Name: Onalespib (AT13387)
Brand: Selleck Chemicals
SKU: S1163
Rating: 5 (19 reviews)

CAS No. 912999-49-6

Selleck's Onalespib (AT13387) has been cited by 19 publications

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HSP (HSP90) Signaling Pathway Map

Biological Activity

Description

Onalespib (AT13387) is a selective potent Hsp90 inhibitor with IC50 of 18 nM in A375 cells, displays a long duration of anti-tumor activity. Phase 2.

Targets

HSP90 ^[1]
(Cell-free assay)

18 nM

In vitro

The K_d for AT13387 binding is 0.7 nM. This compares to a K_d of 6.7 nM for the binding of the ansamycin 17-AAG to the same site. The mean stoichio metry of binding for AT13387 is 1.03. The inhibition of a number of isolated kinases by AT13387 is also investigated including CDK 1, CDK 2, CDK4, FGFR3, PKB-b, JAK2, VEGFR2, PDGFRβ and Aurora B. None of the tested kinases are significantly inhibited at concentrations below 30 μM. AT13387 is a potent inhibitor of the proliferat ion and survival of many different cell lines (such as MES-SA cell line) from a variety of different tumor types. Across a panel of 30 tumor cell lines, AT13387 potently inhibits cell proliferation with GI50 values in the range 13-260 nM. AT13387 inhibits proliferation of the non-tumorigenic human prostate epithelial cell line PNT2 with a GI50 value of 480 nM. ^[2]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID

human HCT116 cells	M1z4XWN6fG:2b4jpZ:Kh[XO\|YYm=			NX;3[JJ[S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUEOWMUG2JINmdGy\|IHL5JGFt[W2jcjDicJVmKGG\|c3H5MEBKSzVyPUCuNFQ5KM7:TR?=	NXzQbmVkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC2OlI2OzRpPkKwOlYzPTN2PD;hQi=>
human HCT116 cells	MmjXSpVv[3Srb36gZZN{[Xl?	M2GyPFExKG6P	M{DJ[VE5KGh?	MlHQTY5lfWO2aX;uJI9nKGGyb4D0c5NqeyCrbjDoeY1idiCKQ2SxNVYh[2WubIOgZZN{\XO\|ZXSgZZMhfXC{ZXf1cIF1cW:wIH;mJGh{eDdyIHzleoVtKGG2IEGwJI5OKGGodHXyJFE5KGi{czDifUBqdW23bn;icI91fGmwZx?=	MoT2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB4NkK1N\|QoRjJyNk[yOVM1RC:jPh?=
human HCT116 cells	MXTGeY5kfGmxbjDhd5NigQ>?	NH;nfG4{OCCwTR?=	NYnu[3dSOThiaB?=	MmDqTY5lfWO2aX;uJI9nKGGyb4D0c5NqeyCrbjDoeY1idiCKQ2SxNVYh[2WubIOgZZN{\XO\|ZXSgZZMhemWmdXP0bY9vKG:oIFPET\|QhdGW4ZXygZZQhOzBibl2gZYZ1\XJiMUigbJJ{KGK7IHntcZVvd2Kub4T0bY5o	MnPQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB4NkK1N\|QoRjJyNk[yOVM1RC:jPh?=
human HCT116 cells	NWrUe3RvTnWwY4Tpc44h[XO\|YYm=	NXvjXJRqOzBibl2=	NIrseVgyQCCq	MoPSTY5lfWO2aX;uJI9nKGGyb4D0c5NqeyCrbjDoeY1idiCKQ2SxNVYh[2WubIOgZZN{\XO\|ZXSgZZMhemWmdXP0bY9vKG:oIGLh[k0yKGyndnXsJIF1KDNyIH7NJIFnfGW{IEG4JIhzeyCkeTDpcY12dm:kbH;0eIlv\w>?	MlzoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB4NkK1N\|QoRjJyNk[yOVM1RC:jPh?=
human HCT116 cells	MXLQdo9tcW[ncnH0bY9vKGG\|c3H5		MV60PEBp	MUDBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiFVEGxOkBk\WyuczDh[pRmeiB2ODDodpMh[nliTWTUJIF{e2G7LDDJR\|UxRTBwMEig{txO	NH7iNo09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEe2N\|I3OSd-MkS3OlMzPjF:L3G+
human SKBR3 cells	M2LsVnBzd2yrZnXyZZRqd25iYYPzZZk>		MUG0PEBp	NU\RWW5{SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTT2JTOyClZXzsd{Bi\nSncjC0PEBpenNiYomgUXRVKGG\|c3H5MEBKSzVyPUCuNVQh\|ryP	M1PnPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2N{[zNlYyLz5{NEe2N\|I3OTxxYU6=
human MCF7 cells	Ml3jVJJwdGmoZYLheIlwdiCjc4PhfS=>		NHHQNlM1QCCq	MlHTRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCPQ1[3JINmdGy\|IHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:OC5{ODFOwG0>	MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDd4M{K2NUc,OjR5NkOyOlE9N2F-
human A231 cells	M3qwcXBzd2yrZnXyZZRqd25iYYPzZZk>		NVHKPIxJPDhiaB?=	MnP0RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCDMkOxJINmdGy\|IHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:OS5yMTFOwG0>	NWrLZ4R4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS3OlMzPjFpPkK0O\|Y{OjZzPD;hQi=>
GIST430	NIHqOWpEgXSxdH;4bYNqfHliYYPzZZk>		MmTQO{Bl[Xm\|	NFLjdYhEgXSxdH;4bYNqfHliYXfhbY5{fCCrbXH0bY5q[i2{ZYPpd5RidnRiaIXtZY4hT0mVVESzNEBk\WyuczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiClZXzsJJZq[WKrbHn0fUBi\nSncjC3JIRigXNiYomgZYxidWG{IHLseYUh[XO\|YYmsJGlEPTB;MD6wN\|TPxE1w	NHzNT4E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nki0OFY5QSd-Mk[4OFQ3QDl:L3G+
GIST48	M2e5cmN6fG:2b4jpZ4l1gSCjc4PhfS=>		M4XYZ\|ch\GG7cx?=	MmPqR5l1d3SxeHnjbZR6KGGpYXnud5QhcW2jdHnubYIuemW\|aYP0ZY51KGi3bXHuJGdKW1R2ODDj[YxteyCjc4Pld5Nm\CCjczDk[YNz\WG\|ZTDpckBk\WyuII\pZYJqdGm2eTDh[pRmeiB5IHThfZMh[nliYXzhcYFzKGKudXWgZZN{[XluIFnDOVA:OC5yNUZOwG0v	MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjh2NE[4PUc,OjZ6NES2PFk9N2F-
MCF7	M2nWc2FvfGmycn;sbYZmemG2aY\lJIF{e2G7		MluzO\|IhcHK\|	MknzRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCPQ1[3JINmdGy\|IHnuZ5Vj[XSnZDDmc5IhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0xNjB\|Mt88UU4>	MmDJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjlyMki1NlcoRjJ7MEK4OVI4RC:jPh?=
SKBR3	MY\BcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?		NVfCSnF[PzJiaILz	M2TnSWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1vCVlMh[2WubIOgbY5kfWKjdHXkJIZweiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR\|UxRTBwMES1{txONg>?	MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTB{OEWyO{c,OjlyMki1Nlc9N2F-
TC32	Mnf4dWhVWyCjc4PhfS=>			NVfEbpIzeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IGTDN\|Ih[2WubIO=	MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
DAOY	M3H6cZFJXFNiYYPzZZk>			MYjxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhTEGRWTDj[Yxtew>?	NHvsXYg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
SJ-GBM2	MnG5dWhVWyCjc4PhfS=>			MlLTdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKFOMLVfCUVIh[2WubIO=	NEHnbHo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
A673	MX\xTHRUKGG\|c3H5			MYrxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSTZ5MzDj[Yxtew>?	Mnn1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
SK-N-MC	MYTxTHRUKGG\|c3H5			MUDxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0tvTj3NR{Bk\Wyucx?=	NFz3VpY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
NB-EBc1	MVfxTHRUKGG\|c3H5			M{PD[pFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCQQj3FRoMyKGOnbHzz	M{LvOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Saos-2	NWfpWXlCeUiWUzDhd5NigQ>?			NXrJSWx[eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IGPhc5MuOiClZXzsdy=>	NUfIS5dqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-SH	Mkj3dWhVWyCjc4PhfS=>			MXLxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0tvTj3TTEBk\Wyucx?=	M{XwOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
NB1643	MUPxTHRUKGG\|c3H5			NUCxRo41eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IF7CNVY1OyClZXzsdy=>	MlPtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
LAN-5	MkHjdWhVWyCjc4PhfS=>			NXi5dpQ6eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IFzBUk02KGOnbHzz	M4fibFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Rh18	M3fJTJFJXFNiYYPzZZk>			NHrJTJpyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiUnixPEBk\Wyucx?=	MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
OHS-50	MVTxTHRUKGG\|c3H5			M1[3OZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCRSGOtOVAh[2WubIO=	MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
RD	MWPxTHRUKGG\|c3H5			MUjxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhWkRiY3XscJM>	Mn;hQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
NB1643	M3\DSpFJXFNiYYPzZZk>			MWfxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDORlE3PDNiY3XscJM>	NFrucG89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
A673	MVzxTHRUKGG\|c3H5			M33jUZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJGE3PzNiY3XscJMq	NFjjbXg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
SK-N-MC	Ml24dWhVWyCjc4PhfS=>			NHTSWFFyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBUUy2QLV3DJINmdGy\|	NVuyS3d[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
BT-12	M4PJfpFJXFNiYYPzZZk>			NYC5SIRueUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhSlRvMUKgZ4VtdHN?	MlTVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
LAN-5	M4G5VJFJXFNiYYPzZZk>			NFvqcnNyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBNSU5vNTDj[Yxtew>?	NET2dJo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
BT-37	MYHxTHRUKGG\|c3H5			NInEUnlyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBDXC1\|NzDj[Yxtew>?	M2j4ZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
TC32	M{PJNpFJXFNiYYPzZZk>			M2HwPJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHREOzJiY3XscJM>	NEPa[489[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
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RD	MmHidWhVWyCjc4PhfS=>			M4XOdJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHJFKGOnbHzz	M{XXelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Rh18	NEGwUmpyUFSVIHHzd4F6			NF\ybotyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBTcDF6IHPlcIx{	NHznZVQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
Rh30	NH[xRlFyUFSVIHHzd4F6			M4SyZ5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHJpOzBiY3XscJM>	M4\YclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SK-N-SH	M1;odpFJXFNiYYPzZZk>			NVrWWHVneUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhW0tvTj3TTEBk\Wyucx?=	M{HGZ\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
NCI-H3122	M3nWSWFvfGmycn;sbYZmemG2aY\lJIF{e2G7		M1HXe\|czKGi{cx?=	MoXuRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCQQ1mtTFMyOjJiY3XscJMh[W[2ZYKgO\|IhcHK\|IHL5JHNTSiCjc4PhfUwhUUN3ME2wMlA2Os7:TT6=	NYq2e\|RZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm2PVg5PTlpPkK5Olk5QDV7PD;hQi=>
PANC1	NHPUOGVHfW6ldHnvckBie3OjeR?=	M3O2TFEhfU1?	M{PJW\|M3KGi{cx?=	MVvJcohq[mm2aX;uJI9nKEiVUEmwZYxxcGFiaX6gbJVu[W5iUFHOR\|Eh[2WubIOgZZN{\XO\|ZXSgZZMhfXBvcnXneYxifGmxbjDv[kBJe3B5MDDheEAyKHWPIHHmeIVzKDN4IHjyd{BjgSCZZYP0[ZJvKGKub4SgZY5idHm\|aYO=	NXfVfXdORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CzOVExODFpPkOwN\|UyODBzPD;hQi=>
PANC1	NUT3WpFyTnWwY4Tpc44h[XO\|YYm=	M3\Cb\|EhfU1?	NWrhdm57OzZiaILz	Mlf0TY5pcWKrdHnvckBw\iCKU2C5NIFteGijIHnuJIh2dWGwIGDBUmMyKGOnbHzzJIF{e2W\|c3XkJIF{KGGtdDDk[Ydz[WSjdHnvckBifCBzIIXNJIFnfGW{IEO2JIhzeyCkeTDX[ZN1\XKwIHLsc5Qh[W6jbInzbZM>	M2TtOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyM{WxNFAyLz5\|MEO1NVAxOTxxYU6=
MCF7	Mo\CRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?		NIHYSZA4OiCqcoO=	NG\vNFZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3DSlch[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1yLkK5{txONg>?	NHTBPHE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9\|MEe4OFg5OSd-M{C3PFQ5QDF:L3G+
NCI-H1299	NX7sflVKSW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		MmXmO\|IhcHK\|	NFjqUWJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF7DTU1JOTJ7OTDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVAvOzgQvF2u	NYH1fmYxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C3PFQ5QDFpPkOwO\|g1QDhzPD;hQi=>
A549	NFzsOIhCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=		NWTXfmVsPzJiaILz	M4HYR2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUW0PUBk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR\|UxRTBwNEVOwG0v	MmjoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB5OES4PFEoRjNyN{i0PFgyRC:jPh?=
Vero E6	NEXJXJdHfW6ldHnvckBie3OjeR?=		MmGxOFghcHK\|	M{iwbmlEPTBiZn;yJIFvfGm4aYLhcEBi[3Srdnn0fUBi\2GrboP0JHNCWlNvQ3;WMVIhcW5idHjlJHZmem9iRU[gZ4VtdCCuaX7lJIF1KDR6IHigZpkhcW2vdX7v[ox2d3Knc3PlcoNmNWKjc3XkJIF{e2G7IDjk[ZRm[3SrbnegeIhmKH[rcnHsJG5RKHC{b4TlbY4hcW5idHjlJI52[2yndYOgc4YhfGinIG\ldo8hTTZiY3XscJMqNCCLQ{WwQVAvOTV2OElOwG0v	M2XHUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzN{M{WzPFU6Lz5\|MkO1N\|g2QTxxYU6=

Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID

Western blot	AXL / c-Myc / p-Mnk1 / Mnk1 / p-eIF4E / eIF4E ; EGFR / p-EGFR / AKT / p-AKT / ERK / p-ERK / S6 / p-S6 ; HSP90 / HSP70	31431614 28679777
Growth inhibition assay	Cell viability	28679777

In vivo

When given on an intermittent basis, AT13387 could be tolerated at doses of up to 70 mg/kg twice weekly or 90 mg/kg once weekly. Body weight loss in mice does not exceed 20% before recovering in all cases except one, and loss is highest following the second dose. Tumor growth inhibition is similar in NCI-H1975 for both dosing regimens. The maintenance of antitumor effects with such a prolonged off-treatment period is consistent with the extended pharmacodynamic action of AT13387 observed for mutant EGFR and other biomarkers in vitro and in vivo and the extended retention of AT13387 in tumors. ^[2]

Protocol (from reference)

Kinase Assay:^[2]	HSP90 competition isothermal calorimetry: K_d values for AT13387 binding to HSP90 are determined with a competition Isothermal Calorimetry (ITC) format. ITC experiments are performed on a Micro Cal VP-ITC at 25 °C in a buffer comprising 25 mM Tris, 100 mM NaCl, 1 mM MgCl₂ and 1 mM Tris(2-carboxy- ethyl)phosphine at pH 7.4 in order to maintain the higher affinit
Cell Research:^[2]	Cell lines: A375, 22RV1 and T474 cells Concentrations: 1 μM Incubation Time: 4 hours Method: The human cell lines including A375, 22RV1, T474, DU1 45, LNCa P, MCF-7, DA-MB-468 are seeded into 96-well plates before the addition of AT13387 in 0.1% (v/v) DMSO. GI50 are determined using a 10-point dose response curve for three cell doubling times. After AT13387 incubation 10% (v/v), Alamar blueis added, and cells are incubated for a further 4 hours. Fluorescence is read. (Only for Reference)
Animal Research:^[2]	Animal Models: Athymic BALB /c mice Dosages: 80 mg/kg Administration: Intraperitoneal adminis tration (Only for Reference)

References

Solubility (25°C)

In vitro	DMSO	25 mg/mL (61.04 mM)
	Water	Insoluble
	Ethanol	Insoluble
In vivo	Add solvents to the product individually and in order (Data is from Selleck tests instead of citations): 2% DMSO+30% PEG 300+ddH2O (prepare before use) For best results, use promptly after mixing. Click to purchase: PEG300	10mg/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	409.52
Formula	C ₂₄H₃₁N₃O₃
CAS No.	912999-49-6
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
Smiles	CC(C)C1=CC(=C(C=C1O)O)C(=O)N2CC3=C(C2)C=C(C=C3)CN4CCN(CC4)C

Download Onalespib (AT13387) SDF

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% 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

Dilution Calculator Molecular Weight Calculator

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

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

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Frequently Asked Questions

Question 1:
How to prepare the compound for in vivo studies?

Answer:
S1163 AT13387 can be dissolved in 2% DMSO/30% PEG 300/ddH2O at 10 mg/ml as a clear solution. But after stayed for about 1 hour, the precipitation will goes out. So it is recommended to be prepared before use.

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