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BMS-754807

Cat. No. M2192
BMS-754807 Structure
Size Price Availability Quantity
10mg USD 200 In stock
50mg USD 560 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

BMS-754807 is a potent and reversible inhibitor of the type-1 insulin-like growth factor receptor family kinases (Ki, <2 nmol/L). BMS-754807 effectively inhibits the growth of a broad range of human tumor types in vitro, including mesenchymal, epithelial and hematopoietic tumor cell lines (IC50, 5-365 nmol/L). In vitro, BMS-754807 showed a median EC(50) value of 0.62 μM against the PPTP cell lines. BMS-754807 caused apoptosis in a human rhabdomyosarcoma cell line, Rh41, as shown by an accumulation of the sub-G1 fraction, as well as by an increase in poly ADP ribose polymerase and Caspase 3 cleavage. BMS-754807 is active in vivo in multiple xenograft tumor models with tumor growth inhibition ranging from 53% to 115% and at a minimum effective dose of as low as 6.25 mg/kg dosed orally daily. BMS-754807 is currently in phase I development for the treatment of a variety of human cancers.

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 461.49
Formula C23H24FN9O
CAS Number 1001350-96-4
Purity >99%
Solubility DMSO
Storage at -20°C
References

Dual IGF-1R/InsR inhibitor BMS-754807 synergizes with hormonal agents in treatment of estrogen-dependent breast cancer.
Hou X, et al. Cancer Res. 2011 Dec 15;71(24):7597-607. PMID: 22042792.

Initial testing (stage 1) of the IGF-1 receptor inhibitor BMS-754807 by the pediatric preclinical testing program.
Kolb EA, et al. Pediatr Blood Cancer. 2011 Apr;56(4):595-603. PMID: 21298745.

Differential mechanisms of acquired resistance to insulin-like growth factor-i receptor antibody therapy or to a small-molecule inhibitor, BMS-754807, in a human rhabdomyosarcoma model.
Huang F, et al. Cancer Res. 2010 Sep 15;70(18):7221-31. PMID: 20807811.

BMS-754807, a small molecule inhibitor of insulin-like growth factor-1R/IR.
Carboni JM, et al. Mol Cancer Ther. 2009 Dec;8(12):3341-9. PMID: 19996272.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: BMS-754807 supplier, IGF-1R, inhibitors

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