- 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.
Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
- View current batch:
- 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. | |
NVP-AEW541 Dilution Calculator
calculate
NVP-AEW541 Molarity Calculator
calculate
| 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.
ebiomall.com
>
>
>
>
>
>
>
>
>
>
>
配胶、上样、跑胶、半干转无特殊，半干转后，就用TBST浸润一下后放入封闭液（试过5%牛奶、5%BSA）2小时，后取出直接抗体孵育（目标蛋白抗体1：1000、1：1500、1：2000【建议浓度1：1000-3000】，二抗1：2000、1：3000、1：5000【建议浓度1：1000-5000】，内参beta-actin差不多，目标蛋白4度过夜，内参室温2小时），孵育完后，TBST洗三次，每次10min，后二抗孵育，完后同样TBST洗三次，每次10min，后进行ECL发光液浸润2min，暗室压片2min(主要问题是在暗室中可以看到整张PVDF膜都有荧光，郁闷），显影定影，结果在胶片PVDF膜位置很黑，虽然可以见到我的条带，但是无法使用，不知道究竟怎样解决？（实验室另一位同学不存这样的问题）
试过几次都是同样的问题，是封闭的不好？抗体稀释度不够？TBST洗得不好？ECL发光步骤问题？渴求园里战友指导，谢谢！
