Eprenetapopt (APR-246)

For research use only.

Catalog No.S7724 Synonyms: PRIMA-1MET

3 publications

Eprenetapopt (APR-246) Chemical Structure

CAS No. 5291-32-7

Eprenetapopt (APR-246, PRIMA-1MET) is a small organic molecule that has been shown to restore tumour-suppressor function primarily to mutant p53 and also to induce cell death in various cancer types. APR-246 induces apoptosis and autophagy.

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Selleck's Eprenetapopt (APR-246) has been cited by 3 publications

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Choose Selective p53 Inhibitors

Biological Activity

Description Eprenetapopt (APR-246, PRIMA-1MET) is a small organic molecule that has been shown to restore tumour-suppressor function primarily to mutant p53 and also to induce cell death in various cancer types. APR-246 induces apoptosis and autophagy.
Targets
Mutant p53 [2]
()
In vitro

APR-246 (PRIMA-1MET) is the first clinical-stage compound that reactivates mutant p53 and induces apoptosis. APR-246 is a prodrug that is converted to the active compound methylene quinuclidinone (MQ), a Michael acceptor that binds to cysteine residues in mutant p53 and restores its wild-type conformation. APR-246 completely restores the cisplatin and doxorubicin sensitivity to p53-mutant drug-resistant ovarian cancer cells. It not only reactivates p53 but also decreases intracellular glutathione levels in a dose-dependent manner. APR-246 can trigger apoptosis in a p53-independent manner by inducing ROS and endoplasmic reticulum (ER) stress and by inhibiting thioredoxin reductase 1 (TrxR1). It was also reported that APR-246 induces cell death in myeloma cells independently of p53 status by impairing the GSH/ROS balance[1]. PRIMA-1Met/APR-246 efficiently inhibited the growth of the SCLC cell lines expressing mutant p53 in vitro and induced apoptosis, associated with increased fraction of cells with fragmented DNA, caspase-3 activation, PARP cleavage, Bax and Noxa upregulation and Bcl-2 downregulation in the cells[2].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
NALM-6 NHvrWFZE\WyuII\pZYJqdGm2eTDhd5NigQ>? M3v1dIhq\2hic3Xud4l1cX[rdImgZY5lKGOnbHyg[IVifGhiaX7keYN1cW:wIHnuJIFtdCCWUEWzcZV1KGyndXvlcYlieyxiYoX0JIxwfyCDUGKtNlQ3KHOnboPpeIl3cXS7IHnuJHRRPTO5dDDBUGw> NXP0T|lVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{GwO|MxPzZpPkOxNFc{ODd4PD;hQi=>
UoCB-6 NFLIW5pE\WyuII\pZYJqdGm2eTDhd5NigQ>? NE[xcWRpcWeqIIPlcpNqfGm4aYT5JIFv\CClZXzsJIRm[XSqIHnu[JVkfGmxbjDpckBidGxiVGC1N412fCCuZYXr[Y1q[XNuIHL1eEBtd3diQWDSMVI1PiC|ZX7zbZRqfmm2eTDpckBVWDV|d4SgRWxN NWn6eXpXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{GwO|MxPzZpPkOxNFc{ODd4PD;hQi=>
EU-3 Ml7FR4VtdCC4aXHibYxqfHliYYPzZZk> NEfPPFBpcWeqIIPlcpNqfGm4aYT5JIFv\CClZXzsJIRm[XSqIHnu[JVkfGmxbjDpckBidGxiVGC1N412fCCuZYXr[Y1q[XNuIHL1eEBtd3diQWDSMVI1PiC|ZX7zbZRqfmm2eTDpckBVWDV|d4SgRWxN MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{OTB5M{C3Okc,OzFyN{OwO|Y9N2F-
MUTZ-5 MVzD[YxtKH[rYXLpcIl1gSCjc4PhfS=> MXzobYdpKHOnboPpeIl3cXS7IHHu[EBk\WyuIHTlZZRpKGmwZIXjeIlwdiCrbjDhcIwhXFB3M331eEBt\XWtZX3pZZMtKGK3dDDsc5chSVCULUK0OkB{\W6|aYTpeol1gSCrbjDUVFU{f3RiQVzM M1Tld|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzMEezNFc3Lz5|MUC3N|A4PjxxYU6=
KOPN-8 MV7D[YxtKH[rYXLpcIl1gSCjc4PhfS=> MmTlbIlocCC|ZX7zbZRqfmm2eTDhcoQh[2WubDDk[YF1cCCrbnT1Z5Rqd25iaX6gZYxtKFSSNUPteZQhdGW3a3XtbYF{NCCkdYSgcI94KEGSUj2yOFYhe2Wwc3n0bZZqfHliaX6gWHA2O3e2IFHMUC=> NEjoTIU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MUC3N|A4Pid-M{GwO|MxPzZ:L3G+
RS4;11 NWL0ZlJ7S2WubDD2bYFjcWyrdImgZZN{[Xl? MV7obYdpKHOnboPpeIl3cXS7IHHu[EBk\WyuIHTlZZRpKGmwZIXjeIlwdiCrbjDhcIwhXFB3M331eEBt\XWtZX3pZZMtKGK3dDDsc5chSVCULUK0OkB{\W6|aYTpeol1gSCrbjDUVFU{f3RiQVzM NGjkO5o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MUC3N|A4Pid-M{GwO|MxPzZ:L3G+
SKBR3 MmP2R4VtdCCleXPs[UBie3OjeR?= M3\QW|UhyrWP NY\TSVA{OiC5ZXXrdy=> M3fKOYxieGG2aX7pZkBqdiClb33ibY5ifGmxbjD3bZRpKEGSUj2yOFYh[2G3c3XkJIEhdG:5ZYKgcIV3\Wxib3[gS|Eh[XK{ZYP0JIFv\CCjbjDpcoNz\WG|ZTDpckB1cGVic4XiMWcyKG[{YXP0bY9v NHu3eFc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEe0N|k6Pid-M{C3OFM6QTZ:L3G+
BT549 NXPhUm5nS2WubDD2bYFjcWyrdImgZZN{[Xl? Mn;ZTWM2OD1|LkGg{txO NVK2T3pbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CxPVYzOzZpPkOwNVk3OjN4PD;hQi=>
MDA-MB-468 NY\MNnNMS2WubDD2bYFjcWyrdImgZZN{[Xl? M3q5WGlEPTB;NTFOwG0> NXOzT5NORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CxPVYzOzZpPkOwNVk3OjN4PD;hQi=>
MDA-MB-231 M2i3WGNmdGxidnnhZoltcXS7IHHzd4F6 NX\Cc25KUUN3ME20MlEh|ryP NEPRZ5A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEG5OlI{Pid-M{CxPVYzOzZ:L3G+
HCC1143 NFrkNpRE\WyuII\pZYJqdGm2eTDhd5NigQ>? NWr4S4N6UUN3ME22Mlgh|ryP MkiyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzBzOU[yN|YoRjNyMUm2NlM3RC:jPh?=
MDA-MB-453 MXfD[YxtKH[rYXLpcIl1gSCjc4PhfS=> MWPJR|UxRTBwOTFOwG0> NYXve2NERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CxPVYzOzZpPkOwNVk3OjN4PD;hQi=>
SKBR3 Mn7FR4VtdCC4aXHibYxqfHliYYPzZZk> NVzpblBHUUN3ME21MlEh|ryP MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODF7NkKzOkc,OzBzOU[yN|Y9N2F-
UACC812 MorxR4VtdCC4aXHibYxqfHliYYPzZZk> NHHsbpFKSzVyPUGxMlMh|ryP NWPob5RPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CxPVYzOzZpPkOwNVk3OjN4PD;hQi=>
MCF7 MnPvR4VtdCC4aXHibYxqfHliYYPzZZk> MlLvTWM2OD1|MT6xJO69VQ>? MlO0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzBzOU[yN|YoRjNyMUm2NlM3RC:jPh?=
MCF10A NXzBeWtDS2WubDD2bYFjcWyrdImgZZN{[Xl? MmH3TWM2OD13LkKg{txO M{S5XVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMUm2NlM3Lz5|MEG5OlI{PjxxYU6=
UMSCC10A NVXBV2xvS2WubDD2bYFjcWyrdImgZZN{[Xl? NEja[HExNTVyIN88US=> M1;iTFczKGh? Mmjkd5VxeHKnc4Pl[EBk\WyuIIP1dpZqfmGuIHHu[EBjd3KnIHGgcY9l\XO2IHXm[oVkfCCxbjD0bIUhc2mubHnu[{Bw\iCKTmPDR{Bk\Wyucx?= Mk\vQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl|NEi0OlIoRjJ7M{S4OFYzRC:jPh?=
FaDu MYHD[YxtKH[rYXLpcIl1gSCjc4PhfS=> NWn5dZJkOC13MDFOwG0> NWi2Z2JKPzJiaB?= NUfIU492e3WycILld5Nm\CClZXzsJJN2en[rdnHsJIFv\CCkb4LlJIEhdW:mZYP0JIVn\mWldDDvckB1cGVia3nscIlv\yCxZjDIUnNESyClZXzsdy=> NXTwWmxDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmzOFg1PjJpPkK5N|Q5PDZ{PD;hQi=>
TC32 MoTKdWhVWyCjc4PhfS=> NX\VUmxyeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGTDN|Ih[2WubIO= MoOwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
DAOY M2mxSpFJXFNiYYPzZZk> NV3FOHh4eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFTBU3kh[2WubIO= MojwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
SJ-GBM2 MVPxTHRUKGG|c3H5 MkX6dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFOMLVfCUVIh[2WubIO= NH;iV2E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
A673 MnLRdWhVWyCjc4PhfS=> NVHWVXFJeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFG2O|Mh[2WubIO= M{fGb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SK-N-MC NWXkSmNreUiWUzDhd5NigQ>? NHTCbolyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1utUk1OSyClZXzsdy=> MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
BT-37 M3TjNpFJXFNiYYPzZZk> M2\2dpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCEVD2zO{Bk\Wyucx?= NHLxeW89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
NB-EBc1 MV;xTHRUKGG|c3H5 NVXMSHkyeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF7CMWVD[zFiY3XscJM> MojjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Saos-2 MWfxTHRUKGG|c3H5 NVLTNIJNeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPhc5MuOiClZXzsdy=> Mlj1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
SK-N-SH NHHGNGFyUFSVIHHzd4F6 MYLxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0tvTj3TTEBk\Wyucx?= NWO0emViRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
NB1643 M2naNZFJXFNiYYPzZZk> NV7TbVd4eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF7CNVY1OyClZXzsdy=> NFy2RVQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
LAN-5 MlfKdWhVWyCjc4PhfS=> MnHodWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEyDTj21JINmdGy| MlPxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
BT-12 MmPsdWhVWyCjc4PhfS=> MmCwdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEKWLUGyJINmdGy| M4TvbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
OHS-50 NHjz[|hyUFSVIHHzd4F6 NWjrXXgxeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF;IV{02OCClZXzsdy=> MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
MG 63 (6-TG R) M1;icZFJXFNiYYPzZZk> MlKzdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE2JIE[zJEg3NVSJIGKpJINmdGy| NIXQTY89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
Rh41 NYXDfG1veUiWUzDhd5NigQ>? MnHCdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKqNEGgZ4VtdHN? Mln6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
FL-PARP / Cleaved PARP ; 

PubMed: 26452133     


PARP cleavage was detected by western blotting analysis after treated with PRIMA-1(met) at different concentrations for 24 hours. 

p-p53; 

PubMed: 26452133     


Phosphorylation of p53 level was determined after PRIMA-1(met) treatment.

26452133
Growth inhibition assay
Cell viability; 

PubMed: 26452133     


A panel of CRC cell lines was treated with either DMSO control or PRIMA-1(met) at indicated dosages for 48 hours, followed by CTG assays. The percentage of cell growth inhibition was normalized with respective DMSO control. 

26452133
In vivo APR-246 showed a good safety profile in a Phase I/II clinical dose-finding study on hematological malignancies and prostate cancer and both clinical and p53-dependent biological responses were observed. In animal studies, APR-246 is well tolerated. Single treatment with APR-246 inhibits tumor growth by 21% in mice bearing the aggressively growing A2780-CP20 tumor xenografts[1].

Protocol

Cell Research:

[1]

- Collapse
  • Cell lines: OVCAR-3 cells
  • Concentrations: 40 μM
  • Incubation Time: 20 h
  • Method:

    OVCAR-3 cells were plated at a density of 75 000 cells per well in 3 ml of medium in 12-well plates. Next day, 2.5 ml medium was removed and cells were treated with cisplatin or APR-246 or in combination for 20 h. Next day, cells were harvested by trypsinization, washed twice and cells were stained with Annexin V and propidium iodine (PI). After staining, the samples were analyzed by LSRII flow cytometer. 


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: CD-1 Nu/Nu mice
  • Dosages: 400 mg/kg/day
  • Administration: i.v.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 40 mg/mL (200.75 mM)
Water 40 mg/mL (200.75 mM)
Ethanol '40 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 199.25
Formula

C10H17NO3

CAS No. 5291-32-7
Storage powder
in solvent
Synonyms PRIMA-1MET
Smiles COCC1(C(=O)C2CCN1CC2)CO

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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)

  • Mass
    Concentration
    Volume
    Molecular Weight

*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

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 )

  • C1
    V1
    C2
    V2

* 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

  • 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):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

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

Total Molecular Weight: g/mol

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)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04383938 Recruiting Drug: APR-246 (eprenetapopt) + Pembrolizumab Bladder Cancer|Gastric Cancer|Non Small Cell Lung Cancer|NSCLC|Urothelial Carcinoma|Advanced Solid Tumor Aprea Therapeutics June 25 2020 Phase 1|Phase 2
NCT04214860 Recruiting Drug: APR-246|Drug: Venetoclax|Drug: Azacitidine Myeloid Malignancy Aprea Therapeutics December 13 2019 Phase 1
NCT03745716 Active not recruiting Drug: APR-246 + azacitidine|Drug: Azacitidine MDS Aprea Therapeutics January 11 2019 Phase 3
NCT03391050 Terminated Drug: APR-246|Drug: Dabrafenib Melanoma Aprea Therapeutics|Jules Bordet Institute January 18 2018 Phase 1|Phase 2

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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