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Crolibulin

Cat. No. M9010
Crolibulin Structure
Synonym:

EPC2407; crinobulin

Size Price Availability
5mg USD 560  USD560 4-7 Days
10mg USD 820  USD820 4-7 Days
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Quality Control & Documentation
Biological Activity

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.

Chemical Information
Molecular Weight 417.26
Formula C18H17BrN4O3
CAS Number 1000852-17-4
Solubility (25°C) DMSO: ≥ 90 mg/mL (Need warming and ultrasonic)
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] Zhai X, et al. Sci Rep. Discovery and Optimization of Novel 5-Indolyl-7-arylimidazo[1,2-a]pyridine-8-carbonitrile Derivatives as Potent Antitubulin Agents Targeting Colchicine-binding Site.

[2] Kalmuk J, et al. Oncotarget. Multimodal imaging guided preclinical trials of vascular targeting in prostate cancer.

[3] Patil SA, et al. Future Med Chem. Chromenes: potential new chemotherapeutic agents for cancer.

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Keywords: Crolibulin, EPC2407; crinobulin supplier, Microtubule, inhibitors, activators


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