A dual inhibitor of IGF-1R and IR
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BMS-536924

Item No. 14666

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[[(2S)-2-(3-chlorophenyl)-2-hydroxyethyl]amino]-3-[7-methyl-5-(4-morpholinyl)-1H-benzimidazol-2-yl]-2(1H)-pyridinone
CAS Number
468740-43-4
Molecular Formula
C25H26ClN5O3
Formula Weight
480.0
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 12 mg/mlDMF:PBS (pH 7.2) (1:9): 0.1 mg/mlDMSO: 10 mg/ml
λmax
217, 239, 355 nm
SMILES
CC1=C2C(N=C(C3=C(NC[C@@H](O)C4=CC=CC(Cl)=C4)C=CNC3=O)N2)=CC(N5CCOCC5)=C1
InChi Code
InChI=1S/C25H26ClN5O3/c1-15-11-18(31-7-9-34-10-8-31)13-20-23(15)30-24(29-20)22-19(5-6-27-25(22)33)28-14-21(32)16-3-2-4-17(26)12-16/h2-6,11-13,21,32H,7-10,14H2,1H3,(H,29,30)(H2,27,28,33)/t21-/m1/s1
InChi Key
ZWVZORIKUNOTCS-OAQYLSRUSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    5 mg

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    10 mg

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    Product Description

    BMS-536924 is a dual inhibitor of insulin-like growth factor receptor (IGF-1R) kinase and insulin receptor (IC50s = 100 and 73 nM, respectively).1 In this way, it blocks IGF-1R autophosphorylation and signaling through MEK1/2 and Akt, leading to G1 arrest and apoptosis in myeloblastic leukemia ML-1 cells. BMS-536924 reverses epithelial-to-mesenchymal transition in immortalized mammary epithelial MCF10A cells overexpressing constitutively activated IGF-1R and causes growth inhibition and polarization of breast cancer MCF-7 cells.2,3 It also induces expression of cytochrome P450 3A4 isoform in primary hepatocytes.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Wittman, M., Carboni, J., Attar, R., et al. Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. J. Med. Chem. 48(18), 5639-5643 (2005).

    2. Kim, H.J., Litzenburger, B.C., Cui, X., et al. Constitutively active type I insulin-like growth factor receptor causes transformation and xenograft growth of immortalized mammary epithelial cells and is acompanied by an epithelial-to-mesenchymal transition mediated by NF-κB and snail. Mol. Cell. Biol. 27(8), 3165-3175 (2007).

    3. Litzenburger, B.C., Kim, H.J., Kuiatse, I., et al. BMS-536924 reverses IGF-IR-induced transformation of mammary epithelial cells and causes growth inhibition and polarization of MCF7 cells. Clin. Cancer Res. 15(1), 226-237 (2009).

    4. Li, L., Sinz, M.W., Zimmermann, K., et al. An insulin-like growth factor 1 receptor inhibitor induces CYP3A4 expression through a pregnane X receptor-independent, noncanonical constitutive androstane receptor-related mechanism. J. Pharmacol. Exp. Ther. 340(3), 688-697 (2012).