Catalog No.S1088 Synonyms: GSK 552602A, ADW742

For research use only.

NVP-ADW742 (GSK 552602A) 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 Chemical Structure

CAS No. 475488-23-4

Selleck's NVP-ADW742 has been cited by 19 publications

Purity & Quality Control

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Biological Activity

Description NVP-ADW742 (GSK 552602A) 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.
IGF-1R [1]
(cellular autophosphorylation assays)
0.17 μM
In vitro

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. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Sf21 cells MWrGeY5kfGmxbjDhd5NigQ>? MoCzTY5pcWKrdHnvckBw\iCqdX3hckBKT0ZzUjDlfJBz\XO|ZXSgbY4hW2Z{MTDj[YxteyCkeTD0bY1mNXKnc3;seoVlKG[udX;y[ZNk\W6lZTDhd5NigSxiSVO1NF0xNjB5ODFOwG0> NEKzXGIyPzZ6OUC3PC=>
MiaPaCa2 cells NE\U[WNHfW6ldHnvckBie3OjeR?= NGDkTFBKdmirYnn0bY9vKEmJRkHSJJBpd3OyaH;yfYxifGmxbjDpckBpfW2jbjDNbYFR[UOjMjDj[YxteyxiSVO1NF0xNjN{MzFOwG0> MXSxO|Y5QTB5OB?=
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. [1]

Protocol (from reference)

Kinase Assay:[1]
  • 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.

Cell Research:[1]
  • Cell lines: MM-1S, MM-1R, RPMI-8226/S, OPM-1, OCI-My5, SKMM2, KMS-12-BM, XG-1, L363, S6B45 cells and et al.
  • Concentrations: Dissolved in DMSO, final concentrations ~ 10 μM
  • Incubation Time: 48 hours
  • Method: Cells are exposed to various concentrations of NVP-ADW742 for 48 hours in the presence or absence of serum. Cell survival is examined using MTT assay.
Animal Research:[1]
  • Animal Models: Male SCID/NOD mice injected i.v. with MM-1S-Luc+ human MM cells
  • Dosages: 10 mg/kg twice daily
  • Administration: Injection i.p. or oral gavage

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 453.58


CAS No. 475488-23-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CCN(C1)CC2CC(C2)N3C=C(C4=C(N=CN=C43)N)C5=CC(=CC=C5)OCC6=CC=CC=C6

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