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编 号:F364681
分子式:C28H31N5O
分子量:453.58
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10mM*1mL in DMSO
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1mg
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2mg
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5mg
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10mg
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50mg
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生物活性:
NVP-ADW742 (ADW742) is an orally active, selective IGF-1R tyrosine kinase inhibitor with an IC50 of 0.17 μM. NVP-ADW742 inhibits insulin receptor (InsR) with an IC50 of 2.8 μM. NVP-ADW742 induces pleiotropic antiproliferative/proapoptotic biologic sequelae in tumor cells.

体内研究:
NVP-ADW742 (ADW742; 10 mg/kg for IP or 50 mg/kg for orally; twice daily for 19 days) significantly suppresses tumor growth and prolongs the survival of mice. Animal Model:6- to 8-week-old male SCID/NOD mice with diffuse skeletal lesions of luciferase-expressing MM cells
Dosage:10 mg/kg (IP) or 50 mg/kg (orally)
Administration:IP or orally; twice daily for 19 days
Result:Significantly suppressed tumor growth and prolonged the survival of mice.

体外研究:
NVP-ADW742 (ADW742; 0.1-10 μM; 72 hours) dose-dependently inhibits serum-induced cell growth in all cell lines. NVP-ADW742 (0.1-9 μM; 20 min) blocks IGF-1-induced phosphorylation of IGF-1R and its known downstream target Akt at submicromolar concentrations. NVP-ADW742 has much higher IC50 values for other kinases (IC50>10 μM for HER2, PDGFR, VEGFR-2, or Bcr-Abl p210; and IC50>5 μM for c-Kit).
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