ADW742 - CAS 475488-23-4
Not Intended for Therapeutic Use. For research use only.
Category:
Inhibitor
Product Name:
ADW742
Catalog Number:
475488-23-4
Synonyms:
NVP-ADW742; NVP-ADW742; ADW 742; GSK 552602A.
CAS Number:
475488-23-4
Description:
NVP-ADW742 is a novel small weight molecular inhibitor of IGF-IR with potential anticancer activity. NVP-ADW742 inhibited IGF-IR-mediated proliferation with an IC50 of 11.12 µmol/l. NVP-ADW742 induced early suppression of Akt, P38 and GSK-3β phosphorylation. NVP-ADW742 was found to suppresse survival and resistance to chemotherapy in acute myeloid leukemia cells.
COA:
Inquire
MSDS:
Inquire
Targets:
IGF-1R
Current Developer:
Novartis Pharmaceuticals.
Chemical Structure
CAS 475488-23-4 ADW742

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Reference Reading


1.The insulin-like growth factor-I receptor kinase inhibitor NVP-ADW742 sensitizes medulloblastoma to the effects of chemotherapy.
Zhou H1, Rao J, Lin J, Yin B, Sheng H, Lin F, Zhang N, Yang L. Oncol Rep. 2011 Jun;25(6):1565-71. doi: 10.3892/or.2011.1233. Epub 2011 Mar 23.
Medulloblastoma is the most common malignant tumor of the central nervous system in children. The insulin-like growth factor-I receptor (IGF-IR) is an important growth factor for medulloblastoma. The novel IGF-I receptor (IGF-IR) kinase inhibitor NVP-ADW742 has in vitro activity against tumors. Daoy cells were treated with NVP-ADW742 combined with temozolomide, which is commonly used in the chemotherapy of medulloblastoma. The effects on proliferation were assayed by CCK-8 assay. Cell cycle status and apoptosis were assayed by FACS analysis. The IGF-IR signaling pathway was analyzed by RT2 Profiler™ PCR arrays and Western blotting. NVP-ADW742 inhibited IGF-IR-mediated proliferation with an IC50 of 11.12 µmol/l. The PCR array data suggested that 14 genes were down-regulated at the mRNA level after NVP-ADW742 treatment. Western blot analysis suggested that NVP-ADW742 induced early suppression of Akt, P38 and GSK-3β phosphorylation, as well as a decrease in the intracellular levels of PI3K, Akt, P38, GSK-3β and Bcl-2.
2.The insulin-like growth factor-1 receptor kinase inhibitor, NVP-ADW742, suppresses survival and resistance to chemotherapy in acute myeloid leukemia cells.
He Y1, Zhang J, Zheng J, Du W, Xiao H, Liu W, Li X, Chen X, Yang L, Huang S. Oncol Res. 2010;19(1):35-43.
Deregulation of insulin-like growth factor-1 receptor (IGF-1R) is closely associated with malignant transformation and tumor cell survival in various cancers. We found that IGF-1R expression level in leukemia cells positively correlated with the percentage of blast in bone marrow from de novo acute myeloid leukemia (AML) patients. Moreover, we showed that NVP-ADW742, a novel small weight molecular inhibitor of IGF-IR, could induce apoptosis in both HL-60 cell line and primary AML blasts. However, no significant alteration of cell cycle was observed in HL-60 cells. Further studies revealed that NVP-ADW742 induced Akt dephosphorylation, which might subsequently induce p38 phosphorylation and decrease antiapoptotic protein Bcl-2 expression in HL-60 cells. Finally, we demonstrated that NVP-ADW742 could synergize with Ara-C to induce the kill in a subset of drug-resistant AML specimens. We suggested that IGF-lR targeting might be therapeutically beneficial for some AML patients.