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BMS 794833

Cat. No. M1683
BMS 794833 Structure
Size Price Availability Quantity
5mg USD 105  USD105 In stock
10mg USD 183  USD183 In stock
50mg USD 700  USD700 In stock
100mg USD 1050  USD1050 In stock
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Quality Control & Documentation
Biological Activity

BMS-794833 is a potent ATP competitive Met/VEGFR-2 kinase inhibitor and it also inhibits Ron (Met family), Axl and Flt-3 with IC50 values <3 nM. BMS-794833 was selective versus a panel of >200 additional RTKs, non-RTKs and serine/threonine kinases based on biochemical or Ambit binding assays. In cell culture, BMS-794833 inhibited the proliferation of human tumor cell lines containing constitutively activated Met receptor (GTL-16 gastric carcinoma). In vivo, BMS-794833 demonstrated dose-dependent tumor growth inhibition following oral administration in the GTL-16 and L2987 lung carcinoma (Met-insensitive) xenograft models.

Protocol (for reference only)
Cell Experiment
Cell lines gastric cancer cell line (GTL-16)
Preparation method cell proliferation assay
Concentrations IC50 = 39 nM
Incubation time
Animal Experiment
Animal models U87 glioblastoma model
Formulation
Dosages 25mg/kg
Administration
Chemical Information
Molecular Weight 468.84
Formula C23H15ClF2N4O3
CAS Number 1174046-72-0
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] Nao Nishida-Aoki, et al. Polypharmacologic Reprogramming of Tumor-Associated Macrophages toward an Inflammatory Phenotype

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Keywords: BMS 794833 supplier, c-Met, inhibitors, activators


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