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BMS-536924

Cat. No. M1957

BMS-536924 Structure
Size Price Availability Quantity
5mg USD 110 In stock
10mg USD 180 In stock
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Quality Control
Biological Activity

BMS-536924 is a potent small molecule dual IGF-IR/IR kinase inhibitor, which shows antitumor activity in multiple tumor models. BMS-536924 inhibits cellular proliferation and disrupts Akt and MAPK phosphorylation. BMS-536924 also inhibits FAK and Lck with IC50 of 150 nM and 341 nM, respectively. BMS-536924 induced a dose-dependent inhibition of proliferation, with an accumulation of cells in G(0)/G(1,), and completely blocked CD8-IGF-IR-induced migration, invasion, and anchorage-independent growth in monolayer culture. In vitro, BMS-536924 inhibited leukemic colony formation in CD34+ clinical AML samples.

Protocol
Cell Experiment
Cell lines TGBC-1TKB, TGBC-2TKB and TGBC-14TKB cell lines
Preparation method In vitro cell growth.
Four thousand cells were seeded into a 96-well plate and each was treated with several concentrations of BMS-536924. Cell growth was measured using WST-1 reagent (Roche, Basel, Switzerland), as described previously.
Concentrations 0, 1, 5, 10μM
Incubation time 0, 1, 2, 3, 4 days
Animal Experiment
Animal models TGBC-1TKB tumour xenograft in nude mice
Formulation a mixture of polyethylene glycol 400 (PEG400 ⁄ water, 4:1 vol ⁄ vol)
Dosages 70 mg ⁄ kg once daily for 2 weeks
Administration oral gavage
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 479.96
Formula C25H26ClN5O3
CAS Number 468740-43-4
Purity 98.65%
Solubility DMSO
Storage at -20°C
References

Insulin-like growth factor receptor expression is associated with aggressive phenotypes and has therapeutic activity in biliary tract cancers.
Ohashi H, et al. Cancer Sci. 2012 Feb;103(2):252-61. PMID: 22044563.

Expression of insulin receptor isoform A and insulin-like growth factor-1 receptor in human acute myelogenous leukemia: effect of the dual-receptor inhibitor BMS-536924 in vitro.
Wahner Hendrickson AE, et al. Cancer Res. 2009 Oct 1;69(19):7635-43. PMID: 19789352.

BMS-536924 reverses IGF-IR-induced transformation of mammary epithelial cells and causes growth inhibition and polarization of MCF7 cells.
Litzenburger BC, et al. Clin Cancer Res. 2009 Jan 1;15(1):226-37. PMID: 19118050.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: BMS-536924 supplier, IGF-1R, inhibitors

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