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 NY\MWHNtWHKxbHnm[ZJifGmxbjDhd5NigQ>? MlLBRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiClb3zvckBk[XKlaX7vcYEhUEOWLUG1JINmdGxibHnu[UhOTFJqLTmpMEBKSzVyPUCuN|Qh|ryP M4naT|EyPDJ3NUO0
HCT116-C9 cell MYPGeY5kfGmxbjDhd5NigQ>? MWfF[oZm[3SrdnWgZ49v[2WwdILheIlwdiC2bzDpcohq[mm2IHPlcIwheHKxbHnm[ZJifGmxbjDifUA2OCVicnXsZZRqfmVidH:geY51emWjdHXkJINwdnS{b3ygZ4VtdCCjZoTldkA4OiCqcjDv[kBkd262aX71c5V{KGW6cH;zeZJmKGmwIFjDWFEyPi2FOTDj[YxtKGyrbnWsJGlEPTB;MD65JO69VQ>? M{jQWlEzOzh|MEG3
NCI-H460 cell M2DKVXBzd2yrZnXyZZRqd25iYYPzZZk> NYnkclhNSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDseY5oKGOjcnPpco9u[SCQQ1mtTFQ3OCClZXzsJIxqdmViKF3EVkgsMSluIFnDOVA:OC5|NTFOwG0> NUn4RWlKOTF2MkW1N|Q>
P388 cell line NFfRcZpHfW6ldHnvckBie3OjeR?= M2\BcVczKGh? MV;F[oZm[3SrdnWgZ49v[2WwdILheIlwdiC2bzDpcohq[mm2IHPlcIwheHKxbHnm[ZJifGmxbjDifUA2OCVicnXsZZRqfmVidH:geY51emWjdHXkJINwdnS{b3ygZ4VtdCCjZoTldkA4OiCqcjDv[kBkd262aX71c5V{KGW6cH;zeZJmKGmwIGCzPFgh[2WubDDsbY5m97zOIFnDOVA:OC5zOTFOwG0> NYLXR3NLOTJ|OEOwNVc>
P388/4.0 r-M cell line MYXGeY5kfGmxbjDhd5NigQ>? Mn7yO|IhcA>? NHLEPY5G\m[nY4TpeoUh[2:wY3XueJJifGmxbjD0c{BqdmirYnn0JINmdGxicILvcIln\XKjdHnvckBjgSB3MDWgdoVt[XSrdnWgeI8hfW62cnXheIVlKGOxboTyc4wh[2WubDDh[pRmeiB5MjDodkBw\iClb370bY52d3W|IHX4dI9{fXKnIHnuJHA{QDhxND6wJJIuVSClZXzsJIxqdmVuIFnDOVA:OTVizszN NELXToUyOjN6M{CxOy=>
human HL60 cells MVzQdo9tcW[ncnH0bY9vKGG|c3H5 MlnyRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKTE[wJINmdGy|LDDJR|UxRTBwM{Sg{txO NH3xSYIyPzJ5NkC1Oi=>
HeLa cells MWHDfZRwfG:6aXPpeJkh[XO|YYm= Mmn5OFguPzJiaB?= NFT2SJFEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJ\UyjIHPlcIx{KGGodHXyJFQ5KHSxIEeyJIhzeyCkeTDXRXQuOSCjc4PhfUwhUUN3ME2wMlI4KM7:TR?= NGD4eVczOTF{NkCyOy=>
MDR1 cells NYm0d3F5S3m2b4TvfIlkcXS7IHHzd4F6 M2LFWFQ5NTd{IHi= M3OxdmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG5EUS2DRGKtVmVUKGW6cILld5NqdmdiTVTSNUBk\WyuczDh[pRmeiB2ODD0c{A4OiCqcoOgZpkhX0GWLUGgZZN{[XluIFnDOVA:OC5{OTFOwG0> NVT2OWxkOjFzMk[wNlc>
Jurkat cells Mo\nSpVv[3Srb36gZZN{[Xl? MkfONlQhcA>? MW\D[YxtKGO7Y3zlJIFzemW|dDDpckBpfW2jbjDKeZJs[XRiY3XscJMh[XO|ZYPz[YQh[XNiYXPjeY12dGG2aX;uJIF1KEd{L12gdIhie2ViYX\0[ZIhOjRiaILzJJV{cW6pIIDyc5Bq\Gm3bTDpc4Rq\GVic4ThbY5qdmdiYomgSmFEWyCjbnHsfZNqeyxiSVO1NF0xNjF4IN88US=> NIntfI0zOTF{NkCyOy=>
SW620 cells NGjS[ZhEgXSxdH;4bYNqfHliYYPzZZk> MkXoOFguPzJiaB?= M2K0[WN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNYPjJyIHPlcIx{KGGodHXyJFQ5KHSxIEeyJIhzeyCkeTDXRXQuOSCjc4PhfUwhUUN3ME2wMlE6KM7:TR?= M1;wflIyOTJ4MEK3
A2780 cells NYn4Ro06S3m2b4TvfIlkcXS7IHHzd4F6 M1TlS|Q5NTd{IHi= NVzXUXdtS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSTJ5OECgZ4VtdHNiYX\0[ZIhPDhidH:gO|IhcHK|IHL5JHdCXC1zIHHzd4F6NCCLQ{WwQVAvOTdizszN NHTrS3ozOTF{NkCyOy=>
HT-29 cells MXXQdo9tcW[ncnH0bY9vKGG|c3H5 M4nHelczKGh? NVnRT|VXSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIWE0zQSClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUCuNlEh|ryP Mmq5NlMzODJ6NEm=
HUVEC MVPGeY5kfGmxbjDhd5NigQ>? Mon2NVAxNTFyMECgcm0> MUG0JIg> NFfaZlFKdmS3Y4Tpc44hd2ZidnHzZ5Vt[XJiZHnzdpVxfGmwZzDhZ5Rqfmm2eTDpckBJXV[HQzDhd5Nme3OnZDDhd{BXTUeILXnu[JVk\WRidIXi[UBnd3KvYYTpc44h[XRiMUCwJJRwKDFyMECgcm0h[W[2ZYKgOEBpenNiYomgcYlkem:|Y3;wbYMh[W6jbInzbZM> MmjVNlQyODZ7OEK=
H460 cells NX\xVVR3S3m2b4TvfIlkcXS7IHHzd4F6 NXHy[nplPzJiaB?= Mmj4R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTFQ3OCClZXzsd{Bie3Onc4Pl[EBieyCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkA4OiCqcoOgZpkhdWW2aIns[Y5mKGKudXWgd5RicW6rbnetZoF{\WRiYYPzZZktKEmFNUC9NE4zOTd5IN88US=> NVvib5BYOjRzME[5PFI>
MKN45 cells NGnR[VZEgXSxdH;4bYNqfHliYYPzZZk> MXy3NkBp NVLnZWd[S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUuQNEWgZ4VtdHNiYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiN{KgbJJ{KGK7IH3leIh6dGWwZTDicJVmKHO2YXnubY5oNWKjc3XkJIF{e2G7LDDJR|UxRTBwMU[2JO69VQ>? MonXNlQyODZ7OEK=
HT-29 cells M1vWcmN6fG:2b4jpZ4l1gSCjc4PhfS=> MojFO|IhcA>? M3\mfWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhVNTJ7IHPlcIx{KGG|c3Xzd4VlKGG|IHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDd{IHjyd{BjgSCvZYTofYxmdmViYnz1[UB{fGGrbnnu[{1j[XOnZDDhd5NigSxiSVO1NF0xNjN|OEeg{txO NWHieI1xOjRzME[5PFI>
human A549 cells M4jBO2N6fG:2b4jpZ4l1gSCjc4PhfS=> MknqOFghcA>? NETQdY5EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCPTR7IHPlcIx{KGGodHXyJFQ5KGi{czDifUBOXFRiYYPzZZktKEmFNUC9NU4{OSEQvF2= NFK3SVkzPDh|NUe4Oi=>
ACHN cells M{e2Z2N6fG:2b4jpZ4l1gSCjc4PhfS=> NI\NfWE1QCCq M2HsPWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGFEUE5iY3XscJMh[W[2ZYKgOFghcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2yMlE{KM7:TR?= NEDuV|YzPDh|NUe4Oi=>
MCF7 cells MYjDfZRwfG:6aXPpeJkh[XO|YYm= Ml7POFghcA>? M3PIemN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1ETjdiY3XscJMh[W[2ZYKgOFghcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2xMlI2KM7:TR?= MmHVNlQ5OzV5OE[=
HT-29 cells NFm3N2lEgXSxdH;4bYNqfHliYYPzZZk> MVm0PEBp MYDDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIWE0zQSClZXzsd{Bi\nSncjC0PEBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUGuOlIh|ryP NH;2ZY4zPDh|NUe4Oi=>
A549 cells MoLFVJJwdGmoZYLheIlwdiCjc4PhfS=> NVzE[WJNOjRiaB?= NVXPbHo4SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBOVQ6KGOnbHzzJIF{e2W|c3XkJIF{KGe{b4f0bEBqdmirYnn0bY9vKGGodHXyJFI1KGi{czDifUBUWkJiYYPzZZktKEeLNUC9NU4{OSEQvF2= NETab2IzPTR4OECzPS=>
human MCF7 cells NFzxOVFRem:uaX\ldoF1cW:wIHHzd4F6 NFf3dHozPCCq Mnz1RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQ1[3JINmdGy|IHHzd4V{e2WmIHHzJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IEK0JIhzeyCkeTDTVmIh[XO|YYmsJGdKPTB;MT6yOUDPxE1? NGD3SGYzPTR4OECzPS=>
KB-S15 cells NV31TlViS3m2b4TvfIlkcXS7IHHzd4F6 NHPzN5k4OiCq MUXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDLRk1UOTViY3XscJMhd3[ncnX4dJJme3OrbnegVE1oeDF5MD;NSHIh[XO|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPzJiaILzJIJ6KG2ndHj5cIVv\SCkbIXlJJN1[WmwaX7nMYJie2WmIHHzd4F6NCCLQ{WwQVAvOjB4IN88US=> NI\JcVUzPDFyNkm4Ni=>
KB-7d cells M4\w[mN6fG:2b4jpZ4l1gSCjc4PhfS=> NU\RXVg2PzJiaB?= NHvBeHZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBMSi15ZDDj[YxteyCxdnXy[ZhxemW|c3nu[{BOWlBiYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiN{KgbJJ{KGK7IH3leIh6dGWwZTDicJVmKHO2YXnubY5oNWKjc3XkJIF{e2G7LDDJR|UxRTBwMkC1JO69VQ>? MX2yOFExPjl6Mh?=
KB-VIN10 cells NVPtT256S3m2b4TvfIlkcXS7IHHzd4F6 MV[3NkBp M{P6ZmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGtDNV[LTkGwJINmdGy|IH;2[ZJmgHC{ZYPzbY5oKFBvZ4CxO|AwVUSUIHHzd4V{e2WmIHHzJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IEeyJIhzeyCkeTDt[ZRpgWynbnWgZox2\SC|dHHpcolv\y2kYYPl[EBie3OjeTygTWM2OD1yLkKyO{DPxE1? NHPR[pUzPDFyNkm4Ni=>
human PC3 cells NULTdZl1S3m2b4TvfIlkcXS7IHHzd4F6 NEPrb4w1QCCq NFvESZREgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBRSzNiY3XscJMh[XO|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPDhiaILzJIJ6KHO3bH\vdohw\GGvaX7lJGIh[XO|YYmsJGdKPTB;MD62NkDPxE1? MY[yOlI1OTB|Mh?=
human AsPC1 cells MmO1R5l1d3SxeHnjbZR6KGG|c3H5 NXezOG1qPDhiaB?= NF3u[INEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCe1CFMTDj[YxteyCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB2ODDodpMh[nlic4Xs[o9zcG:mYX3pcoUhSiCjc4PhfUwhT0l3ME20MlEyKM7:TR?= M3LkSFI3OjRzMEOy
human A549 cells NWHSTXlbS3m2b4TvfIlkcXS7IHHzd4F6 NYTNbY1tPDhiaB?= MUjDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBOVQ6KGOnbHzzJIF{e2W|c3XkJIF{KGe{b4f0bEBqdmirYnn0bY9vKGGodHXyJFQ5KGi{czDifUB{fWyob4Loc4RidWmwZTDCJIF{e2G7LDDHTVUxRTVwM{Og{txO M3ThWFI3OjRzMEOy
Hep3B cells M1m4eWN6fG:2b4jpZ4l1gSCjc4PhfS=> NGDSV401QCCq MVvDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDI[ZA{SiClZXzsd{Bie3Onc4Pl[EBieyCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkA1QCCqcoOgZpkhe3WuZn;ybI9l[W2rbnWgRkBie3OjeTygS2k2OD1yLki0JO69VQ>? NWDWTYtKOjZ{NEGwN|I>
KB cells NWm2V2w5S3m2b4TvfIlkcXS7IHHzd4F6 MXq3NkBp MmXUR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gT2Ih[2WubIOgZZN{\XO|ZXSgZZMh\3Kxd4ToJIlvcGmkaYTpc44h[W[2ZYKgO|IhcHK|IHL5JI1mfGi7bHXu[UBjdHWnIIP0ZYlvcW6pLXLhd4VlKGG|c3H5MEBKSzVyPUCuNlUyOyEQvF2= M2XGelI1OTB4OUiy
DU145 cells M4jmVnBzd2yrZnXyZZRqd25iYYPzZZk> NFztNI4zPCCq NX\GZ2ZLSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDEWVE1PSClZXzsd{Bie3Onc4Pl[EBieyCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkAzPCCqcoOgZpkhW1KEIHHzd4F6NCCJSUWwQVEvQDFizszN MWqyOVQ3QDB|OR?=
DU145 cells MVXDfZRwfG:6aXPpeJkh[XO|YYm= M1na[lQ5KGh? NYC4WWtNS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hTFVzNEWgZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5Nige,:jDDHTVUxRTFwOEGg{txO NFXufXIzPDh|NUe4Oi=>
human SKBR3 cells M{DmdGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MWi0PEBp NEPPSnVIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBUU0KUMzDj[YxteyCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVAvPzRizszN NWjobHNQOjJ6NUCyNVQ>
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.
  • (Only for Reference)
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.
  • (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 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)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

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% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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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