Cat. No. Name Size Price Add Cart
KI0509ABT-75110 mg$192
ABT-75150 mg$752
ABT-751200 mg$2512

Chemical Characteristic

Product NameABT-751
SynonymsE7010
CAS No.141430-65-1
Molecular Weight 371.41
FormulaC18H17N3O4S
Chemical NameN-[2-[(4-Hydroxyphenyl)amino]-3-pyridyl]-4-methoxybenzenesulfonamide
Smilesc1(ccc(cc1)OC)S(=O)(=O)Nc1c(nccc1)Nc1ccc(cc1)O
Chemical Structure

Biological activities

ABT-751 is a novel sulfonamide antimitotic agent. ABT-751 binds preferentially and competitively to the colchicine site of the β3 isoform of tubulin with a Ki of 3.3 mM. ABT-751 inhibits microtubule polymerization with an IC50 of 3.1 mM. ABT-751 exposure results in inhibition of microtubule assembly with resultant G2-M arrest and apoptosis.[1] ABT-751, at concentrations corresponding to plasma levels achieved in vivo, causes endothelial cell retraction and significant loss of microtubules within 1 hour. [2] ABT-751 (3, 10, and 30 mg/kg; i.v.) produces modest transient increases in mean arterial pressure with no effect on heart rate. Administration of ABT-751 produces transient modest increases in mesenteric vascular resistance (VR) and no effect on renal VR. ABT-751 exerts tumor-selective, anti-vascular effects in the rat. [3] ABT-751 has shown significant preclinical tumor activity in a variety of syngeneic and human xenograft models (colon, lung, stomach, breast, pancreas, prostate, nasopharyngeal). [4]

Protocols

ABT-751 is dissolved in a vehicle of PEG200/5% dextrose (1:1) in water. [1]

References

[1] Yee KW, et al. Phase 1 study of ABT-751, a novel microtubule inhibitor, in patients with refractory hematologic malignancies. Clin Cancer Res. 2005, 11(18): 6615-6624.
[2] Luo Y, et al. ABT-751, a novel tubulin-binding agent, decreases tumor perfusion and disrupts tumor vasculature. Anticancer Drugs. 2009, 20(6): 483-492.
[3] Segreti JA, et al. Tumor selective anti-vascular effects of the novel antimitotic compound ABT-751: an in vivo rat regional hemodynamic study. Cancer Chemother Pharmacol. 2004, 54(3): 273-281.
[4] Hande KR, et al. The pharmacokinetics and safety of ABT-751, a novel, orally bioavailable sulfonamide antimitotic agent: results of a phase 1 study. Clin Cancer Res. 2006, 12(9): 2834-2840.

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