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BMS-214662 hydrochloride

Cat. No. M7661
BMS-214662 hydrochloride Structure
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Biological Activity

BMS-214662 is an orally available, potent and selective inhibitor of farnesyltransferase that reduces Ras prenylation in NF90-8 and ST88-14 sheath tumor (MPNST) cell lines. BMS-214662 induces apoptosis in cancer cell lines, and potently inhibits growth of human tumor xenografts.

Chemical Information
Molecular Weight 526.07
Formula C25H23N5O2S2.HCl
CAS Number 195981-08-9
Solubility (25°C) Water 20 mg/mL
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] M Bays, et al. Gateways to clinical trials

[2] M Bayes, et al. Gateways to clinical trials

[3] M Bays, et al. Gateways to clinical trials

[4] M Bays, et al. Gateways to clinical trials

[5] M Bayes, et al. Gateways to Clinical Trials. June 2002

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Keywords: BMS-214662 hydrochloride supplier, Farnesyl Transferase, inhibitors, activators


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