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D-64131

Cat. No. M3755
D-64131 Structure
Size Price Availability Quantity
5mg USD 60  USD60 In stock
10mg USD 88  USD88 In stock
50mg USD 345  USD345 In stock
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Quality Control & Documentation
Biological Activity

D-64131 is cytotoxic and inhibits tumor cell proliferation in vitro (IC50 = 74 nM). D-64131 prevents growth of tumor models in mice following oral administration in vivo.D-64131 has significant potential in cancer treatment.D-64131 and analogues have the potential to be developed for cancer therapy, replacing or supplementing standard therapy regimens with tubulin-targeting drugs from natural sources.

Chemical Information
Molecular Weight 251.28
Formula C16H13NO2
CAS Number 74588-78-6
Solubility (25°C) DMSO 100 mM
Ethanol 20 mM
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] Putey A, et al. J Med Chem. Indolobenzazepin-7-ones and 6-, 8-, and 9-membered ring derivatives as tubulin polymerization inhibitors: synthesis and structure--activity relationship studies.

[2] Beckers T, et al. Cancer Res. 2-aroylindoles, a novel class of potent, orally active small molecule tubulin inhibitors.

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