475488-23-4
475488-23-4 structure
- Name: NVP-ADW742
- Chemical Name: 5-(3-phenylmethoxyphenyl)-7-[3-(pyrrolidin-1-ylmethyl)cyclobutyl]pyrrolo[2,3-d]pyrimidin-4-amine
- CAS Number: 475488-23-4
- Molecular Formula: C28H31N5O
- Molecular Weight: 453.579
- Catalog: Biochemical Inhibitor Protein tyrosine kinase
- Create Date: 2018-12-24 07:36:19
- Modify Date: 2025-08-20 19:04:00
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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.IC50 value: 0.17 uM [1]Target: IGF-1Rin 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].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].
| Name | 5-(3-phenylmethoxyphenyl)-7-[3-(pyrrolidin-1-ylmethyl)cyclobutyl]pyrrolo[2,3-d]pyrimidin-4-amine |
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| Synonyms |
ADW742
UNII:MXS2N5862L NVP-ADW742 7H-pyrrolo[2,3-d]pyrimidin-4-amine, 5-[3-(phenylmethoxy)phenyl]-7-[trans-3-(1-pyrrolidinylmethyl)cyclobutyl]- S1088_Selleck 5-[3-(benzyloxy)phenyl]-7-[trans-3-(pyrrolidin-1-ylmethyl)cyclobutyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine ADW742,NVP-ADW742 5-[3-(Benzyloxy)phenyl]-7-[trans-3-(1-pyrrolidinylmethyl)cyclobutyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine Kinome_2540 cc-532 |
| 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.IC50 value: 0.17 uM [1]Target: IGF-1Rin 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].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]. |
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| Related Catalog | |
| References |
| Density | 1.3±0.1 g/cm3 |
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| Boiling Point | 677.5±55.0 °C at 760 mmHg |
| Molecular Formula | C28H31N5O |
| Molecular Weight | 453.579 |
| Flash Point | 363.5±31.5 °C |
| Exact Mass | 453.252869 |
| PSA | 69.20000 |
| LogP | 5.23 |
| Vapour Pressure | 0.0±2.1 mmHg at 25°C |
| Index of Refraction | 1.699 |
| Storage condition | -20°C |