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ABT-751

Cat. No. M1642
ABT-751 Structure
Size Price Availability Quantity
10mg USD 90 In stock
50mg USD 360 In stock
100mg USD 630 In stock
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Quality Control
Biological Activity

ABT-751 is an orally bioavailable tubulin inhibitor with IC50 of about 1.5 and 3.4 µM in neuroblastoma and non-neuroblastoma cell lines, respectively. ABT-751 had a broad spectrum of antitumor activity in a panel of 30 tumor cell lines in vitro and in xenograft models of human tumors in vivo, including gastric, colorectal, lung, and breast cancer models. ABT-751 showed antitumor activity against a broad spectrum of tumor lines including those resistant to conventional chemotherapies. A single dose of ABT-751 (30 mg/kg, intravenously) induced a rapid, transient reduction in tumor perfusion. After 1 h, tumor perfusion decreased by 57% before recovering to near pretreatment levels within 6 h. In contrast, ABT-751 produced little change in muscle perfusion at either time point. ABT-751, at concentrations corresponding to plasma levels achieved in vivo, caused endothelial cell retraction and significant loss of microtubules within 1 h.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 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.

Chemical Information
Molecular Weight 371.41
Formula C18H17N3O4S
CAS Number 141430-65-1
Purity >99%
Solubility DMSO ≥72 mg/mL
Storage at -20°C
References

ABT-751 in Relapsed Childhood Acute Lymphoblastic Leukemia.
Gaynon et al. J Pediatr Hematol Oncol. 2012 May 10. PMID: 22584778.

Evaluation of the oral antimitotic agent (ABT-751) in dogs with lymphoma.
Silver et al. J Vet Intern Med. 2012 Mar-Apr;26(2):349-54. PMID: 22369215.

Phase I/II study of pemetrexed with or without ABT-751 in advanced or metastatic non-small-cell lung cancer.
Rudin et al. J Clin Oncol. 2011 Mar 10;29(8):1075-82. PMID: 21300929.

Pharmacokinetics of orally administered ABT-751 in children with neuroblastoma and other solid tumors.
Fox et al. Cancer Chemother Pharmacol. 2010 Sep;66(4):737-43. PMID: 20044751.

Clinical outcome in children with recurrent neuroblastoma treated with ABT-751 and effect of ABT-751 on proliferation of neuroblastoma cell lines and on tubulin polymerization in vitro.
Meany et al. Pediatr Blood Cancer. 2010 Jan;54(1):47-54. PMID: 19731320.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: ABT-751 supplier, Microtubule, inhibitors

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