An IGF-1R inhibitor
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Alternative(s)
33946NVP-AEW541
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NVP-AEW541 (hydrochloride)

Item No. 13641

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
7-[cis-3-(1-azetidinylmethyl)cyclobutyl]-5-[3-(phenylmethoxy)phenyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine, dihydrochloride
CAS Number
2320261-63-8
Molecular Formula
C27H29N5O • 2HCl
Formula Weight
512.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
Ethanol: 0.3 mg/mlPBS (pH 7.2): 2.5 mg/ml
λmax
288 nm
SMILES
NC1=C2C(N([C@@H]3C[C@H](CN4CCC4)C3)C=C2C5=CC=CC(OCC6=CC=CC=C6)=C5)=NC=N1.Cl.Cl
InChi Code
InChI=1S/C16H16N6O/c1-8(2)22-16-13(15(17)18-7-19-16)14(21-22)12-6-9-5-10(23)3-4-11(9)20-12/h3-8,20,23H,1-2H3,(H2,17,18,19)
InChi Key
MFAQYJIYDMLAIM-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $90

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    1 mg

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    5 mg

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    10 mg

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    Product Description

    NVP-AEW541 is an inhibitor of insulin-like growth factor 1 receptor (IGF-1R; IC50 = 0.15 µM in a cell-free assay).1 It is selective for IGF-1R over a panel of 20 kinases but also inhibits the insulin receptor (InsR), VEGFR1, FMS-related tyrosine kinase 3 (FLT3), and tunica interna endothelial cell kinase 2 (Tie2; IC50s = 0.14, 0.6, 0.42, and 0.53 µM, respectively, in cell-free assays). NVP-AEW541 selectively inhibits the autophosphorylation of IGF-1R over InsR, EGFR, PDGFR, c-Kit, and Bcr-Abl in cells (IC50s = 0.086, 2.3, >10, >10, >5, and >10 µM, respectively). It reduces tumor volume in an NWT-21 murine fibrosarcoma model when administered at doses of 20, 30, or 50 mg/kg twice per day.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. García-Echeverría, C., Pearson, M.A., Marti, A., et al. In vivo antitumor activity of NVP-AEW541—a novel, potent, and selective inhibitor of the IGF-IR kinase. Cancer Cell 5(3), 231-239 (2004).