| NVP-ADW742Selective IGF-1R inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
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- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
| Description | NVP-ADW742 is an inhibitor of IGF-1R with an IC50 value of 0.17 μM. | |||||
| Targets | IGF-1R | |||||
| IC50 | 0.17 μM | |||||
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| Cas No. | 475488-23-4 | SDF | Download SDF |
| Chemical Name | 5-(3-phenylmethoxyphenyl)-7-[3-(pyrrolidin-1-ylmethyl)cyclobutyl]pyrrolo[2,3-d]pyrimidin-4-amine | ||
| Canonical SMILES | C1CCN(C1)CC2CC(C2)N3C=C(C4=C3N=CN=C4N)C5=CC(=CC=C5)OCC6=CC=CC=C6 | ||
| Formula | C28H31N5O | M.Wt | 453.58 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| Physical Appearance | A crystalline solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
NVP-ADW742 is a novel inhibitor of IFG-1receptor (IGF-1R) kinase with the IC50 value of 0.17μM [1].
NVP-ADW742 has shown above 16-fold effective function against IGF-1R than insulin receptor (InsR). Furthermore, NVP-ADW742 has also been reported to inhibit other kinases , with the IC50 values of ＞10μM for HER2, PDGFR, VEGFR-2, or Bcr-Abl p210, and the IC50 values ＞5μM for c-Kit [1]. Besides, NVP-ADW742 combined with etoposide and carboplatin has been reported to inhibit cell growth and induce cytotoxicity by MTT assay using the small cell lung cancer (SCLC), including H526, H146, WBA and H209 cell lines. In addition, NVP-ADW742 has been revealed to completely inhibit the expression of VEGF mRNA which induced by IGF-I in H526 cells [2].
References:[1] Mitsiades CS1, Mitsiades NS, McMullan CJ, Poulaki V, Shringarpure R, Akiyama M, Hideshima T, Chauhan D, Joseph M, Libermann TA, García-Echeverría C, Pearson MA, Hofmann F, Anderson KC, Kung AL. Inhibition of the insulin-like growth factor receptor-1 tyrosine kinase activity as a therapeutic strategy for multiple myeloma, other hematologic malignancies, and solid tumors .Cancer Cell. 2004 Mar; 5(3):221-30.[2]Warshamana-Greene GS1, Litz J, Buchdunger E, García-Echeverría C, Hofmann F, Krystal GW. 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. 2005 Feb 15;11(4):1563-71.
