple small cell lung cancer cell lines to the chemotherapeutics etoposide (Cat. No. 1226) and carboplatin (Cat. No. 2626).
Compound Libraries
NVP ADW 742 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox II. Find out more about compound libraries available from Tocris.
Technical Data
M. Wt | 453.58 |
Formula | C28H31N5O |
Storage | Store at -20°C |
Purity | ≥99% (HPLC) |
CAS Number | 475488-23-4 |
PubChem ID | 9825149 |
InChI Key | LSFLAQVDISHMNB-UHFFFAOYSA-N |
Smiles | NC1=NC=NC2=C1C(C4=CC(OCC5=CC=CC=C5)=CC=C4)=CN2[C@@H]3C[C@@H](CN6CCCC6)C3 |
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 | 22.68 | 50 | |
ethanol | 4.54 | 10 |
Preparing Stock Solutions
The following data is based on the product molecular weight 453.58. 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 | 2.2 mL | 11.02 mL | 22.05 mL |
5 mM | 0.44 mL | 2.2 mL | 4.41 mL |
10 mM | 0.22 mL | 1.1 mL | 2.2 mL |
50 mM | 0.04 mL | 0.22 mL | 0.44 mL |
Molarity Calculator
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Product Datasheets
References
References are publications that support the products' biological activity.
Warshamana-Greene et al (2005) The insulin-like growth factor-I receptor kinase inhibitor, NVP-ADW742, sensitizes small cell lung cancer cell lines to the effects of chemotherapy. Clin.Cancer Res. 11 1563 PMID: 15746061
Warshamana-Greene et al (2004) The insulin-like growth factor-I (IGF-I) receptor kinase inhibitor NVP-ADW742, in combination with STI571, delineates a spectrum of dependence of small cell lung cancer on IGF-I and stem cell factor signaling. Mol.Cancer Ther. 3 527 PMID: 15141010
Zhou et al (2011) The insulin-like growth factor-I receptor kinase inhibitor NVP-ADW742 sensitizes medulloblastoma to the effects of chemotherapy. Oncol. Rep. 25 1565 PMID: 21455580
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