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Brivanib alaninate

Cat. No. M1687

Brivanib alaninate Structure

Synonym: BMS-582664

Size Price Availability Quantity
10mg USD 210 In stock
50mg USD 740 In stock
100mg USD 1180 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Brivanib alaninate is a prodrug of brivanib (BMS-540215), a potent oral VEGFR-2 inhibitor and is currently in development for the treatment of hepatocellular and colon carcinomas. In vitro and in vivo studies were conducted to characterize the preclinical pharmacokinetics and disposition of brivanib and brivanib alaninate, and antitumor efficacy in mice bearing human xenografts.

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 441.46
Formula C22H24FN5O4
CAS Number 649735-63-7
Purity >99%
Solubility DMSO
Storage at -20°C
References

Reversible and pH-dependent weak drug-excipient binding does not affect oral bioavailability of high dose drugs.
Narang et al. J Pharm Pharmacol. 2012 Apr;64(4):553-65. PMID: 22420661.

Acid-catalyzed hydrolysis of BMS-582664: Degradation product identification and mechanism elucidation.
Zhao et al. J Pharm Sci. 2012 Sep;101(9):3526-30. PMID: 22189636.

Phase I dose-escalation study to determine the safety, pharmacokinetics and pharmacodynamics of brivanib alaninate in combination with full-dose cetuximab in patients with advanced gastrointestinal malignancies who have failed prior therapy.
Garrett et al. Br J Cancer. 2011 Jun 28;105(1):44-52. PMID: 21629245.

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Keywords: Brivanib alaninate, BMS-582664 supplier, VEGFR/PDGFR, inhibitors

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