ABT-751 (E7010)

Catalog No.S1165

ABT-751 (E7010) Chemical Structure

Molecular Weight(MW): 371.41

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.

Size Price Stock Quantity  
In DMSO USD 160 In stock
USD 120 In stock
USD 470 In stock
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Cited by 2 Publications

3 Customer Reviews

  • Cell viability in H292 monolayer cells after 3-day treatment and spheroid volume in H292 3D culture after 7-day treatment with ABT751. Data points are means ?SD for three individual experiments. IC50 values were calculated to emphasize the differences in drug potency in 2D verses 3D cultures. ABT751, IC50 of 177.2 ?17.3 nM for 2D and 670.2 ?257.6 nM for 3D.

    Bioorg Med Chem 2013 21, 922-31. ABT-751 (E7010) purchased from Selleck.

    3D spheroid integrity following treatment with ABT751. Representative phase contrast imagines of H292 multi-cellular 3D spheroid at the onset of the treatment and after a 7-day treatment interval with various concentrations. Magnification: 10 X objective, scan bar: 200 μm. Dose and time dependent curves of ABT751 with 3D spheroid assay.

    Bioorg Med Chem 2013 21, 922-31. ABT-751 (E7010) purchased from Selleck.

  • Western blot analysiswas used to validate the regulation of β1-tubulin to vinculin. (A) Inhibited effects of ABT-751 on the β1-tubulin.Washed human plateletswere treatedwith 0, 2.5, 5, 10 and 20 μg/ml ABT-751 for 60 min then stimulated with 0.3 U thrombin (B) Protein expression of vinculin and Talin1 in washed platelets. The representative bands were from different gels for repeated experiments. After densitometric analysis, the values of proteins were normalized against GAPDH, respectively. Data are shown as the mean ± S.D. (n =3-4 per group). ##P < 0.01 vs normal group, **P < 0.01 vs thrombin group, ++P < 0.01 vs thrombin group.

    Fitoterapia, 2017, 116:106-115. ABT-751 (E7010) purchased from Selleck.

Purity & Quality Control

Choose Selective Microtubule Associated Inhibitors

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 M3rDZXBzd2yrZnXyZZRqd25iYYPzZZk> MUfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKGOxbH;uJINiemOrbn;tZUBJS1RvMUWgZ4VtdCCuaX7lLG1FWihvKTmsJGlEPTB;MD6zOEDPxE1? M1rITFEyPDJ3NUO0
HCT116-C9 cell M4naSmZ2dmO2aX;uJIF{e2G7 MVTF[oZm[3SrdnWgZ49v[2WwdILheIlwdiC2bzDpcohq[mm2IHPlcIwheHKxbHnm[ZJifGmxbjDifUA2OCVicnXsZZRqfmVidH:geY51emWjdHXkJINwdnS{b3ygZ4VtdCCjZoTldkA4OiCqcjDv[kBkd262aX71c5V{KGW6cH;zeZJmKGmwIFjDWFEyPi2FOTDj[YxtKGyrbnWsJGlEPTB;MD65JO69VQ>? M1SxU|EzOzh|MEG3
NCI-H460 cell NFe3OotRem:uaX\ldoF1cW:wIHHzd4F6 MoPvRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCudX7nJINiemOrbn;tZUBPS0lvSES2NEBk\WyuIHzpcoUhME2GUjirLUktKEmFNUC9NE4{PSEQvF2= NFHJTZIyOTR{NUWzOC=>
P388 cell line M33x[2Z2dmO2aX;uJIF{e2G7 NV3qOoZQPzJiaB?= NHqzdopG\m[nY4TpeoUh[2:wY3XueJJifGmxbjD0c{BqdmirYnn0JINmdGxicILvcIln\XKjdHnvckBjgSB3MDWgdoVt[XSrdnWgeI8hfW62cnXheIVlKGOxboTyc4wh[2WubDDh[pRmeiB5MjDodkBw\iClb370bY52d3W|IHX4dI9{fXKnIHnuJHA{QDhiY3XscEBtcW6n78{MJGlEPTB;MD6xPUDPxE1? MWWxNlM5OzBzNx?=
P388/4.0 r-M cell line MXjGeY5kfGmxbjDhd5NigQ>? MWW3NkBp M{XOUmVn\mWldHn2[UBkd26lZX70doF1cW:wIITvJIlvcGmkaYSgZ4VtdCCycn;sbYZmemG2aX;uJIJ6KDVyJTDy[YxifGm4ZTD0c{B2dnS{ZXH0[YQh[2:wdILvcEBk\WyuIHHmeIVzKDd{IHjyJI9nKGOxboTpcpVwfXNiZYjwc5N2emViaX6gVFM5QC92LkCgdk1OKGOnbHygcIlv\SxiSVO1NF0yPSEQvF2= MkjmNVI{QDNyMUe=
human HL60 cells MVjQdo9tcW[ncnH0bY9vKGG|c3H5 MXrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiONkCgZ4VtdHNuIFnDOVA:OC5|NDFOwG0> M1;3WlE4Ojd4MEW2
HeLa cells NFv6e45EgXSxdH;4bYNqfHliYYPzZZk> M2rjUVQ5NTd{IHi= M2PBRmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhmVGFiY3XscJMh[W[2ZYKgOFghfG9iN{KgbJJ{KGK7IGfBWE0yKGG|c3H5MEBKSzVyPUCuNlch|ryP NHfme4czOTF{NkCyOy=>
MDR1 cells NUDDc4RzS3m2b4TvfIlkcXS7IHHzd4F6 MmTUOFguPzJiaB?= Ml[xR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUmNKNUGGUj3SSXMh\XiycnXzd4lv\yCPRGKxJINmdGy|IHHmeIVzKDR6IITvJFczKGi{czDifUBYSVRvMTDhd5NigSxiSVO1NF0xNjJ7IN88US=> Mkj2NlEyOjZyMke=
Jurkat cells MlHiSpVv[3Srb36gZZN{[Xl? NXzHPXZCOjRiaB?= NFnqSJdE\WyuIHP5Z4xmKGG{cnXzeEBqdiCqdX3hckBLfXKtYYSgZ4VtdHNiYYPz[ZN{\WRiYYOgZYNkfW23bHH0bY9vKGG2IFeyM20heGijc3WgZYZ1\XJiMkSgbJJ{KHW|aX7nJJBzd3CrZHn1cUBqd2SrZHWgd5RicW6rbnegZpkhTkGFUzDhcoFtgXOrczygTWM2OD1yLkG2JO69VQ>? Mnj5NlEyOjZyMke=
SW620 cells NUTqc405S3m2b4TvfIlkcXS7IHHzd4F6 Mn7HOFguPzJiaB?= NFLHPZNEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUXzZ{MDDj[YxteyCjZoTldkA1QCC2bzC3NkBpenNiYomgW2FVNTFiYYPzZZktKEmFNUC9NE4yQSEQvF2= MlHXNlEyOjZyMke=
A2780 cells M{PaZmN6fG:2b4jpZ4l1gSCjc4PhfS=> MWe0PE04OiCq MXfDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBNlc5OCClZXzsd{Bi\nSncjC0PEB1dyB5MjDodpMh[nliV1HUMVEh[XO|YYmsJGlEPTB;MD6xO{DPxE1? NWPyXWtlOjFzMk[wNlc>
HT-29 cells NV\hbXd[WHKxbHnm[ZJifGmxbjDhd5NigQ>? NUm0eHJXPzJiaB?= M1n4dGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSGStNlkh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1yLkKxJO69VQ>? Mkj4NlMzODJ6NEm=
HUVEC NX\u[XBMTnWwY4Tpc44h[XO|YYm= M3S0S|ExOC1zMECwJI5O NHnuSW81KGh? M1LHNGlv\HWldHnvckBw\iC4YYPjeYxieiCmaYPyeZB1cW6pIHHjeIl3cXS7IHnuJGhWXkWFIHHzd4V{e2WmIHHzJHZGT0ZvaX7keYNm\CC2dXLlJIZwem2jdHnvckBifCBzMECgeI8hOTByMDDuUUBi\nSncjC0JIhzeyCkeTDtbYNzd3Olb4DpZ{BidmGueYPpdy=> NV2zO5Q{OjRzME[5PFI>
H460 cells MlnRR5l1d3SxeHnjbZR6KGG|c3H5 MWW3NkBp NFrZdHREgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJPDZyIHPlcIx{KGG|c3Xzd4VlKGG|IHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDd{IHjyd{BjgSCvZYTofYxmdmViYnz1[UB{fGGrbnnu[{1j[XOnZDDhd5NigSxiSVO1NF0xNjJzN{eg{txO MYWyOFExPjl6Mh?=
MKN45 cells M2LId2N6fG:2b4jpZ4l1gSCjc4PhfS=> MUC3NkBp MVLDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNT241PSClZXzsd{Bie3Onc4Pl[EBieyCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkA4OiCqcoOgZpkhdWW2aIns[Y5mKGKudXWgd5RicW6rbnetZoF{\WRiYYPzZZktKEmFNUC9NE4yPjZizszN MmXtNlQyODZ7OEK=
HT-29 cells NVvGSIx1S3m2b4TvfIlkcXS7IHHzd4F6 Ml3QO|IhcA>? Mn;xR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTHQuOjliY3XscJMh[XO|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPzJiaILzJIJ6KG2ndHj5cIVv\SCkbIXlJJN1[WmwaX7nMYJie2WmIHHzd4F6NCCLQ{WwQVAvOzN6NzFOwG0> MYCyOFExPjl6Mh?=
human A549 cells NXywdGVLS3m2b4TvfIlkcXS7IHHzd4F6 NY\qTXBqPDhiaB?= M1;J[mN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGE2PDliY3XscJMh[W[2ZYKgOFghcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2xMlMyKM7:TR?= NFGzepczPDh|NUe4Oi=>
ACHN cells MV7DfZRwfG:6aXPpeJkh[XO|YYm= NH\CXY81QCCq MorTR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRWNJViClZXzsd{Bi\nSncjC0PEBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUKuNVMh|ryP MXyyOFg{PTd6Nh?=
MCF7 cells MWDDfZRwfG:6aXPpeJkh[XO|YYm= NV7vcoZXPDhiaB?= MUPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MT6yOUDPxE1? MknGNlQ5OzV5OE[=
HT-29 cells NX7zfIJVS3m2b4TvfIlkcXS7IHHzd4F6 NVGyU3RFPDhiaB?= MVnDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIWE0zQSClZXzsd{Bi\nSncjC0PEBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUGuOlIh|ryP NY\SWnlxOjR6M{W3PFY>
A549 cells NX;6NIpuWHKxbHnm[ZJifGmxbjDhd5NigQ>? MkT1NlQhcA>? NG\Hc2NCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFG1OFkh[2WubIOgZZN{\XO|ZXSgZZMh\3Kxd4ToJIlvcGmkaYTpc44h[W[2ZYKgNlQhcHK|IHL5JHNTSiCjc4PhfUwhT0l3ME2xMlMyKM7:TR?= MmW5NlU1PjhyM{m=
human MCF7 cells M4XHZnBzd2yrZnXyZZRqd25iYYPzZZk> MWmyOEBp MoDqRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQ1[3JINmdGy|IHHzd4V{e2WmIHHzJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IEK0JIhzeyCkeTDTVmIh[XO|YYmsJGdKPTB;MT6yOUDPxE1? NHSxSHczPTR4OECzPS=>
KB-S15 cells MV;DfZRwfG:6aXPpeJkh[XO|YYm= MlHOO|IhcA>? NGXlNmJEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBMSi2VMUWgZ4VtdHNib4\ldoV5eHKnc4PpcochWC2pcEG3NE9OTFJiYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiN{KgbJJ{KGK7IH3leIh6dGWwZTDicJVmKHO2YXnubY5oNWKjc3XkJIF{e2G7LDDJR|UxRTBwMkC2JO69VQ>? M2nET|I1OTB4OUiy
KB-7d cells NFL6R4VEgXSxdH;4bYNqfHliYYPzZZk> M4\hb|czKGh? NGT3Z|BEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBMSi15ZDDj[YxteyCxdnXy[ZhxemW|c3nu[{BOWlBiYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiN{KgbJJ{KGK7IH3leIh6dGWwZTDicJVmKHO2YXnubY5oNWKjc3XkJIF{e2G7LDDJR|UxRTBwMkC1JO69VQ>? M2m0WFI1OTB4OUiy
KB-VIN10 cells M{\jN2N6fG:2b4jpZ4l1gSCjc4PhfS=> NEDvelM4OiCq MknNR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gT2IuXkmQMUCgZ4VtdHNib4\ldoV5eHKnc4PpcochWC2pcEG3NE9OTFJiYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiN{KgbJJ{KGK7IH3leIh6dGWwZTDicJVmKHO2YXnubY5oNWKjc3XkJIF{e2G7LDDJR|UxRTBwMkK3JO69VQ>? MVqyOFExPjl6Mh?=
human PC3 cells MmC2R5l1d3SxeHnjbZR6KGG|c3H5 MXe0PEBp NUfDd2FZS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hWEN|IHPlcIx{KGG|c3Xzd4VlKGG|IHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDR6IHjyd{BjgSC|dXzmc5Jpd2SjbXnu[UBDKGG|c3H5MEBIUTVyPUCuOlIh|ryP M4DDOFI3OjRzMEOy
human AsPC1 cells MVfDfZRwfG:6aXPpeJkh[XO|YYm= MkXMOFghcA>? NV7ZZo44S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSXOSQ{GgZ4VtdHNiYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiNEigbJJ{KGK7IIP1cIZwemixZHHtbY5mKEJiYYPzZZktKEeLNUC9OE4yOSEQvF2= M2n3UFI3OjRzMEOy
human A549 cells MnHtR5l1d3SxeHnjbZR6KGG|c3H5 NX33T4NqPDhiaB?= NX;2bFlXS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSTV2OTDj[YxteyCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB2ODDodpMh[nlic4Xs[o9zcG:mYX3pcoUhSiCjc4PhfUwhT0l3ME21MlM{KM7:TR?= MnTSNlYzPDFyM{K=
Hep3B cells NGeyUnVEgXSxdH;4bYNqfHliYYPzZZk> NXjrXm1kPDhiaB?= M3LzVWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhmeDOEIHPlcIx{KGG|c3Xzd4VlKGG|IHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDR6IHjyd{BjgSC|dXzmc5Jpd2SjbXnu[UBDKGG|c3H5MEBIUTVyPUCuPFQh|ryP MXuyOlI1OTB|Mh?=
KB cells NH\wOYxEgXSxdH;4bYNqfHliYYPzZZk> Ml[0O|IhcA>? NVrB[oV[S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hU0JiY3XscJMh[XO|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPzJiaILzJIJ6KG2ndHj5cIVv\SCkbIXlJJN1[WmwaX7nMYJie2WmIHHzd4F6NCCLQ{WwQVAvOjVzMzFOwG0> NVv3UXdsOjRzME[5PFI>
DU145 cells NYfuSXc6WHKxbHnm[ZJifGmxbjDhd5NigQ>? Ml;CNlQhcA>? NFT4bVhCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFTVNVQ2KGOnbHzzJIF{e2W|c3XkJIF{KGe{b4f0bEBqdmirYnn0bY9vKGGodHXyJFI1KGi{czDifUBUWkJiYYPzZZktKEeLNUC9NU45OSEQvF2= MYOyOVQ3QDB|OR?=
DU145 cells M2H3WWN6fG:2b4jpZ4l1gSCjc4PhfS=> NVr5O5dbPDhiaB?= NHGzSIZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBFXTF2NTDj[YxteyCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F697zOIFfJOVA:OS56MTFOwG0> NVKwNYZiOjR6M{W3PFY>
human SKBR3 cells NIXyNnZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3PkUVQ5KGh? MlH0S5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gV2tDWjNiY3XscJMh[W[2ZYKgOFghcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2wMlc1KM7:TR?= Mn\kNlI5PTB{MUS=

... Click to View More Cell Line Experimental Data

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

Cell Research:[1]
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  • 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.
    (Only for Reference)
Animal Research:[2]
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  • Animal Models: Calu-6 NSCLC, HT-29 colon, and HCT-116 cells are injected into athymic mice.
  • Formulation: ABT-751 is dissolved 4% ethanol/96% dextrose solution (D5W) with 1 eq. 1 N HCl.
  • Dosages: 75 or 100 mg/kg/day
  • Administration: Administered via p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 74 mg/mL (199.24 mM)
Ethanol 12 mg/mL (32.3 mM)
Water Insoluble
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

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 371.41
Formula

C18H17N3O4S

CAS No. 141430-65-1
Storage powder
in solvent
Synonyms N/A

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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

Tel: +1-832-582-8158 Ext:3

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Microtubule Associated Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID