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

3 Customer Reviews

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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 M1nD[nBzd2yrZnXyZZRqd25iYYPzZZk> NYnNeWxQSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDjc4xwdiClYYLjbY5wdWFiSFPUMVE2KGOnbHygcIlv\SiPRGKoMUkqNCCLQ{WwQVAvOzRizszN Mk\2NVE1OjV3M{S=
HCT116-C9 cell M1\5bGZ2dmO2aX;uJIF{e2G7 MYPF[oZm[3SrdnWgZ49v[2WwdILheIlwdiC2bzDpcohq[mm2IHPlcIwheHKxbHnm[ZJifGmxbjDifUA2OCVicnXsZZRqfmVidH:geY51emWjdHXkJINwdnS{b3ygZ4VtdCCjZoTldkA4OiCqcjDv[kBkd262aX71c5V{KGW6cH;zeZJmKGmwIFjDWFEyPi2FOTDj[YxtKGyrbnWsJGlEPTB;MD65JO69VQ>? MX:xNlM5OzBzNx?=
NCI-H460 cell MoXBVJJwdGmoZYLheIlwdiCjc4PhfS=> NU[0bVVjSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDseY5oKGOjcnPpco9u[SCQQ1mtTFQ3OCClZXzsJIxqdmViKF3EVkgsMSluIFnDOVA:OC5|NTFOwG0> NX[xRWtMOTF2MkW1N|Q>
P388 cell line MX7GeY5kfGmxbjDhd5NigQ>? MWe3NkBp MUHF[oZm[3SrdnWgZ49v[2WwdILheIlwdiC2bzDpcohq[mm2IHPlcIwheHKxbHnm[ZJifGmxbjDifUA2OCVicnXsZZRqfmVidH:geY51emWjdHXkJINwdnS{b3ygZ4VtdCCjZoTldkA4OiCqcjDv[kBkd262aX71c5V{KGW6cH;zeZJmKGmwIGCzPFgh[2WubDDsbY5m97zOIFnDOVA:OC5zOTFOwG0> NFzKWHUyOjN6M{CxOy=>
P388/4.0 r-M cell line NFfZU3hHfW6ldHnvckBie3OjeR?= M1zyZVczKGh? MkHrSYZn\WO2aY\lJINwdmOnboTyZZRqd25idH:gbY5pcWKrdDDj[YxtKHC{b3zp[oVz[XSrb36gZpkhPTBnIILlcIF1cX[nIITvJJVvfHKnYYTl[EBkd262cn;sJINmdGxiYX\0[ZIhPzJiaIKgc4Yh[2:wdHnueY92eyCneIDvd5Vz\SCrbjDQN|g5NzRwMDDyMW0h[2WubDDsbY5mNCCLQ{WwQVE2KM7:TR?= M2LjWVEzOzh|MEG3
human HL60 cells M3q0WnBzd2yrZnXyZZRqd25iYYPzZZk> NHLpUplCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjMOlAh[2WubIOsJGlEPTB;MD6zOEDPxE1? NIGxZ3YyPzJ5NkC1Oi=>
HeLa cells NYLtdZM1S3m2b4TvfIlkcXS7IHHzd4F6 M1z6b|Q5NTd{IHi= M4HUT2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhmVGFiY3XscJMh[W[2ZYKgOFghfG9iN{KgbJJ{KGK7IGfBWE0yKGG|c3H5MEBKSzVyPUCuNlch|ryP M{\ucFIyOTJ4MEK3
MDR1 cells NILwbGNEgXSxdH;4bYNqfHliYYPzZZk> MojTOFguPzJiaB?= NU\0fmRKS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVkOLLVHEVk1TTVNiZYjwdoV{e2mwZzDNSHIyKGOnbHzzJIFnfGW{IES4JJRwKDd{IHjyd{BjgSCZQWStNUBie3OjeTygTWM2OD1yLkK5JO69VQ>? NFLHUpAzOTF{NkCyOy=>
Jurkat cells MYLGeY5kfGmxbjDhd5NigQ>? NGDXZWozPCCq NIXjWYRE\WyuIHP5Z4xmKGG{cnXzeEBqdiCqdX3hckBLfXKtYYSgZ4VtdHNiYYPz[ZN{\WRiYYOgZYNkfW23bHH0bY9vKGG2IFeyM20heGijc3WgZYZ1\XJiMkSgbJJ{KHW|aX7nJJBzd3CrZHn1cUBqd2SrZHWgd5RicW6rbnegZpkhTkGFUzDhcoFtgXOrczygTWM2OD1yLkG2JO69VQ>? NYK3SldFOjFzMk[wNlc>
SW620 cells MVrDfZRwfG:6aXPpeJkh[XO|YYm= NFHaPWQ1QC15MjDo Mlu3R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV3c3OjBiY3XscJMh[W[2ZYKgOFghfG9iN{KgbJJ{KGK7IGfBWE0yKGG|c3H5MEBKSzVyPUCuNVkh|ryP M335elIyOTJ4MEK3
A2780 cells NWGwVZljS3m2b4TvfIlkcXS7IHHzd4F6 NF;NZnI1QC15MjDo MWnDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBNlc5OCClZXzsd{Bi\nSncjC0PEB1dyB5MjDodpMh[nliV1HUMVEh[XO|YYmsJGlEPTB;MD6xO{DPxE1? MUGyNVEzPjB{Nx?=
HT-29 cells MV\Qdo9tcW[ncnH0bY9vKGG|c3H5 MXq3NkBp MXzBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiWLUK5JINmdGy|IHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:OC5{MTFOwG0> NVvNNYFYOjN{MEK4OFk>
HUVEC MlnMSpVv[3Srb36gZZN{[Xl? NUfrbVVIOTByLUGwNFAhdk1? NVHnephYPCCq M{[5VWlv\HWldHnvckBw\iC4YYPjeYxieiCmaYPyeZB1cW6pIHHjeIl3cXS7IHnuJGhWXkWFIHHzd4V{e2WmIHHzJHZGT0ZvaX7keYNm\CC2dXLlJIZwem2jdHnvckBifCBzMECgeI8hOTByMDDuUUBi\nSncjC0JIhzeyCkeTDtbYNzd3Olb4DpZ{BidmGueYPpdy=> Mn\BNlQyODZ7OEK=
H460 cells NVzkUXJIS3m2b4TvfIlkcXS7IHHzd4F6 M3rUWVczKGh? M4HNUWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGg1PjBiY3XscJMh[XO|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPzJiaILzJIJ6KG2ndHj5cIVv\SCkbIXlJJN1[WmwaX7nMYJie2WmIHHzd4F6NCCLQ{WwQVAvOjF5NzFOwG0> NYLXO4FPOjRzME[5PFI>
MKN45 cells MlfOR5l1d3SxeHnjbZR6KGG|c3H5 MmL4O|IhcA>? MX\DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNT241PSClZXzsd{Bie3Onc4Pl[EBieyCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkA4OiCqcoOgZpkhdWW2aIns[Y5mKGKudXWgd5RicW6rbnetZoF{\WRiYYPzZZktKEmFNUC9NE4yPjZizszN MVWyOFExPjl6Mh?=
HT-29 cells M2fjbWN6fG:2b4jpZ4l1gSCjc4PhfS=> NFPSW5Q4OiCq MnXmR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTHQuOjliY3XscJMh[XO|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPzJiaILzJIJ6KG2ndHj5cIVv\SCkbIXlJJN1[WmwaX7nMYJie2WmIHHzd4F6NCCLQ{WwQVAvOzN6NzFOwG0> MmXjNlQyODZ7OEK=
human A549 cells M3vC[GN6fG:2b4jpZ4l1gSCjc4PhfS=> MmrIOFghcA>? NGC5d|VEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCPTR7IHPlcIx{KGGodHXyJFQ5KGi{czDifUBOXFRiYYPzZZktKEmFNUC9NU4{OSEQvF2= NUXUNGk5OjR6M{W3PFY>
ACHN cells NXPRPXFMS3m2b4TvfIlkcXS7IHHzd4F6 NEPab3Q1QCCq MUHDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBR2hPKGOnbHzzJIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;Mj6xN{DPxE1? M3S3[VI1QDN3N{i2
MCF7 cells NH:0b|hEgXSxdH;4bYNqfHliYYPzZZk> MUK0PEBp NH3KZXlEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOS0Z5IHPlcIx{KGGodHXyJFQ5KGi{czDifUBOXFRiYYPzZZktKEmFNUC9NU4zPSEQvF2= NX;iPJJ6OjR6M{W3PFY>
HT-29 cells NYjsb|Q{S3m2b4TvfIlkcXS7IHHzd4F6 MknsOFghcA>? NIrDdXhEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJXC1{OTDj[YxteyCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVEvPjJizszN M1LidVI1QDN3N{i2
A549 cells NWnlXpNwWHKxbHnm[ZJifGmxbjDhd5NigQ>? NFHkN2wzPCCq NIXzfm5CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFG1OFkh[2WubIOgZZN{\XO|ZXSgZZMh\3Kxd4ToJIlvcGmkaYTpc44h[W[2ZYKgNlQhcHK|IHL5JHNTSiCjc4PhfUwhT0l3ME2xMlMyKM7:TR?= Mn\KNlU1PjhyM{m=
human MCF7 cells M3TYRXBzd2yrZnXyZZRqd25iYYPzZZk> M2XSb|I1KGh? NEHQ[2hCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3DSlch[2WubIOgZZN{\XO|ZXSgZZMh\3Kxd4ToJIlvcGmkaYTpc44h[W[2ZYKgNlQhcHK|IHL5JHNTSiCjc4PhfUwhT0l3ME2xMlI2KM7:TR?= MnvTNlU1PjhyM{m=
KB-S15 cells MUXDfZRwfG:6aXPpeJkh[XO|YYm= NXThUG9VPzJiaB?= NYHuVWxnS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hU0JvU{G1JINmdGy|IH;2[ZJmgHC{ZYPzbY5oKFBvZ4CxO|AwVUSUIHHzd4V{e2WmIHHzJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IEeyJIhzeyCkeTDt[ZRpgWynbnWgZox2\SC|dHHpcolv\y2kYYPl[EBie3OjeTygTWM2OD1yLkKwOkDPxE1? MYiyOFExPjl6Mh?=
KB-7d cells MoPUR5l1d3SxeHnjbZR6KGG|c3H5 MnvaO|IhcA>? NI[xbJZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBMSi15ZDDj[YxteyCxdnXy[ZhxemW|c3nu[{BOWlBiYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiN{KgbJJ{KGK7IH3leIh6dGWwZTDicJVmKHO2YXnubY5oNWKjc3XkJIF{e2G7LDDJR|UxRTBwMkC1JO69VQ>? NG[3NXgzPDFyNkm4Ni=>
KB-VIN10 cells NGP0XpJEgXSxdH;4bYNqfHliYYPzZZk> M4npNFczKGh? MWPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDLRk1XUU5zMDDj[YxteyCxdnXy[ZhxemW|c3nu[{BRNWeyMUewM21FWiCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB5MjDodpMh[nlibXX0bJlt\W6nIHLseYUhe3SjaX7pcocu[mG|ZXSgZZN{[XluIFnDOVA:OC5{Mkeg{txO MVyyOFExPjl6Mh?=
human PC3 cells MV\DfZRwfG:6aXPpeJkh[XO|YYm= MWi0PEBp NUDOdndjS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hWEN|IHPlcIx{KGG|c3Xzd4VlKGG|IHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDR6IHjyd{BjgSC|dXzmc5Jpd2SjbXnu[UBDKGG|c3H5MEBIUTVyPUCuOlIh|ryP M2rTTVI3OjRzMEOy
human AsPC1 cells MkLLR5l1d3SxeHnjbZR6KGG|c3H5 M4T1WlQ5KGh? NG[5XWFEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCe1CFMTDj[YxteyCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB2ODDodpMh[nlic4Xs[o9zcG:mYX3pcoUhSiCjc4PhfUwhT0l3ME20MlEyKM7:TR?= MUCyOlI1OTB|Mh?=
human A549 cells M{TV[WN6fG:2b4jpZ4l1gSCjc4PhfS=> MlvWOFghcA>? NVP3XXl6S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSTV2OTDj[YxteyCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB2ODDodpMh[nlic4Xs[o9zcG:mYX3pcoUhSiCjc4PhfUwhT0l3ME21MlM{KM7:TR?= MlL5NlYzPDFyM{K=
Hep3B cells NIrZT4NEgXSxdH;4bYNqfHliYYPzZZk> M4TRWVQ5KGh? NVT1NJNNS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUGWyM1KgZ4VtdHNiYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiNEigbJJ{KGK7IIP1cIZwemixZHHtbY5mKEJiYYPzZZktKEeLNUC9NE45PCEQvF2= NGPYdlEzPjJ2MUCzNi=>
KB cells NGfxT3pEgXSxdH;4bYNqfHliYYPzZZk> M1PTUlczKGh? MnXjR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gT2Ih[2WubIOgZZN{\XO|ZXSgZZMh\3Kxd4ToJIlvcGmkaYTpc44h[W[2ZYKgO|IhcHK|IHL5JI1mfGi7bHXu[UBjdHWnIIP0ZYlvcW6pLXLhd4VlKGG|c3H5MEBKSzVyPUCuNlUyOyEQvF2= Mm[yNlQyODZ7OEK=
DU145 cells M4PNSnBzd2yrZnXyZZRqd25iYYPzZZk> MXuyOEBp MoHMRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCGVUG0OUBk\WyuczDhd5Nme3OnZDDhd{Boem:5dHigbY5pcWKrdHnvckBi\nSncjCyOEBpenNiYomgV3JDKGG|c3H5MEBIUTVyPUGuPFEh|ryP MXWyOVQ3QDB|OR?=
DU145 cells MVrDfZRwfG:6aXPpeJkh[XO|YYm= NFTKWnE1QCCq M{\YemN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGRWOTR3IHPlcIx{KGGodHXyJFQ5KGi{czDifUBOXFRiYYPzZZnwxIxiR1m1NF0yNjhzIN88US=> NUOxemlQOjR6M{W3PFY>
human SKBR3 cells NUP4bJVrT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NG[1bVQ1QCCq M4DqNGdzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJHNMSlJ|IHPlcIx{KGGodHXyJFQ5KGi{czDifUBOXFRiYYPzZZktKEmFNUC9NE44PCEQvF2= MojkNlI5PTB{MUS=
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 2022-11-29)

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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