NVP-ADW742

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 17 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.
Targets
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 MUjGeY5kfGmxbjDhd5NigQ>? NFHIV3VKdmirYnn0bY9vKG:oIHj1cYFvKEmJRkHSJIV5eHKnc4Pl[EBqdiCVZkKxJINmdGy|IHL5JJRqdWVvcnXzc4x3\WRiZnz1c5Jme2OnbnPlJIF{e2G7LDDJR|UxRTBwMEe4JO69VQ>? MnzCNVc3QDlyN{i=
MiaPaCa2 cells MnrYSpVv[3Srb36gZZN{[Xl? MWfJcohq[mm2aX;uJGlITjGUIIDoc5NxcG:{eXzheIlwdiCrbjDoeY1idiCPaXHQZWNiOiClZXzsd{whUUN3ME2wMlMzOyEQvF2= M2LsTlE4Pjh7MEe4
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.
  • (Only for Reference)
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
  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO 10 mg/mL warmed
(22.04 mM)
Ethanol 3 mg/mL
(6.61 mM)
Water Insoluble

* 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.

Chemical Information

Molecular Weight 453.58
Formula

C28H31N5O

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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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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