ABT-751 (E7010)

Catalog No.S1165

For research use only.

ABT-751 (E7010) binds to the colchicine site on β-tubulin and inhibits polymerization of microtubules, not a substrate for the MDR transporter and is active against cell lines resistant to vincristine, doxorubicin, and cisplatin. Phase 1/2.

ABT-751 (E7010) Chemical Structure

CAS No. 141430-65-1

Selleck's ABT-751 (E7010) has been cited by 5 Publications

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Biological Activity

Description ABT-751 (E7010) binds to the colchicine site on β-tubulin and inhibits polymerization of microtubules, not a substrate for the MDR transporter and is active against cell lines resistant to vincristine, doxorubicin, and cisplatin. Phase 1/2.
Features An orally bioavailable tubulin-binding and antimitotic sulfonamide.
Targets
Microtubules [1]
In vitro

In vitro, ABT-751 shows the selective cytotoxicity with IC50 of 0.6–2.6 μM in neuroblastoma and 0.7–4.6 μM in other solid tumor cell lines. Furthermore, ABT-751 also exhibits a selective effect on dynamic microtubules and spares stable microtubules, accounting for the persistence of acetylated and detyrosinated α-tubulin positive polymerized tubules at the IC90 concentration of ABT-751. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HCT-15 cell M3[2ZnBzd2yrZnXyZZRqd25iYYPzZZk> M4HmVWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iY3;sc44h[2G{Y3nuc41iKEiFVD2xOUBk\WyuIHzpcoUpVUSUKD2pLUwhUUN3ME2wMlM1KM7:TR?= NFTPOmEyOTR{NUWzOC=>
HCT116-C9 cell NHrJfFZHfW6ldHnvckBie3OjeR?= MVXF[oZm[3SrdnWgZ49v[2WwdILheIlwdiC2bzDpcohq[mm2IHPlcIwheHKxbHnm[ZJifGmxbjDifUA2OCVicnXsZZRqfmVidH:geY51emWjdHXkJINwdnS{b3ygZ4VtdCCjZoTldkA4OiCqcjDv[kBkd262aX71c5V{KGW6cH;zeZJmKGmwIFjDWFEyPi2FOTDj[YxtKGyrbnWsJGlEPTB;MD65JO69VQ>? M1XXN|EzOzh|MEG3
NCI-H460 cell MoD4VJJwdGmoZYLheIlwdiCjc4PhfS=> MoroRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCudX7nJINiemOrbn;tZUBPS0lvSES2NEBk\WyuIHzpcoUhME2GUjirLUktKEmFNUC9NE4{PSEQvF2= MW[xNVQzPTV|NB?=
P388 cell line MkTDSpVv[3Srb36gZZN{[Xl? MXu3NkBp NXXGS|lMTW[oZXP0bZZmKGOxbnPlcpRz[XSrb36geI8hcW6qaXLpeEBk\WyuIIDyc4xq\mW{YYTpc44h[nliNUClJJJmdGG2aY\lJJRwKHWwdILlZZRm\CClb370do9tKGOnbHygZYZ1\XJiN{KgbJIhd2ZiY3;ueIlvfW:3czDlfJBwe3W{ZTDpckBROzh6IHPlcIwhdGmwZf-8kEBKSzVyPUCuNVkh|ryP NG\rdHoyOjN6M{CxOy=>
P388/4.0 r-M cell line M4mzUWZ2dmO2aX;uJIF{e2G7 MXu3NkBp MUnF[oZm[3SrdnWgZ49v[2WwdILheIlwdiC2bzDpcohq[mm2IHPlcIwheHKxbHnm[ZJifGmxbjDifUA2OCVicnXsZZRqfmVidH:geY51emWjdHXkJINwdnS{b3ygZ4VtdCCjZoTldkA4OiCqcjDv[kBkd262aX71c5V{KGW6cH;zeZJmKGmwIGCzPFgwPC5yIIKtUUBk\WyuIHzpcoUtKEmFNUC9NVUh|ryP NVHwdY8{OTJ|OEOwNVc>
human HL60 cells NHfId5RRem:uaX\ldoF1cW:wIHHzd4F6 MmGxRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKTE[wJINmdGy|LDDJR|UxRTBwM{Sg{txO NELpPJgyPzJ5NkC1Oi=>
HeLa cells M{PLOWN6fG:2b4jpZ4l1gSCjc4PhfS=> M3rte|Q5NTd{IHi= MnrlR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTIVN[SClZXzsd{Bi\nSncjC0PEB1dyB5MjDodpMh[nliV1HUMVEh[XO|YYmsJGlEPTB;MD6yO{DPxE1? MUGyNVEzPjB{Nx?=
MDR1 cells MUjDfZRwfG:6aXPpeJkh[XO|YYm= Mnv3OFguPzJiaB?= MkLTR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUmNKNUGGUj3SSXMh\XiycnXzd4lv\yCPRGKxJINmdGy|IHHmeIVzKDR6IITvJFczKGi{czDifUBYSVRvMTDhd5NigSxiSVO1NF0xNjJ7IN88US=> M3rqW|IyOTJ4MEK3
Jurkat cells MWDGeY5kfGmxbjDhd5NigQ>? NUHkcXEzOjRiaB?= MUHD[YxtKGO7Y3zlJIFzemW|dDDpckBpfW2jbjDKeZJs[XRiY3XscJMh[XO|ZYPz[YQh[XNiYXPjeY12dGG2aX;uJIF1KEd{L12gdIhie2ViYX\0[ZIhOjRiaILzJJV{cW6pIIDyc5Bq\Gm3bTDpc4Rq\GVic4ThbY5qdmdiYomgSmFEWyCjbnHsfZNqeyxiSVO1NF0xNjF4IN88US=> NXvCOVhqOjFzMk[wNlc>
SW620 cells M37MTGN6fG:2b4jpZ4l1gSCjc4PhfS=> MWO0PE04OiCq M3HCNGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNYPjJyIHPlcIx{KGGodHXyJFQ5KHSxIEeyJIhzeyCkeTDXRXQuOSCjc4PhfUwhUUN3ME2wMlE6KM7:TR?= M4\EWFIyOTJ4MEK3
A2780 cells NHPpRpFEgXSxdH;4bYNqfHliYYPzZZk> Moi1OFguPzJiaB?= MWTDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBNlc5OCClZXzsd{Bi\nSncjC0PEB1dyB5MjDodpMh[nliV1HUMVEh[XO|YYmsJGlEPTB;MD6xO{DPxE1? M{\ZO|IyOTJ4MEK3
HT-29 cells MmjsVJJwdGmoZYLheIlwdiCjc4PhfS=> NXW0O2FzPzJiaB?= MV\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiWLUK5JINmdGy|IHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:OC5{MTFOwG0> MlXaNlMzODJ6NEm=
HUVEC NVr5fIV7TnWwY4Tpc44h[XO|YYm= MkXhNVAxNTFyMECgcm0> NYC1TGVDPCCq Mm\4TY5lfWO2aX;uJI9nKH[jc3P1cIFzKGSrc4L1dJRqdmdiYXP0bZZqfHliaX6gTHVXTUNiYYPz[ZN{\WRiYYOgWmVITi2rbnT1Z4VlKHS3YnWg[o9zdWG2aX;uJIF1KDFyMDD0c{AyODByIH7NJIFnfGW{IESgbJJ{KGK7IH3pZ5Jwe2OxcHnjJIFv[Wy7c3nz Mlf2NlQyODZ7OEK=
H460 cells NX[2ZmFxS3m2b4TvfIlkcXS7IHHzd4F6 M1u2TVczKGh? NEPWS5hEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJPDZyIHPlcIx{KGG|c3Xzd4VlKGG|IHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDd{IHjyd{BjgSCvZYTofYxmdmViYnz1[UB{fGGrbnnu[{1j[XOnZDDhd5NigSxiSVO1NF0xNjJzN{eg{txO NF3FPYYzPDFyNkm4Ni=>
MKN45 cells MWfDfZRwfG:6aXPpeJkh[XO|YYm= MmX5O|IhcA>? MWLDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNT241PSClZXzsd{Bie3Onc4Pl[EBieyCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkA4OiCqcoOgZpkhdWW2aIns[Y5mKGKudXWgd5RicW6rbnetZoF{\WRiYYPzZZktKEmFNUC9NE4yPjZizszN NV;SWoNTOjRzME[5PFI>
HT-29 cells MVHDfZRwfG:6aXPpeJkh[XO|YYm= MX63NkBp M3y4NGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhVNTJ7IHPlcIx{KGG|c3Xzd4VlKGG|IHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDd{IHjyd{BjgSCvZYTofYxmdmViYnz1[UB{fGGrbnnu[{1j[XOnZDDhd5NigSxiSVO1NF0xNjN|OEeg{txO MX[yOFExPjl6Mh?=
human A549 cells NV;CepRUS3m2b4TvfIlkcXS7IHHzd4F6 MnLjOFghcA>? M3e0[WN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGE2PDliY3XscJMh[W[2ZYKgOFghcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2xMlMyKM7:TR?= MoO5NlQ5OzV5OE[=
ACHN cells NXHwSWhNS3m2b4TvfIlkcXS7IHHzd4F6 NWXjfWw2PDhiaB?= MWPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBR2hPKGOnbHzzJIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;Mj6xN{DPxE1? MWSyOFg{PTd6Nh?=
MCF7 cells NHfvOVZEgXSxdH;4bYNqfHliYYPzZZk> Mo\TOFghcA>? M2fFSWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1ETjdiY3XscJMh[W[2ZYKgOFghcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2xMlI2KM7:TR?= NILoeYczPDh|NUe4Oi=>
HT-29 cells M3K0U2N6fG:2b4jpZ4l1gSCjc4PhfS=> MYi0PEBp MUPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIWE0zQSClZXzsd{Bi\nSncjC0PEBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUGuOlIh|ryP NH\V[WEzPDh|NUe4Oi=>
A549 cells NYC4V4hZWHKxbHnm[ZJifGmxbjDhd5NigQ>? MX[yOEBp M1i3[GFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUW0PUBk\WyuczDhd5Nme3OnZDDhd{Boem:5dHigbY5pcWKrdHnvckBi\nSncjCyOEBpenNiYomgV3JDKGG|c3H5MEBIUTVyPUGuN|Eh|ryP M32xSFI2PDZ6MEO5
human MCF7 cells M1j0VXBzd2yrZnXyZZRqd25iYYPzZZk> MWmyOEBp M{HobGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVPGO{Bk\WyuczDhd5Nme3OnZDDhd{Boem:5dHigbY5pcWKrdHnvckBi\nSncjCyOEBpenNiYomgV3JDKGG|c3H5MEBIUTVyPUGuNlUh|ryP NFjX[lkzPTR4OECzPS=>
KB-S15 cells NUT1eoxzS3m2b4TvfIlkcXS7IHHzd4F6 NH[xR3o4OiCq M123eWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGtDNVNzNTDj[YxteyCxdnXy[ZhxemW|c3nu[{BRNWeyMUewM21FWiCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB5MjDodpMh[nlibXX0bJlt\W6nIHLseYUhe3SjaX7pcocu[mG|ZXSgZZN{[XluIFnDOVA:OC5{ME[g{txO MmrsNlQyODZ7OEK=
KB-7d cells MV3DfZRwfG:6aXPpeJkh[XO|YYm= MkT4O|IhcA>? NVzqOFZuS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hU0JvN3SgZ4VtdHNib4\ldoV5eHKnc4PpcochVVKSIHHzd4V{e2WmIHHzJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IEeyJIhzeyCkeTDt[ZRpgWynbnWgZox2\SC|dHHpcolv\y2kYYPl[EBie3OjeTygTWM2OD1yLkKwOUDPxE1? M1Lw[FI1OTB4OUiy
KB-VIN10 cells NF3WbWVEgXSxdH;4bYNqfHliYYPzZZk> M2j1PVczKGh? NHfVUItEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBMSi2YSV6xNEBk\WyuczDveoVz\XiycnXzd4lv\yCSLXfwNVcxN02GUjDhd5Nme3OnZDDhd{Boem:5dHigbY5pcWKrdHnvckBi\nSncjC3NkBpenNiYomgcYV1cHmuZX7lJIJtfWVic4ThbY5qdmdvYnHz[YQh[XO|YYmsJGlEPTB;MD6yNlch|ryP NILjXoYzPDFyNkm4Ni=>
human PC3 cells NVrHUlZCS3m2b4TvfIlkcXS7IHHzd4F6 NVnTdnBOPDhiaB?= M{XacGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHBEOyClZXzsd{Bie3Onc4Pl[EBieyCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkA1QCCqcoOgZpkhe3WuZn;ybI9l[W2rbnWgRkBie3OjeTygS2k2OD1yLk[yJO69VQ>? NV7DTllmOjZ{NEGwN|I>
human AsPC1 cells NWLjRW9GS3m2b4TvfIlkcXS7IHHzd4F6 Mmr4OFghcA>? NYG4S|ZiS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSXOSQ{GgZ4VtdHNiYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiNEigbJJ{KGK7IIP1cIZwemixZHHtbY5mKEJiYYPzZZktKEeLNUC9OE4yOSEQvF2= NVXsVos2OjZ{NEGwN|I>
human A549 cells MX\DfZRwfG:6aXPpeJkh[XO|YYm= NXLBcnl7PDhiaB?= M4KwXGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGE2PDliY3XscJMh[XO|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPDhiaILzJIJ6KHO3bH\vdohw\GGvaX7lJGIh[XO|YYmsJGdKPTB;NT6zN{DPxE1? MYeyOlI1OTB|Mh?=
Hep3B cells NXzIdmpKS3m2b4TvfIlkcXS7IHHzd4F6 M1jiXFQ5KGh? NWHKSmQ3S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUGWyM1KgZ4VtdHNiYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiNEigbJJ{KGK7IIP1cIZwemixZHHtbY5mKEJiYYPzZZktKEeLNUC9NE45PCEQvF2= NFL6dmUzPjJ2MUCzNi=>
KB cells M1noemN6fG:2b4jpZ4l1gSCjc4PhfS=> M1TxfVczKGh? M1\6eWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGtDKGOnbHzzJIF{e2W|c3XkJIF{KGe{b4f0bEBqdmirYnn0bY9vKGGodHXyJFczKGi{czDifUBu\XSqeXzlcoUh[my3ZTDzeIFqdmmwZz3iZZNm\CCjc4PhfUwhUUN3ME2wMlI2OTNizszN NYThS|JOOjRzME[5PFI>
DU145 cells MlG3VJJwdGmoZYLheIlwdiCjc4PhfS=> NYfmOFVvOjRiaB?= NULrTJRpSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDEWVE1PSClZXzsd{Bie3Onc4Pl[EBieyCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkAzPCCqcoOgZpkhW1KEIHHzd4F6NCCJSUWwQVEvQDFizszN Mon4NlU1PjhyM{m=
DU145 cells NUHJVm16S3m2b4TvfIlkcXS7IHHzd4F6 NGHG[5A1QCCq MnXNR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gSHUyPDViY3XscJMh[W[2ZYKgOFghcHK|IHL5JG1VXCCjc4Phfg+9lCCJSUWwQVEvQDFizszN MX:yOFg{PTd6Nh?=
human SKBR3 cells NV\3blFpT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFPZWGQ1QCCq NFz0OnJIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBUU0KUMzDj[YxteyCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVAvPzRizszN NHTzbnAzOjh3MEKxOC=>
In vivo In this Calu-6 xenograft model, ABT-751 as a single agent at 100 and 75 mg/kg/day shows significant antitumor activity, while in combination with cisplatin, ABT-751 shows a dose-dependent enhancement in growth delay. In the HT-29 colon xenograft model, ABT-751 also shows significant antitumor activity as a single agent and produced a dose-dependent enhancement in growth delay In combination with 5-FU. [2] In dogs with lymphoma, ABT-751 exhibits the dose-limiting toxicities that included vomiting, diarrhea, anorexia, or some combination of these with a maximum tolerated dose (MTD) of 350 mg/m2 PO q24h. Furthermore, the mean AUC and Cmax for ABT-751 at the MTD of 350 mg/m2 is 5.55 μg-hour/mL and 0.9 μg/mL, respectively. [3]

Protocol (from reference)

Cell Research:[1]
  • Cell lines: HOS, HTB-186 Daoy, TC-71, RD, SK-N-AS, SK-N-DZ, LD and KCNR cells
  • Concentrations: 0 to 100 μM
  • Incubation Time: 72 hours
  • Method: Cells, in 1640 RPMI media with FBS, are plated in triplicate onto 96 well tissue culture plates in numbers determined optimal for confluent monolayer growth (5,000 cells/well for HOS, HTB-186 Daoy; 10,000 cells/well for TC-71, RD, SK-N-AS, SK-N-DZ, LD; 30,000 cells/well for KCNR), with an automated, multichannel pipette system. Cells are incubated for 24 hours at 37 °C/5% CO2 then exposed to vehicle control (1.25% DMSO/H2O), VCR (0.1–1000 nM), ABT-751 (0.1 nM–100 μM), and in 4 cell lines (SK-N-AS, KCNR, RD, TC-71) combretastatin (0.1–1000 nM) for 72 hours. Cells are fixed with trichloroacetic acid (final concentration 10%) at 4 °C, washed, then dried at room temperature, stained with SRB in 1% acetic acid and dye is then solubilized with Tris base. Optical density measurements are performed at 540 and 405 nm dual wavelengths in a Bio-Tek EL 340 UV plate reader.
Animal Research:[2]
  • Animal Models: Calu-6 NSCLC, HT-29 colon, and HCT-116 cells are injected into athymic mice.
  • Dosages: 75 or 100 mg/kg/day
  • Administration: Administered via p.o.

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
30% propylene glycol, 5% Tween 80, 65% D5W
For best results, use promptly after mixing.

15 mg/mL

Chemical Information

Molecular Weight 371.41
Formula

C18H17N3O4S

CAS No. 141430-65-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles COC1=CC=C(C=C1)S(=O)(=O)NC2=C(N=CC=C2)NC3=CC=C(C=C3)O

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT00436852 Completed Drug: ABT-751|Procedure: quality-of-life assessment Disseminated Neuroblastoma|Recurrent Neuroblastoma Children''s Oncology Group|National Cancer Institute (NCI) January 2007 Phase 2
NCT00735878 Terminated Drug: ABT-751 and Carboplatin Non Small Cell Lung Cancer|Lung Cancer Konstantin Dragnev|Abbott|Dartmouth-Hitchcock Medical Center September 2004 Phase 1|Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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