BMS 536924

Name BMS 536924
Supplier Tocris Bioscience
Catalog 5009
Prices $255.00, $1,045.00
Sizes 10 mg, 50 mg
Function Type Inhibitor
Cas Number 468740-43-4
Chemical Name 4-[[(2S)-2-(3-Chlorophenyl)-2-hydroxyethyl]amino]-3-[7-methyl-5-(4-morpholinyl)-1H-benzimidazol-2-yl]-2(1H)-pyridinone
Formula C25H26ClN5O3
Molecular Weight 479.96
Purity >98 %
Description Dual inhibitor of the insulin receptor (IR) and insulin-like growth factor-1 receptor (IGF1R) (IC 50 values are 73 and 100 nM respectively). Inhibits receptor autophosphorylation and downstream MEK1/2 and Akt signaling. Induces G 1 arrest and apoptosis in ML-1 cells; also inhibits cell proliferation in multiple tumor types. Reverses EMT through the attenuation of Snail mRNA expression in MCF10A cell over expressing IGF1R.
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Product References

Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of - Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of

Wittman M, Carboni J, Attar R, Balasubramanian B, Balimane P, Brassil P, Beaulieu F, Chang C, Clarke W, Dell J, Eummer J, Frennesson D, Gottardis M, Greer A, Hansel S, Hurlburt W, Jacobson B, Krishnananthan S, Lee FY, Li A, Lin TA, Liu P, Ouellet C, Sang X, Saulnier MG, Stoffan K, Sun Y, Velaparthi U, Wong H, Yang Z, Zimmermann K, Zoeckler M, Vyas D. J Med Chem. 2005 Sep 8;48(18):5639-43.

Constitutively active type I insulin-like growth factor receptor causes - Constitutively active type I insulin-like growth factor receptor causes

Kim HJ, Litzenburger BC, Cui X, Delgado DA, Grabiner BC, Lin X, Lewis MT, Gottardis MM, Wong TW, Attar RM, Carboni JM, Lee AV. Mol Cell Biol. 2007 Apr;27(8):3165-75. Epub 2007 Feb 12.

Expression of insulin receptor isoform A and insulin-like growth factor-1 - Expression of insulin receptor isoform A and insulin-like growth factor-1

Wahner Hendrickson AE, Haluska P, Schneider PA, Loegering DA, Peterson KL, Attar R, Smith BD, Erlichman C, Gottardis M, Karp JE, Carboni JM, Kaufmann SH. Cancer Res. 2009 Oct 1;69(19):7635-43.

The mechanisms of differential sensitivity to an insulin-like growth factor-1 - The mechanisms of differential sensitivity to an insulin-like growth factor-1

Huang F, Greer A, Hurlburt W, Han X, Hafezi R, Wittenberg GM, Reeves K, Chen J, Robinson D, Li A, Lee FY, Gottardis MM, Clark E, Helman L, Attar RM, Dongre A, Carboni JM. Cancer Res. 2009 Jan 1;69(1):161-70.