Onalespib (AT13387)

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

For research use only.

Catalog No.S1163

19 publications

CAS No. 912999-49-6

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.

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

Cell, 2017, 168(5):856-866

PubMed: 28215707 ( click the link to review the publication )

Nat Med, 2017, 23(1):69-78

PubMed: 27941792 ( click the link to review the publication )

Cell Chem Biol, 2021, S2451-9456(21)00221-X

PubMed: 34077750 ( click the link to review the publication )

Transl Res, 2021, 235:1-14

PubMed: 33887528 ( click the link to review the publication )

Front Oncol, 2021, 11:642603

PubMed: 34178628 ( click the link to review the publication )

Connect Tissue Res, 2021, 1-11

PubMed: 34100663 ( click the link to review the publication )

Eur J Nucl Med Mol Imaging, 2020, 47(4):980-990

PubMed: 31912256 ( click the link to review the publication )

Sci Rep, 2020, 3;10(1):5923

PubMed: 32246062 ( click the link to review the publication )

Cell Biochem Funct, 2020, 10.1002/cbf.3566

PubMed: 32567086 ( click the link to review the publication )

Nat Commun, 2019, 10(1):5661

PubMed: 31827092 ( click the link to review the publication )

Int J Oncol, 2019, 55(6):1287-1295

PubMed: 31638190 ( click the link to review the publication )

Biomed Res, 2019, 40(4):169-178

PubMed: 31413238 ( click the link to review the publication )

ACS Chem Neurosci, 2019, 10(6):2890-2902

PubMed: 31017387 ( click the link to review the publication )

Prostaglandins Other Lipid Mediat, 2019, 143:106327

PubMed: 30946899 ( click the link to review the publication )

Mol Med Rep, 2018, 17(6):8542-8547

PubMed: 29658585 ( click the link to review the publication )

Nat Commun, 2017, 8(1):422

PubMed: 28871086 ( click the link to review the publication )

PLoS One, 2017, 12(5):e0177878

PubMed: 28542188 ( click the link to review the publication )

Medicinal Chemistry Research, 2016, 10.1007/s00044-016-1553-7

PubMed: ( click the link to review the publication )

PLoS One, 2013, 8(4):e59315

PubMed: 23565147 ( click the link to review the publication )

Purity & Quality Control

Choose Selective HSP (HSP90) Inhibitors

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	Activity Description	PMID
human HCT116 cells	NXXRcotRS3m2b4TvfIlkyqCjc4PhfS=>			NFfyN5JEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJS1RzMU[gZ4VtdHNiYomgRYxidWG{IHLseYUh[XO\|YYmsJGlEPTB;MD6wOFgh\|ryP	M1zuSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyNk[yOVM1Lz5{ME[2NlU{PDxxYU6=
human HCT116 cells	MkPrSpVv[3Srb36gZZN{[Xl?	Mm[xNVAhdk1?	NUH1XHQ{OThiaB?=	NWSy[\|A{UW6mdXP0bY9vKG:oIHHwc5B1d3OrczDpckBpfW2jbjDIR3QyOTZiY3XscJMh[XO\|ZYPz[YQh[XNidYDy[Yd2dGG2aX;uJI9nKEi\|cEewJIxmfmWuIHH0JFExKG6PIHHmeIVzKDF6IHjyd{BjgSCrbX31co9jdG:2dHnu[y=>	NUfJRXRbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC2OlI2OzRpPkKwOlYzPTN2PD;hQi=>
human HCT116 cells	M1HvZ2Z2dmO2aX;uJIF{e2G7	NIjRe\|A{OCCwTR?=	NV:2SHZYOThiaB?=	NHH5VGxKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m\|IHnuJIh2dWGwIFjDWFEyPiClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25ib3[gR2RMPCCuZY\lcEBifCB\|MDDuUUBi\nSncjCxPEBpenNiYomgbY1ufW6xYnzveJRqdmd?	M2D0O\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyNk[yOVM1Lz5{ME[2NlU{PDxxYU6=
human HCT116 cells	M4nwS2Z2dmO2aX;uJIF{e2G7	M1XLdVMxKG6P	M3fCW\|E5KGh?	NIfDfYdKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m\|IHnuJIh2dWGwIFjDWFEyPiClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25ib3[gVoFnNTFibHX2[Ywh[XRiM{Cgcm0h[W[2ZYKgNVghcHK\|IHL5JIludXWwb3Lsc5R1cW6p	NHTBc4o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{ME[2NlU{PCd-MkC2OlI2OzR:L3G+
human HCT116 cells	MVfQdo9tcW[ncnH0bY9vKGG\|c3H5		MV20PEBp	M1XabmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUNVE3KGOnbHzzJIFnfGW{IES4JIhzeyCkeTDNWHQh[XO\|YYmsJGlEPTB;MD6wPEDPxE1?	MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDd4M{K2NUc,OjR5NkOyOlE9N2F-
human SKBR3 cells	MmDQVJJwdGmoZYLheIlwdiCjc4PhfS=>		NVzBbHcyPDhiaB?=	MnzCRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCVS1LSN{Bk\WyuczDh[pRmeiB2ODDodpMh[nliTWTUJIF{e2G7LDDJR\|UxRTBwMUSg{txO	NGjyR5Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEe2N\|I3OSd-MkS3OlMzPjF:L3G+
human MCF7 cells	MUjQdo9tcW[ncnH0bY9vKGG\|c3H5		MYG0PEBp	NXjEO2prSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIFnfGW{IES4JIhzeyCkeTDNWHQh[XO\|YYmsJGlEPTB;MD6yPEDPxE1?	NWPH[mdZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS3OlMzPjFpPkK0O\|Y{OjZzPD;hQi=>
human A231 cells	NVLs[G5YWHKxbHnm[ZJifGmxbjDhd5NigQ>?		NEO0dFI1QCCq	NF;YV2xCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFGyN\|Eh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1zLkCxJO69VQ>?	NXTNbWgyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS3OlMzPjFpPkK0O\|Y{OjZzPD;hQi=>
GIST430	MoHpR5l1d3SxeHnjbZR6KGG\|c3H5		MYi3JIRigXN?	MYnDfZRwfG:6aXPpeJkh[WejaX7zeEBqdWG2aX7pZk1z\XOrc4ThcpQhcHWvYX6gS2lUXDR\|MDDj[YxteyCjc4Pld5Nm\CCjczDk[YNz\WG\|ZTDpckBk\WyuII\pZYJqdGm2eTDh[pRmeiB5IHThfZMh[nliYXzhcYFzKGKudXWgZZN{[XluIFnDOVA:OC5yM{VOwG0v	MlHCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ6NES2PFkoRjJ4OES0Olg6RC:jPh?=
GIST48	NEPxTnlEgXSxdH;4bYNqfHliYYPzZZk>		MUG3JIRigXN?	NUOwN291S3m2b4TvfIlkcXS7IHHnZYlve3RiaX3heIlvcWJvcnXzbZN1[W62IHj1cYFvKEeLU2S0PEBk\WyuczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiClZXzsJJZq[WKrbHn0fUBi\nSncjC3JIRigXNiYomgZYxidWG{IHLseYUh[XO\|YYmsJGlEPTB;MD6wOVXPxE1w	NVKxWXpvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[4OFQ3QDlpPkK2PFQ1Pjh7PD;hQi=>
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NB1643	MW\xTHRUKGG\|c3H5			M3LLV5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCQQkG2OFMh[2WubIO=	MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
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NB1643	NHqxNmZyUFSVIHHzd4F6			MYTxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDORlE3PDNiY3XscJM>	NXXSNWppRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
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SK-N-MC	NUHodIQ4eUiWUzDhd5NigQ>?			MW\xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDTT{1PNU2FIHPlcIx{	NFz0fnQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
BT-12	MlLrdWhVWyCjc4PhfS=>			NWXYc5A5eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhSlRvMUKgZ4VtdHN?	M3LxSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
LAN-5	NHm1WGVyUFSVIHHzd4F6			NXLpXoNKeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhVEGQLUWgZ4VtdHN?	NXzx[nBrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
BT-37	M33EOpFJXFNiYYPzZZk>			MoK2dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgRnQuOzdiY3XscJM>	M{DpVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
TC32	MknrdWhVWyCjc4PhfS=>			MUfxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDUR\|MzKGOnbHzz	MmjLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
U-2 OS	MXLxTHRUKGG\|c3H5			Ml\sdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgWU0zKE:VIHPlcIx{	MoTDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
Rh41	MVrxTHRUKGG\|c3H5			M1fDe5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHJpPDFiY3XscJM>	NGPq[GY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
RD	NXW5WmpseUiWUzDhd5NigQ>?			MWfxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDSSEBk\Wyucx?=	NYW1NmJKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
Rh18	NI\B[pByUFSVIHHzd4F6			M2XL[pFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHJpOThiY3XscJM>	NUnxOHEyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
Rh30	M1jldZFJXFNiYYPzZZk>			NXrafGM2eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhWmh\|MDDj[Yxtew>?	Ml7IQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
SK-N-SH	MWTxTHRUKGG\|c3H5			MlfOdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgV2suVi2VSDDj[Yxtew>?	MoHmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
NCI-H3122	MUDBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?		Ml3mO\|IhcHK\|	NVi3ZZVpSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2kuUDNzMkKgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KFOUQjDhd5NigSxiSVO1NF0xNjB3Mt88UU4>	MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTZ7OEi1PUc,Ojl4OUi4OVk9N2F-
PANC1	NWPpXJg6TnWwY4Tpc44h[XO\|YYm=	MknQNUB2VQ>?	NUXaU2Z4OzZiaILz	NI\0[GJKdmirYnn0bY9vKG:oIFjTVFkx[WyyaHGgbY4hcHWvYX6gVGFPSzFiY3XscJMh[XO\|ZYPz[YQh[XNidYCtdoVofWyjdHnvckBw\iCKc4C3NEBifCBzIIXNJIFnfGW{IEO2JIhzeyCkeTDX[ZN1\XKwIHLsc5Qh[W6jbInzbZM>	MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODN3MUCwNUc,OzB\|NUGwNFE9N2F-
PANC1	MmrUSpVv[3Srb36gZZN{[Xl?	M3;lW\|EhfU1?	Mnj0N\|YhcHK\|	NHfKUnpKdmirYnn0bY9vKG:oIFjTVFkx[WyyaHGgbY4hcHWvYX6gVGFPSzFiY3XscJMh[XO\|ZYPz[YQh[XNiYXv0JIRm\3KjZHH0bY9vKGG2IEGgeW0h[W[2ZYKgN\|YhcHK\|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>?	M{\NT\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyM{WxNFAyLz5\|MEO1NVAxOTxxYU6=
MCF7	NEfOWolCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=		NIrXXVY4OiCqcoO=	NXLuV4xPSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO\|YYmsJGlEPTB;MD6yPe69VS5?	NFLyR4k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9\|MEe4OFg5OSd-M{C3PFQ5QDF:L3G+
NCI-H1299	Mn3DRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?		MoDSO\|IhcHK\|	NEjkXGpCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF7DTU1JOTJ7OTDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVAvOzgQvF2u	MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODd6NEi4NUc,OzB5OES4PFE9N2F-
A549	Mmn6RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?		NVjJTIJWPzJiaILz	NEW1O4lCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFG1OFkh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1yLkS0{txONg>?	NW\KNpl1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C3PFQ5QDFpPkOwO\|g1QDhzPD;hQi=>
Vero E6	MonPSpVv[3Srb36gZZN{[Xl?		M4\DNlQ5KGi{cx?=	MnXYTWM2OCCob4KgZY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgV2FTWy2Fb2[tNkBqdiC2aHWgWoVzdyCHNjDj[YxtKGyrbnWgZZQhPDhiaDDifUBqdW23bn;mcJVwemW\|Y3XuZ4Uu[mG\|ZXSgZZN{[XliKHTleIVkfGmwZzD0bIUhfmm{YXygUnAheHKxdHXpckBqdiC2aHWgcpVkdGW3czDv[kB1cGViVnXyc{BGPiClZXzsd{ktKEmFNUC9NE4yPTR6ON88UU4>	NHP0bGk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9\|MkO1N\|g2QSd-M{KzOVM5PTl:L3G+

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	AXL / c-Myc / p-Mnk1 / Mnk1 / p-eIF4E / eIF4E ; PubMed: 31431614 Oncogenesis Immunoblots of A549 and A549R cells treated with onalespib for the indicated time. EGFR / p-EGFR / AKT / p-AKT / ERK / p-ERK / S6 / p-S6 ; PubMed: 28679777 Clin Cancer Res LN229, U251HF and A172 cells were exposed to 0.1, 0.2 and 0.4 μM onalespib for 48 h before being evaluated for the expression of EGFR, pEGFR, AKT, pAKT, ERK1/2, p-ERK1/2, S6, p-S6 by immunoblotting. GAPDH was assayed as a loading control. HSP90 / HSP70 ; PubMed: 28679777 Clin Cancer Res HSP90 and HSP70 protein expression (upper panel) were evaluated by immunoblotting after treatment with onalespib 0.1, 0.2 and 0.4 μM for 48h on LN229, U251HF and A172 cell lines; GAPDH was used as loading control (lower panel). Immunoblots are representative of three independent experiments and DMSO was used as vehicle control.	31431614 28679777
Growth inhibition assay	Cell viability; PubMed: 28679777 Clin Cancer Res MES (GSC2 and GSC20) and PN (GSC11 and GSC23) GSC lines were exposed to increasing concentrations and times of onalespib before being assayed for viability using the WST-1 assay in all four GSC lines *p<0.05. Data represents the mean ± SEM of triplicate values from two independent experiments.	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

Kinase Assay:^[2]	- Collapse 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]	- Collapse 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]	- Collapse 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.	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 Download Onalespib (AT13387) SDF

Molecular Weight	409.52
Formula	C ₂₄H₃₁N₃O₃
CAS No.	912999-49-6
Storage	3 years-20°C powder 2 years-80°C in solvent
Synonyms	N/A
Smiles	CC(C)C1=CC(=C(C=C1O)O)C(=O)N2CC3=C(C2)C=C(C=C3)CN4CCN(CC4)C

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

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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

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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.

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.

Bio Calculators

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration _(start) x Volume _(start) = Concentration _(final) x Volume _(final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

The Serial Dilution Calculator Equation

Serial Dilutions
Concertration (start):
Dilution-folds:

Computed Result

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
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C8=C7/X	C8:	LOG(C8):

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
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Molarity 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.

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.

HSP (HSP90) Signaling Pathway Map

HSP (HSP90) Inhibitors with Unique Features

Selective HSP90 Inhibitor

NVP-BEP800 : HSP90β-selective, IC50=58 nM.
Most Potent HSP90 Inhibitor

KW-2478 : HSP90, IC50=3.8 nM.
HSP90 Inhibitor in Clinical Trial

17-AAG (Tanespimycin) : Phase III for Gastrointestinal Stromal Tumors.
Newest HSP90 Inhibitor

XL888 : ATP-competitive inhibitor of HSP90 with IC50 of 24 nM.

Related HSP (HSP90) Products

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Zelavespib (PU-H71, NSC 750424) is a potent and selective inhibitor of HSP90 with IC50 of 51 nM. Phase 1.
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VER155008 ^New

VER155008 (C07) is a potent Hsp70 family inhibitor with IC50 of 0.5 μM, 2.6 μM, and 2.6 μM in cell-free assays for HSP70, HSC70, and GRP78 (HSPA5, Bip), respectively, >100-fold selectivity over HSP90. VER155008 inhibits autophagy and causes reduced levels of HSP90 client proteins.
Tanespimycin (17-AAG)

Tanespimycin (17-AAG, CP127374, NSC-330507, KOS 953) is a potent HSP90 inhibitor with IC50 of 5 nM in a cell-free assay, having a 100-fold higher binding affinity for HSP90 derived from tumour cells than HSP90 from normal cells. Tanespimycin (17-AAG) induces apoptosis, necrosis, autophagy and mitophagy. Phase 3.

Features:Displays very low toxicity toward normal cells.
Luminespib (NVP-AUY922)

Luminespib (AUY-922, NVP-AUY922, VER-52296) is a highly potent HSP90 inhibitor for HSP90α/β with IC50 of 13 nM /21 nM in cell-free assays, weaker potency against the HSP90 family members GRP94 and TRAP-1, exhibits the tightest binding of any small-molecule HSP90 ligand. Luminespib (AUY-922, NVP-AUY922) effectively downregulates and destabilizes the IGF-1Rβ protein and results in growth inhibition, autophagy and apoptosis. Phase 2.
Ganetespib (STA-9090)

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HSP990 (NVP-HSP990)

HSP990 (NVP-HSP990) is a novel, potent and selective HSP90 inhibitor for HSP90α/β with IC50 of 0.6 nM/0.8 nM. NVP-HSP990 induces cell cycle arrest and apoptosis.

Features:NVP-HSP990 is an orally available HSP90 inhibitor and is structurally distinct from other clinical HSP90 inhibitors.
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Onalespib (AT13387)