AEW-541
NVP-AEW541
CAS: 475489-16-8
Molecular Formula: C27H29N5O
AEW-541 - Names and Identifiers
AEW-541 - Physico-chemical Properties
| Molecular Formula | C27H29N5O |
| Molar Mass | 439.55 |
| Density | 1.33 |
| Melting Point | 145℃ |
| Boling Point | 669.0±55.0 °C(Predicted) |
| Solubility | Chloroform (Slightly), Methanol (Slightly) |
| Appearance | powder |
| Color | white to beige |
| pKa | 9.59±0.10(Predicted) |
| Storage Condition | 2-8°C |
| In vitro study | In the purified kinase/recombinant kinase domain assay, NVP-AEW541 also inhibited InsR, Tek, Flt1 and Flt3 with IC50 of 140 nM, 530 nM, 600 nM and 420 nM, respectively. At the cellular level, the NVP-AEW541 selectivity was higher, 27-fold higher than the InsR selectivity. NVP-AEW541 inhibited IGF-I conditioned survival, soft agar, and MCF-7 cell proliferation with an IC50 of 0.162 μm, 0.105 μm, and 1.64 μm, respectively. NVP-AEW541 action on NWT-21 cells also reduced levels by p-IGF-IR and p-PKB. NVP-AEW541, the growth of TC-71 musculoskeletal sarcoma cells cultured in low serum medium and medium containing 10% FBS was inhibited. NVP-AEW541 acts on sarcoma cell lines (TC-71, SK-N-MC, SaoS-2, RD/18 and RH4) to inhibit cell cycle progression and induce cell cycle arrest in the G1 phase. NVP-AEW541 can inhibit the growth of neuroblastoma cells, IC50 is 0.4-6.8 μm. An increase in hypodiploid fragments and depletion of S and G2-M phase cells can be detected in these cells. In neuroblastoma cells, NVP-AEW541 of the IGF-IR drive was inhibited to reduce Akt phosphorylation but not Erk1 and Erk2 phosphorylation. NVP-AEW541 inhibits the growth of glioma cells and destroys the Autocrine Loop initiated by HIF1α stabilization. The latest research shows NVP-AEW541 inhibition of PC3, DU145, And 22Rv1 prostate cancer cell proliferation and activity. NVP-AEW541 action on 22Rv1 and DU415 cells but not on PC3 cells reduced levels by p-Akt and did not affect overall Akt levels, suggesting that PTEN status can determine the effectiveness of NVP-AEW541. The NVP-AEW541 induced radiosensitivity is determined by the Akt activation status. NVP-AEW541 increased H2AX phosphorylation in PC3, DU145, and 22Rv1 cells. |
| In vivo study | NVP-AEW541(50 mg/kg, oral treatment) on NWT-21 of the transplanted tumor, resulting in the abolition of the basic type and IGF-I induced receptor, also inhibited PKB and MAPK phosphorylation, T/C value of 14%. NVP-AEW541(50 mg/kg) on HTLA-230 and SK-N-BE2c of the transplanted tumor, causing tumor shrinkage, no signs of systemic toxicity. NVP-AEW541 acts on Matrigel coated cells and HTLA-230 of the transplanted tumor, which can inhibit tumor invasion. |
AEW-541 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.275 ml | 11.375 ml | 22.751 ml |
| 5 mM | 0.455 ml | 2.275 ml | 4.55 ml |
| 10 mM | 0.228 ml | 1.138 ml | 2.275 ml |
| 5 mM | 0.046 ml | 0.228 ml | 0.455 ml |
Last Update：2024-01-02 23:10:35
AEW-541 - Reference Information
| biological activity | NVP-AEW541 is an effective IGF-1R/InsR inhibitor. IC50 is 150 nM/140 nM in cell-free test, which has high effect and selectivity on IGF-1R in cell test. |
| target | TargetValue Insulin Receptor (Cell-free Assay) 0.14 μM IGF-1R (Cell-free Assay) 0.15 μM FLT3 (Cell-free Assay) 0.42 μM Tek (Cell-free Assay) 0.53 μM FLT1 (Cell-free Assay) 0.6 μM |
| Target | Value |
| Insulin Receptor (Cell-free assay) | 0.14 μM |
| IGF-1R (Cell-free assay) | 0.15 μM |
| FLT3 (Cell-free assay) | 0.42 μM |
| Tek (Cell-free assay) | 0.53 μM |
| FLT1 (Cell-free assay) | <0.6 μM |
| in vitro study | in purified kinase/recombinant kinase domain experiment, NVP-AEW541 also inhibited InsR, Tek, Flt1 and Flt3,IC50 were 140 nM, 530 nM, 600 nM and 420 nM respectively. At the cellular level, NVP-AEW541 selectivity is higher, 27 times higher than InsR selectivity. NVP-AEW541 inhibit IGF-I-regulated survival, soft agar, and MCF-7 cell proliferation with IC50 of 0.162 μM, 0.105 μM, and 1.64 μM, respectively. NVP-AEW541 acts on NWT-21 cells and also reduces p-IGF-IR and p-PKB levels. NVP-AEW541 acts on TC-71 musculoskeletal sarcoma cells cultured in low serum medium and medium containing 10% FBS to inhibit growth. NVP-AEW541 act on sarcoma cell lines (TC-71, SK-N-MC, SaoS-2, RD/18 and RH4), inhibit cell cycle progression and induce cell cycle to pause in G1 phase. NVP-AEW541 can inhibit the growth of neuroblastoma cells with IC50 of 0.4-6.8 μM. Increased subdiploid fragments and cell consumption in S and G2-M phases can be detected in these cells. In neuroblastoma cells, inhibition of NVP-AEW541-driven IGF-IR reduces Akt phosphorylation instead of Erk1 and Erk2 phosphorylation. NVP-AEW541 inhibit the growth of glioma cells and destroy the autocrine loop initiated by HIF1α stabilization. The latest research shows that NVP-AEW541 inhibits the proliferation and activity of PC3, DU145, and 22Rv1 prostate cancer cells. NVP-AEW541 acts on 22Rv1 and DU415 cells instead of PC3 cells, reducing p-Akt levels without affecting overall Akt levels, indicating that PTEN status can determine the effectiveness of NVP-AEW541. NVP-AEW541-induced radiosensitivity is determined by Akt activation. NVP-AEW541 acts on PC3, DU145, and 22Rv1 cells to increase H2AX phosphorylation. |
| in vivo study | NVP-AEW541(50 mg/kg, orally treated) acts on NWT-21 transplanted tumors, leading to the abolition of basic and IGF-I inducible receptors, and also inhibiting phosphorylation of PKB and MAPK, with a T/C value of 14%. NVP-AEW541(50 mg/kg) acts on HTLA-230 and SK-N-BE2c transplanted tumors, causing tumor shrinkage without signs of systemic toxicity. NVP-AEW541 acting on Matrigel-coated cells and HTLA-230 transplanted tumors can inhibit tumor invasion. |
Last Update：2024-04-09 15:16:35
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CAS: 475489-16-8
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Product Name: NVP-AEW541 Visit Supplier Webpage Request for quotation
CAS: 475489-16-8
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 475489-16-8
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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