- BMS-754807
- BMS-536924
- NVP-ADW742
- Linsitinib
- GSK1904529A
- AG-1024
| NVP-AEW541IGF-IR inhibitor, novel, potent and selective |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
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- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
| Description | NVP-AEW541 is a novel, potent and selective inhibitor of IGF-IR kinasewith IC50 value of 0.086 μM. | |||||
| Targets | IGF-IR kinase | |||||
| IC50 | 0.086 μM | |||||
| Kinase experiment [1]: | |
In vitro kinase assays | NVP-AEW541 was dissolved in DMSO (10 mM) and stored at -20°C. Dilutions were freshly made in DMSO/water 1:1. The final concentration of DMSO in the enzyme assays was < 0.5="" %.="" the="" protein="" kinase="" assays="" were="" carried="" out="" in="" 96-well="" plates="" at="" rt="" and="" terminated="" by="" the="" addition="" of="" 20="" μl="" of="" 125="" mm="" edta.="" subsequently,="" 30="" μl="" (c-abl,="" c-src,="" igf-1r)="" of="" the="" reaction="" mixture="" were="" transferred="" onto="" immobilon-pvdf="" presoaked="" for="" 5="" mins="" with="" methanol,="" rinsed="" with="" water,="" then="" soaked="" for="" 5="" mins="" with="" 0.5="" %="" h3po4="" and="" mounted="" on="" vacuum="" manifold.="" after="" spotting="" all="" samples,="" vacuum="" was="" connected="" and="" each="" well="" rinsed="" with="" 200="" μl="" 0.5="" %="" h3po4.="" membranes="" were="" removed="" and="" washed="" 4="" times="" on="" a="" shaker="" with="" 1.0="" %="" h3po4,="" once="" with="" ethanol.="" after="" drying,="" mounting="" in="" packard="" topcount="" 96-well="" frame,="" and="" adding="" of="" 10="" μl/well="" of="" microscint,="" membranes="" were="" counted.="" the="" ic50="" values="" were="" calculated="" by="" linear="" regression="" analysis="" of="" the="" percentage="" inhibition="" of="" nvp-aew541="" in="" duplicate,="" at="" 4="" concentrations="" (usually="" 0.01,="" 0.1,="" 1,="" and="" 10="" μm).="" one="" unit="" of="" protein="" kinase="" activity="" was="" defined="" as="" 1="" nmol="" of="" 33p="" transferred="" from="" [γ33p]atp="" to="" the="" substrate="" protein="" per="" minute="" per="" mg="" of="" protein="" at=""> |
| Cell experiment [1]: | |
Cell lines | MCF-7 cells |
Preparation method | The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
Reaction Conditions | ~ 10 μM; 72 hrs |
Applications | In MCF-7 cells, NVP-AEW541 suppressed the IGF-I-mediated survival, soft agar and cell proliferation with IC50 values of 0.162 μM, 0.105 μM and 1.64 μM, respectively. |
| Animal experiment [1]: | |
Animal models | Female Harlan athymic nude mice with NWT-21 cells |
Dosage form | 20, 30, or 50 mg/kg; p.o.; twice daily, 7 days/week |
Applications | NVP-AEW541 dose-dependently inhibited tumor growth with T/C values of 32%, 28% and 14% at the doses of 20 mg, 30 mg, or 50 mg, respectively. NVP-AEW541 was well tolerated at the indicated doses, and the recorded variations in body weight were not statistically significant. |
Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
References: [1]. García-Echeverría C, Pearson MA, Marti A, et al. In vivo antitumor activity of NVP-AEW541-A novel, potent, and selective inhibitor of the IGF-IR kinase. Cancer Cell, 2004, 5(3): 231-239. | |
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| Cas No. | 475489-16-8 | SDF | Download SDF |
| Chemical Name | 7-[3-(azetidin-1-ylmethyl)cyclobutyl]-5-(3-phenylmethoxyphenyl)pyrrolo[2,3-d]pyrimidin-4-amine | ||
| Canonical SMILES | C1CN(C1)CC2CC(C2)N3C=C(C4=C3N=CN=C4N)C5=CC(=CC=C5)OCC6=CC=CC=C6 | ||
| Formula | C27H29N5O | M.Wt | 439.55 |
| Solubility | ≥22mg/mL in DMSO | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
NVP-AEW541 is a novel, potent and selective inhibitor of IGF-IR kinase with IC50 value of 0.086 μM [1].
NVP-AEW541 is a pyrrolo(2,3-d) pyrimidine derivative. It has been reported to abolish IGF-I-induced IGF-IR autophosphorylation and to block the IGF-IR signaling pathway mainly in ECC-1 and USPC-1 cancer cells. Also in these cell lines, NVP-AEW541 has been shown to change the IGF-I induced cell cycle and to lead apoptotic cell death as well as exhibit antiproliferative effects [2]. In addition, it is observed that NVP-AEW541 can induce radiosensitization in PTEN wild-type cell lines [3].
Reference:[1] Carlos Garc a-Echeverr a, Mark A. Pearson, Andreas Marti, Thomas Meyer, Juergen Mestan, Johann Zimmermann, Jiaping Gao, Josef Brueggen, Hans-Georg Capraro, Robert Cozens, Dean B. Evans, Doriano Fabbro, Pascal Furet, Diana Graus Porta, Janis Liebetanz, Georg Martiny-Baron, Stephan Ruetz, and Francesco Hofmann. In vivo antitumor activity of NVP-AEW541—A novel, potent, and selective inhibitor of the IGF-IR kinase. Cancer Cell.2004 Mar (5):231-239. [2] Zohar Attias-Geva, Itay Bentov, Ami Fishman, Haim Werner, Ilan Bruchim. Insulin-like growth factor-I receptor inhibition by speci c tyrosine kinase inhibitor NVP-AEW541 in endometrioid and serous papillary endometrial cancer cell lines. Gynecologic Oncology. 2011 Feb (121):383-389. [3] Sofie F. Isebaert, Johannes V. Swinnen, William H. Mcbride, and Karin M. Haustermans. Insulin-like growth factor–type 1 receptor inhibitor NVP-AEW541 enhances radiosensitivity of PTEN wild-type but not PTEN-deficient human prostate cancer cells. International Journal of Radiation Oncology Biology Physics. 2011 (81):239-247.
