Crolibulin is a small molecule tubulin polymerization inhibitor. Microtubulin inhibitor Crolibulin (EPC2407) binds to the colchicine-binding site on beta-tubulin and inhibits the polymerization of tubulin into microtubules, which may result in cell cycle arrest, the induction of apoptosis, and the inhibition of tumor cell proliferation. Crolibulin also disrupts tumor neovascularization, which may result in a reduction in tumor blood flow and tumor hypoxia and ischemic necrosis.
|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: ≥ 90 mg/mL (Need warming and ultrasonic)|
Discovery and Optimization of Novel 5-Indolyl-7-arylimidazo[1,2-a]pyridine-8-carbonitrile Derivatives as Potent Antitubulin Agents Targeting Colchicine-binding Site.
Zhai X, et al. Sci Rep. 2017 Feb 27;7:43398. PMID: 28240326.
Multimodal imaging guided preclinical trials of vascular targeting in prostate cancer.
Kalmuk J, et al. Oncotarget. 2015 Sep 15;6(27):24376-92. PMID: 26203773.
Chromenes: potential new chemotherapeutic agents for cancer.
Patil SA, et al. Future Med Chem. 2013 Sep;5(14):1647-60. PMID: 24047270.
|Related Microtubule Products|
VcMMAE is a anti-mitotic agent, monomethyl auristatin E (MMAE), linked via the lysosomally cleavable dipeptide, valine-citrulline (vc).
Maytansinol, also known as Ansamitocin P-0, is a potent microtubule depolymerizing agent.
Epothilone D is a potent microtubule stabilizer.
|Estramustine phosphate sodium
Estramustine phosphate sodium is an antimicrotubule chemotherapy agent; arrests prostate cancer cells in the G2/M phase of the cell cycle.
Docetaxel trihydrate(Taxotere trihydrate), an analog of taxol, is an inhibitor of depolymerisation of microtubules through binding to stabilized microtubules.
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