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BMS-754807

Chemical Structure : BMS-754807

CAS No.: 1001350-96-4

BMS-754807 (BMS 754807;BMS754807)

Catalog No.: PC-42444Not For Human Use, Lab Use Only.

BMS-754807 (BMS 754807, BMS754807) is a potent, reversible, orally active inhibitor of IGF-1R/Insulin receptor with IC50 of 1.8 and 1.7 nM, respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

BMS-754807 (BMS 754807, BMS754807) is a potent, reversible, orally active inhibitor of IGF-1R/Insulin receptor with IC50 of 1.8 and 1.7 nM, respectively; shows additional off-target activities Met, RON, TrkA, TrkB, AurA, and AurB (IC50=5-45 nM) in a panel of 27 kinases; inhibits the growth of a broad range of human tumor types in vitro (IC50=5-365 nM), induces PARP and Caspase 3 cleavage, promotes apoptosis; exhibits tumor growth inhibition in xenograft tumor models.

Breast Cancer

Phase 2 Discontinued

Physicochemical Properties

M.Wt 461.4948
Formula C23H24FN9O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-Pyrrolidinecarboxamide, 1-[4-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]-N-(6-fluoro-3-pyridinyl)-2-methyl-, (2S)-

References

1. Wittman MD, et al. Mol Cancer Ther. 2009 Dec;8(12):3341-9.

2. Carboni JM, et al. Mol Cancer Ther. 2009 Dec;8(12):3341-9.

3. Dinchuk JE, et al. Endocrinology. 2010 Sep;151(9):4123-32.

4. Huang F, et al. Cancer Res. 2010 Sep 15;70(18):7221-31.

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