NVP-ADW742(ADW742)
NVP-ADW742
CAS: 475488-23-4
Molecular Formula: C28H31N5O
NVP-ADW742(ADW742) - Names and Identifiers
NVP-ADW742(ADW742) - Physico-chemical Properties
| Molecular Formula | C28H31N5O |
| Molar Mass | 453.58 |
| Density | 1.31 |
| Boling Point | 677.5±55.0 °C(Predicted) |
| Solubility | DMSO:10 mg/mL heat (22 mM),Water:<1 mg/mL (<1 mM),Ethanol:3 mg/mL (6 mM) |
| pKa | 10.00±0.20(Predicted) |
| Storage Condition | -20℃ |
| Use | An IGF-1R inhibitor with IC50 of 0.17 μM |
| In vitro study | NVP-ADW742 is more than 6 times more selective at IGF-1R than at insulin receptor (InsR), with an IC50 of 2.8 μm, and has the lowest inhibitory activity at c-Kit, HER1, PDGFR, VEGFR-2, or Bcr-Abl p210, IC50>5-10 μm, consistent with significant inhibition of IGF-1-induced phosphorylation of IGF-1R and its downstream target, Akt. NVP-ADW742 significantly inhibited the proliferation of a variety of cells stimulated by serum in a dose-dependent manner, with IC50 of 0.1-0.5 μm in multiple myeloma (MM) cell lines, co-culture with BMSCs could not overcome the anticancer effect on MM. In the presence of serum, NVP-ADW742 also abrogated the tumor cell response to IL-6. In addition, NVP-ADW742 effectively acts on MM cell lines against conventional anti-cancer agents (toxic chemotherapeutic agents, Dexamethasone) or anti-cancer agents for research (Thalidomide, CC-5013, TRAIL/Apo2L, PS-341), it also effectively acts on primary tumor cells in MM patients who are resistant to multiple drugs. NVP-ADW742 acts on tumor cells and bone marrow stromal stem cells, reduces VEGF production, and inhibits IGF-1-induced VEGF secretion in a variety of tumor types, such as thyroid cancer cells and MM cells. The 0.75 μm NVP-ADW742 inhibits IGF-1R and also sensitizes MM cells or prostate cancer cells to other anti-cancer agents such as Doxorubicin, Melphalan, Dexamethasone, TRAIL/Apo2L, or PS-341. |
| In vivo study | NVP-ADW742 treatment of a mouse model with diffusion MM at a dose of 10 mg/kg twice daily significantly inhibited tumor growth, prolonged life, and enhanced anti-cancer effects. |
NVP-ADW742(ADW742) - Introduction
NVP-ADW742 is a IGF-1R inhibitor with IC50 of 0.17 μM, which is more than 16 times stronger on IGF-1R than on InsR. It has little activity on HER2, PDGFR, VEGFR-2, Bcr-Abl and c-Kit.
Last Update：2022-10-16 17:41:40
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CAS: 475488-23-4
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CAS: 475488-23-4
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
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