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My CartCAS：141430-65-1
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to off-white Solid
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| CAS | 141430-65-1 |
| Name | ABT-751 |
| Molecular Formula | C18H17N3O4S |
| Molecular Weight | 371.41 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC | EINECS 256-495-9 |
| MDL | MFCD00910291 |
| SMILES | COC1=CC=C(C=C1)S(=O)(NC2=C(N=CC=C2)NC3=CC=C(C=C3)O)=O |
| Target Point | Microtubule/Tubulin |
| Passage | Cytoskeleton |
| Background | ABT-751/E-7010 are novel biocompatible tubulin binding agents and antimitotic sulfonamides. |
| Biological Activity | ABT-751 (Abbott Laboratories， Abbott Park， IL) is an orally bioavailable sulfonamide that binds to the colchicine binding site on β-tubulin and inhibits the polymerization of microtubules. ABT-751 had antitumor activity in a panel of 30 tumor cell lines in vitro including cell lines resistant to Vinca alkaloids and taxanes due to P-glycoprotein overexpression. ABT-751 is a novel orally available antimitotic agent that targets microtubule polymerization.[1-2] |
| In Vivo | The maximum tolerated dose of ABT-751 was 350 mg/m(2)PO q24h. Dose-limiting toxicities included vomiting and diarrhea，which resolved with a schedule adjustment to 350 mg/m(2)PO q48h. ABT-751 was consistently detected in lymphoma tissue samples from dogs treated at or above the maximum tolerated dose. In the cohort expansion，objective responses were seen in 3/15(20%)dogs with a response duration ranging from 21 to 111 days. Decreases in circulating endothelial cells were seen in 10 dogs at day 7(2 responding dogs and 8 nonresponding dogs).[2] |
| Animal Experiment | Dogs(n = 11)were enrolled in a rapid dose escalation study to define the maximum tolerated dose. Upon definition of a maximally tolerated dose，a cohort expansion of 19 dogs allowed verification of long-term tolerability and assessment of activity. Study endpoints in the cohort expansion included chronic tolerability，response rate，response duration，and time to progression. Additional endpoints included serum pharmacokinetics，lymph node drug concentrations，and changes in circulating endothelial cells.[2] |
| Data Literature Source | [1]. Elizabeth Fox et al. A Phase I Study of ABT-751，an Orally Bioavailable Tubulin Inhibitor，Administered Daily for 21 Days Every 28 Days in Pediatric Patients with Solid Tumors Clin Cancer Res February 15，2008 14; 1111 [2]. Silver M，Rusk A，Phillips B，Beck E，Jankowski M，Philibert J，Hahn K，Hershey E，McKeegan E，Bauch J，Krivoshik A，Khanna C.，Evaluation of the oral antimitotic agent (ABT-751) in dogs with lymphoma.，J Vet Intern Med. 2012 Mar-Apr;26(2):349-54. doi: 10.1 |
| Unit | Bottle |
| Specification | 10mg 50mg |
是新型的生物相容性的微管蛋白结合剂和抗有丝分裂磺胺类化合物。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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