AEW-541 cis-isomer (NVP-AEW541)
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
| Size | Price | Stock |
|---|---|---|
| 250mg | $1350 | To Be Confirmed |
| 500mg | $2000 | To Be Confirmed |
| 1g | $3000 | To Be Confirmed |
: Cat #: V10412 CAS #: 475489-16-8 Purity ≥ 98%
Description: NVP-AEW541 cis-isomer (also known as AEW541 cis-isomer), the cis-isomer of AEW541 is a novel and potent inhibitor of IGF-1R/InsR with IC50 of 150 nM/140 nM in cell-free assays, it has greater potency and selectivity for IGF-1R in a cell-based assay.
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| Molecular Weight (MW) | 439.55 |
|---|---|
| Molecular Formula | C27H29N5O |
| CAS No. | 475489-16-8 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO:88 mg/mL (200.2 mM)r |
| Water: <1 mg/mLr | |
| Ethanol: <1 mg/mL | |
| Solubility In Vivo | 30% PEG400+0.5% Tween80+5% propylene glycol: 20 mg/mL |
| SMILES Code | NC1=C2C(N([C@H]3C[C@H](CN4CCC4)C3)C=C2C5=CC=CC(OCC6=CC=CC=C6)=C5)=NC=N1 |
| Synonyms | AEW541 cis-isomer; NVP-AEW541; NVP-AEW 541; NVP-AEW-541; AEW-541; AEW 541; AEW541 |
| Protocol | In Vitro | NVP-AEW541 inhibits the in vitro kinase activity of the recombinant IGF-IR kinase domain with an IC50 value of 0.15 μM and to be equipotent against the recombinant InsR kinase domain. NVP-AEW541 is confirmed active toward the IGF-IR kinase (IC50=86 nM) and shown to be selective at the cellular level. Indeed, NVP-AEW541 is found to be 27-fold more potent toward the native IGF-IR, as compared to the structurally related native InsR (IC50=2.3 μM). NVP-AEW541 suppresses the IGF-I-mediated survival, soft agar and proliferation of MCF-7 cells with IC50 of 0.162 μM, 0.105 μM and 1.64 μM, respectively. |
|---|---|---|
| In Vivo | Oral administration of NVP-AEW541 (20, 30, or 50 mg/kg) results in abrogation of basal and IGF-I-induced receptor, and PKB and MAPK phosphorylation in the NWT-21 tumor xenograft[1]. NVP-AEW541 is administered by oral gavage [50 mg/kg in 0.2 mL of 25 mM L-(+)-tartaric acid] twice a day for 14 consecutive days. The control group is similarly treated with 0.2 mL carrier [25 mM L-(+)-tartaric acid] twice a day. Tumor volume and animal weight are measured thrice a week till the end of the treatment. At that time, animals are sacrificed and tumors are collected and formalin fixed for histologic and immunohistochemical analyses. In both cases, NVP-AEW541 treatment causes tumor shrinkage that reached the statistical significance (P=0.0156 and P=0.0111 for HTLA-230 and SK-N-BE2c, respectively). |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 2.2751 mL | 11.3753 mL | 22.7505 mL | 45.5011 mL |
| 5mM | 0.4550 mL | 2.2751 mL | 4.5501 mL | 9.1002 mL |
| 10mM | 0.2275 mL | 1.1375 mL | 2.2751 mL | 4.5501 mL |
| 20mM | 0.1138 mL | 0.5688 mL | 1.1375 mL | 2.2751 mL |
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Step Two: Enter the in vivo formulation
%DMSO
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%ddH2O
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Method for preparing DMSO master liquid:
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,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:
Take
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DMSO master liquid, next add
µL
PEG300, mix and clarify, next add
µL
Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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