NVP-ADW742|cas 475488-23-4|Price|Buy|DC Chem

Cas No.:	475488-23-4
Chemical Name:	5-(3-(benzyloxy)phenyl)-7-((1r,3r)-3-(pyrrolidin-1-ylmethyl)cyclobutyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine
Synonyms:	ADW742
SMILES:	C1=NC(N)=C2C(C3=CC=CC(OCC4=CC=CC=C4)=C3)=CN([C@H]3C[C@H](CN4CCCC4)C3)C2=N1
Formula:	C₂₈H₃₁N₅O
M.Wt:	453.58
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

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.
Target:	IC50 value: 0.17 uM [1] Target: IGF-1R
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].
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 [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].
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

Cat. No.	Product name	Field of application
DC7052	AG-1024 (Tyrphostin)	AG-1024 (Tyrphostin) inhibits IGF-1R autophosphorylation with IC50 of 7 μM, less potent to IR with IC50 of 57 μM.
DC4105	Linsitinib(OSI-906)	OSI-906 (Linsitinib) is a selective inhibitor of IGF-1R and IR with IC50 of 35 nM and 75 nM, respectively.
DC4174	NVP-AEW541	NVP-AEW541 is a potent inhibitor of IGF-1R with IC50 of 86 nM.
DC7549	NVP-ADW742	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.
DC3126	BMS754807	BMS-754807 is a potent and reversible inhibitor of IGF-1R/IR family kinases, inhibits IGF-1R, IR, Met, TrkA and TrkB with IC50 of 1.8 nM, 1.7 nM, 5.6 nM, 7.4 nM and 4.1 nM, respectively.