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BMS-754807

Catalog No. T2349 CAS 1001350-96-4

Dual IGF-1R/InsR Inhibitor BMS-754807 is an oral small molecule inhibitor of insulin-like growth factor 1 receptor (IGF-1R) and insulin receptor (InsR) tyrosine kinases with potential antineoplastic activity.

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BMS-754807, CAS 1001350-96-4

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Purity: 98%

Biological Description

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Description	Dual IGF-1R/InsR Inhibitor BMS-754807 is an oral small molecule inhibitor of insulin-like growth factor 1 receptor (IGF-1R) and insulin receptor (InsR) tyrosine kinases with potential antineoplastic activity.
Targets&IC50	TrkA:7.4 nM, Insulin Receptor:1.7 nM, TrkB:4.1 nM, Met:5.6 nM, IGF-1R:1.8 nM
Kinase Assay	Kinase inhibition assays: The primary screen for BMS-754807 is an in vitro kinase assay using recombinant human IGF-1 receptor enzyme in biochemical assays using synthetic peptide KKSRGDYMTMQIG as a phosphoacceptor substrate. The selectivity profile is evaluated against multiple recombinant enzymes that are generated at BMS or purchased externally. The enzymatic assays are performed in Ubottom 384-well plates using a 30 μL reaction volume in assay buffer (100 mM Hepes pH 7.4, 10 mM MgCl2, 0.015% Brij35 and 4 mM DTT). The 60 minute reactions are initiated by combining ATP (concentration equivalent to Km ATP), 1.5 μM fluoresceinlabeled peptide substrate, enzyme and BMS-754807. The reactions are terminated with EDTA. The reaction mixtures are analyzed on the Caliper LabChip 3000 by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data are calculated by comparison to enzyme-free control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. Compounds are dissolved in dimethylsulfoxide (DMSO, 10 mM stock) and evaluated at eleven concentrations. IC50 values are derived by non-linear regression analysis of the dose response curves.
Cell Research	Cells are grown at their optimal density in RPMI +GlutaMax supplemented with 10% heat-inactivated fetal bovine serum (FBS), 10 mM Hepes, penicillin, and streptomycin. Cell proliferation is evaluated by incorporation of 3H-thymidine into DNA after exposure of cells to BMS-754807 for 72 hours. Results are expressed as an IC50, which is the drug concentration required to inhibit cell proliferation by 50% compared with untreated control cells.(Only for Reference)

Molecular Weight	461.49
Formula	C23H24FN9O
CAS No.	1001350-96-4

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

Ethanol: 85 mg/mL (184.2 mM)

H2O: <1 mg/mL

DMSO: 85 mg/mL (184.2 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Carboni JM, et al. Mol Cancer Ther, 2009, 8(12), 3341-3349. 2. Wittman MD, et al. J Med Chem, 2009, 52(23), 7360-7363. 3. Kolb EA, et al. Pediatr Blood Cancer, 2011, 56(4), 595-603. 4. Silbermann K, Stefan S, Elshawadfy R, et al. Identification of Thienopyrimidine Scaffold as Inhibitor of the ABC Transport Protein ABCC1 (MRP1) and Related Transporters Using a Combined Virtual Screening Approach[J]. Journal of Medicinal Chemistry. 2019.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

BMS-754807 1001350-96-4 Tyrosine Kinase/Adaptors IGF-1R Trk receptor c-Met/HGFR Insulin Receptor BMS 754807 inhibit BMS754807 Inhibitor inhibitor

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