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BMS-690514

Cat. No. M2464
BMS-690514 Structure
Size Price Availability
5mg USD 300  USD300 4-7 Days
10mg USD 447  USD447 4-7 Days
50mg USD 1150  USD1150 4-7 Days
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Quality Control & Documentation
Biological Activity

BMS-690514 is a potent inhibitor of EGFR and VEGFR2 with IC50 of 5 nM and 50 nM, respectively.

Chemical Information
Molecular Weight 368.43
Formula C19H24N6O2
CAS Number 859853-30-8
Solubility (25°C) DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Hiroshi Nokihara, et al. A phase I study of BMS-690514 in Japanese patients with advanced or metastatic solid tumors

[2] Blisse Vakkalagadda, et al. Food increased the bioavailability of BMS-690514, an orally active EGFR/HER2/VEGF receptor kinase inhibitor, in healthy subjects

[3] Y Loriot, et al. BMS-690514, a VEGFR and EGFR tyrosine kinase inhibitor, shows anti-tumoural activity on non-small-cell lung cancer xenografts and induces sequence-dependent synergistic effect with radiation

[4] Haizheng Hong, et al. Metabolism and disposition of [14C]BMS-690514 after oral administration to rats, rabbits, and dogs

[5] Punit Marathe, et al. Preclinical pharmacokinetics and in vitro metabolism of BMS-690514, a potent inhibitor of EGFR and VEGFR2

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  Catalog
Abmole Inhibitor Catalog




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