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.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Solubility||DMSO 100 mM
Ethanol 20 mM
Indolobenzazepin-7-ones and 6-, 8-, and 9-membered ring derivatives as tubulin polymerization inhibitors: synthesis and structure--activity relationship studies.
Putey A, et al. J Med Chem. 2009 Oct 8;52(19):5916-25. PMID: 19743863.
2-aroylindoles, a novel class of potent, orally active small molecule tubulin inhibitors.
Beckers T, et al. Cancer Res. 2002 Jun 1;62(11):3113-9. PMID: 12036922.
|Related Microtubule Products|
VcMMAE is a anti-mitotic agent, monomethyl auristatin E (MMAE), linked via the lysosomally cleavable dipeptide, valine-citrulline (vc).
Crolibulin (also known as EPC2407 and crinobulin) is a small molecule tubulin polymerization inhibitor with potential antineoplastic activity.
Maytansinol, also known as Ansamitocin P-0, is a potent microtubule depolymerizing agent.
|Ansamitocin P 3
Ansamitocin P-3 is a microtubule inhibitor, it is also a macrocyclic antitumor antibiotic.
Epothilone D is a potent microtubule stabilizer.
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