NVP-ADW742 b

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

NVP-ADW742 是一种 IGF-1R 抑制剂，IC50 为 0.17 μM，抗 IGF-1R 的效力是 InsR 的 16 倍；对 HER2、PDGFR、VEGFR-2、Bcr-Abl 和 c-Kit 几乎没有活性。

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.

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). Cell Viability Assay Cell Line:A panel of cell lines from multiple myeloma (MM), other hematologic malignancies and solid tumors Concentration:0.1, 0.5, 1, 2, 5, 10 μM Incubation Time:72 hours Result:Dose-dependently inhibited serum-induced cell growth in all cell lines.Western Blot Analysis Cell Line:NWT-21 cells Concentration:0.1, 0.3, 1, 3, 9 μM Incubation Time:20 min Result:Blocked IGF-1-induced phosphorylation of IGF-1R and its known downstream target Akt at submicromolar concentrations.

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.

ADW | GSK 552602A | ADW742

Angiogenesis

IGF-1R

IGF-1R

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475488-23-4

453.58

C28H31N5O

>98% (HPLC)

DMSO:10 mg/mL (22.04 mM) warmed;Ethanol:3 mg/mL (6.61 mM);Water:<1 mg/mL

C1CCN(C1)CC2CC(C2)N3C=C(C4=C3N=CN=C4N)C5=CC(=CC=C5)OCC6=CC=CC=C6

5-(3-(benzyloxy)phenyl)-7-((1r3r)-3-(pyrrolidin-1-ylmethyl)cyclobutyl)-7H-pyrrolo[23-d]pyrimidin-4-amine

(-20℃)

With Ice Pack

≥ 2 years