Catalog No.S1088 Synonyms: GSK 552602A, ADW742
Molecular Weight(MW): 453.58
NVP-ADW742 is an IGF-1R inhibitor with IC50 of 0.17 μM, >16-fold more potent against IGF-1R than InsR; little activity to HER2, PDGFR, VEGFR-2, Bcr-Abl and c-Kit.
Cited by 9 Publications
3 Customer Reviews
HER3 plus IGF-1R up-regulation contribute to enhanced SKOV3/T cell proliferation. (A) SKOV3/T cells transfected with HER3 or control shRNA were treated with 2 μM NVP-ADW742 (NVP) followed by SRB assay. Values are mean ± SD from 3 independent experiments. **P < 0.01, NVP-ADW742 treated group or HER3 shRNA group vs. control. (B) SKOV3/T cells transfected with HER3 or control shRNA were treated with or without 2 μM NVP-ADW742 (NVP) and their cell cycle distribution determined by ﬂow cytometry. The data are representative of 3 independent experiments.
Biochem Biophys Res Commun 2013 436(4), 740-5. NVP-ADW742 purchased from Selleck.
Relative cell viability of 72 hours of treatment with IGF1R/IR inhibitors. a-b OSI-906 does not inhibit chondrosarcoma cell viability, even in the presence of IGF1. c-d IGF1R inhibitors NVP-ADW742 and GSK1838705A do not inhibit chondrosarcoma cell viability
BMC Cancer, 2016, 16:475. NVP-ADW742 purchased from Selleck.
Reporter activity was determined upon co-transfection of Top-Flash (TOP) or Fop-Flash (FOP) and Renilla plasmids into HepG2 cells along with IGF1R-GFP (WT) and IGF1R tyrosine kinase inhibitor NVP-ADW742 at the indicated concentrations with 0.01% DMSO under basal conditions. The data shown represents the average ± SD of three experiments. ***P < 0.001.
Biochim Biophys Acta, 2018, 1865(6):920-931. NVP-ADW742 purchased from Selleck.
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Choose Selective IGF-1R Inhibitors
|Description||NVP-ADW742 is an IGF-1R inhibitor with IC50 of 0.17 μM, >16-fold more potent against IGF-1R than InsR; little activity to HER2, PDGFR, VEGFR-2, Bcr-Abl and c-Kit.|
NVP-ADW742 exhibits a 6-fold greater selectivity for IGF-1R versus InsR with IC50 of 2.8 μM; minimal inhibitory activity against c-Kit, HER1, PDGFR, VEGFR2, or Bcr-Abl p210 with IC50 greater than 5 μM. NVP-ADW742 significantly inhibits the serum-stimulated cell proliferation in a variety of tumor cell lines in dose-dependent manner, with IC50 values of 0.1-0.5 μM for the multiple myeloma (MM) cell lines, and the antitumor effects on MM cells can not be overcome by the co-culture with BMSCs. NVP-ADW742 also abrogates the responsiveness of tumor cells to IL-6 in the presence of serum. In addition, NVP-ADW742 is active against MM cell lines with resistance to conventional (cytotoxic chemotherapy, dexamethasone) or investigational (thalidomide, CC-5013, TRAIL/Apo2L, PS-341) anticancer agents, as well as primary tumor cells from MM patients with multi-drug-resistant disease. NVP-ADW742 decreases the production of VEGF by tumor cells and bone marrow stromal cells, and suppresses the IGF-1-induced secretion of VEGF by various tumor types such as thyroid cancer cells or MM cells. IGF-1R inhibition by NVP-ADW742 (0.75 μM) sensitizes MM cells or prostate cancer cells to other anticancer agents such as doxorubicin, melphalan, dexamethasone, TRAIL/Apo2L, or PS-341. 
|In vivo||Administration of NVP-ADW742 at 10 mg/kg twice daily significantly inhibits tumor growth, prolongs survival, and enhances the antitumor effect of cytotoxic chemotherapy melphalan in the mice model of diffuse MM. |
Cellular kinase activity assay:The IC50 value for the effect of NVP-ADW742 on the autophosphorylation of IGF-1R is determined at the cellular level in the presence of increasing concentrations of NVP-ADW742, using 96-well “Capture ELISAs” assays. Briefly, NWT-21 cells are seeded into 96-well tissue culture plates in complete growth medium and grown to 70-80% confluency, and are then starved for 24 hours in 0.5% FCS medium. Subsequently, cells are incubated for 90 minutes in the presence of NVP-ADW742 followed by the stimulation with of IGF-I (10 ng/mL) for 10 minutes at 37 °C. Subsequently, the cells are washed twice with ice-cold PBS and lysed at 4 °C with 50 μL/well RIPA-buffer (50 mM Tris-HCl, pH 7.2, 120 mM NaCl, 1 mM EDTA, 6 mM EGTA, 1% NP-40, 20 mM NaF, 1 mM benzamidine, 15 mM sodium pyrophosphate, 1 mM PMSF and 0.5 mM Na3VO4). The lysates from each experiment are then transferred to black ELISA plates precoated with capture antibodies specific for IGF-1R. After capture by the antibodies, lysates are mixed with 40 μL of an alkaline phosphatase (AP) labelled anti-phosphotyrosine Ab (PY20(AP) diluted to 0.2 μg/mL in RIPA buffer, and incubated overnight at 4 °C. After washing (PBST) and incubation for 45 minutes at RT with the luminescent AP-substrate CDPStar RTU with Emerald II (90 μL/well), luminescence is measured using a Packard Top Count Scintillation Counter.
|In vitro||DMSO||10 mg/mL warmed (22.04 mM)|
|Ethanol||3 mg/mL (6.61 mM)|
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
|Synonyms||GSK 552602A, ADW742|
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