NVP-ADW742

Names

[ Name ]:
NVP-ADW742

[Synonym ]:
ADW742
UNII:MXS2N5862L
NVP-ADW742
7H-pyrrolo[2,3-d]pyrimidin-4-amine, 5-[3-(phenylmethoxy)phenyl]-7-[trans-3-(1-pyrrolidinylmethyl)cyclobutyl]-
S1088_Selleck
5-[3-(benzyloxy)phenyl]-7-[trans-3-(pyrrolidin-1-ylmethyl)cyclobutyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine
ADW742,NVP-ADW742
5-[3-(Benzyloxy)phenyl]-7-[trans-3-(1-pyrrolidinylmethyl)cyclobutyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine
Kinome_2540
cc-532

Biological Activity

[Description]:

NVP-ADW742(ADW742; GSK 552602A ) is an selective 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.IC50 value: 0.17 uM [1]Target: IGF-1Rin 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 [1]. Pretreatment of the H526 cell line with NVP-ADW742 inhibited IGF-IR signaling and growth with IC(50) values between 0.1 and 0.4 micro M [2].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].

[Related Catalog]:

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> IGF-1R

Research Areas >> Cancer

[References]

[1]. Mitsiades CS, et 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 GS, et al. 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. 2004 May;3(5):527-35.

[Related Small Molecules]

OSI-906(Linsitinib) | BMS-754807 | Picropodophyllotoxin | NVP-AEW541 | BMS-536924 | AZD-3463 | XL228 | GSK1838705A | AG-1024 | Ginsenoside Rg5 | PQ 401 | GSK1904529A | Indirubin E804

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
677.5±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₈H₃₁N₅O

[ Molecular Weight ]:
453.579

[ Flash Point ]:
363.5±31.5 °C

[ Exact Mass ]:
453.252869

[ PSA ]:
69.20000

[ LogP ]:
5.23

[ Vapour Pressure ]:
0.0±2.1 mmHg at 25°C

[ Index of Refraction ]:
1.699

[ Storage condition ]:
-20°C

Related Compounds

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