GMX1778 (CHS828)

Catalog No.S8117

For research use only.

GMX1778 (CHS828) is a potent and specific inhibitor of nicotinamide phosphoribosyltransferase (NAMPT) with IC50 and Kd of < 25 nM and 120 nM, respectively. GMX1778 induces programmed cell death with apoptotic features. Phase 1.

GMX1778 (CHS828) Chemical Structure

CAS No. 200484-11-3

Selleck's GMX1778 (CHS828) has been cited by 3 Publications

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Biological Activity

Description GMX1778 (CHS828) is a potent and specific inhibitor of nicotinamide phosphoribosyltransferase (NAMPT) with IC50 and Kd of < 25 nM and 120 nM, respectively. GMX1778 induces programmed cell death with apoptotic features. Phase 1.
Targets
NAMPT [1] NAMPT [1]
<25 nM 120 nM(Kd)
In vitro

GMX1778 induces NAD+ depletion through inhibition of NAD+ biosynthesis, followed by ATP depletion and ultimately resulted in cell death. [1] GMX1778 induces programmed cell death with apoptotic features. [2] GMX1778 suppresses nuclear factor-kappa B activity in cancer cells through downregulation of IKK activity (IC50=8 nM). [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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NYH M{XHemN6fG:2b4jpZ4l1gSCjc4PhfS=> MlnmN{B4\WWtcx?= NVnzTlRqS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVlmKIHPlcIx{KGGodHXyJFMhf2Wna4OgZpkh[2yxbn;n[Y5q[yC|dYL2bZZidCCjc4PhfUwhVER3ME2wMlAxOTgQvF2= NV\GTnNWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2O|k6OTVpPkKzOlc6QTF3PD;hQi=>
A2780 NW\LOHZSSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= MkHpO|IhcHK| Ml30RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCDMke4NEBk\WyuczDhd5Nme3OnZDDhd{Boem:5dHigbY5pcWKrdHnvckBi\nSncjC3NkBpenNiYomgV3JDNWKjc3XkJI1q[3KxcHzheIUhemWjZHXyJIFv[Wy7c3nzMEBKSzVyPUCuNFA2|ryP MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzh3OUGxPEc,OjN6NUmxNVg9N2F-
A2780 NWGzVlc3S3m2b4TvfIlkcXS7IHHzd4F6 M1nWbVczKGi{cx?= MYrDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBNlc5OCClZXzsd{Bie3Onc4Pl[EBieyCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkA4OiCqcoOgZpkhX1OWLUGgZZN{[XluIFnDOVA:OC5yMEC1Ou69VQ>? NF7xdWw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEG2OFA5Pid-MkSxOlQxQDZ:L3G+
MCF-7 Moq4R5l1d3SxeHnjbZR6KGG|c3H5 MnHiO|IhcHK| M32zPGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1ETi15IHPlcIx{KGG|c3Xzd4VlKGG|IHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDd{IHjyd{BjgSCZU2StNUBie3OjeTygTWM2OD1yLkCwNVbPxE1? MojYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRzNkSwPFYoRjJ2MU[0NFg3RC:jPh?=
HepG2 MkPISpVv[3Srb36gZZN{[Xl? M2\tUVEhcHJ? M3O3RWlvcGmkaYTpc44hd2ZiTlHNVHQhcW5iaIXtZY4hUGWyR{KgZ4VtdHNidYPpcochYzF2Q22tcolkd3SrbnHtbYRmN1CUUGCgZZMhe3Wkc4TyZZRmKGG|c3Xzd4VlKGG|IH\vdo1ifGmxbjDv[kBcOTSFXT3ubYNwfGmwYX3p[IUhdW:wb371Z4xmd3SrZHWgZYZ1\XJiMTDodkBjgSCuaYH1bYQhe2OrboTpcIxifGmxbjDjc5VvfGmwZzDhcoFtgXOrczygTWM2OD1yLkCxPFPPxE1? NUHVUplERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSxOlQxQDZpPkK0NVY1ODh4PD;hQi=>
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DLD1 MkSxR5l1d3SxeHnjbZR6KGG|c3H5 MVSyOEBpenN? NVXENFZUS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hTEyGMTDj[YxteyCjZoTldkAzPCCqcoOgZpkhW1KEIHHzd4F6NCCLQ{WwQVIvOzF3zszN MlmyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVzNEexOFgoRjJ3MUS3NVQ5RC:jPh?=
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Rosetta (DE3) M4rBUGZ2dmO2aX;uJIF{e2G7 NFvyRo0yPSCvaX7z MofSTY5pcWKrdHnvckBw\iCqdX3hckBnfWyuIHzlcod1cCCFLYTldo1qdmGuIFjpd|YufGGpZ3XkJG5CVVCWIHX4dJJme3OnZDDpckBGe2OqZYLpZ4hq[SClb3zpJHJwe2W2dHGgLGRGOyliY3XscJMhfXOrbnegcolkd3SrbnHtbYRmKGG|IIP1ZpN1emG2ZTDpcoN2[mG2ZXSg[o9zKDF3IH3pcpMheHKrb4KgeI8he3Wkc4TyZZRmKGGmZHn0bY9vKG2nYYP1doVlKGGodHXyJFMxKG2rboOgbY4heHKnc3XuZ4Uhd2ZiUGLQVEwhUUN3ME2wMlAxOs7:TR?= NX;ye49KRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke1OFEzPzFpPkK3OVQyOjdzPD;hQi=>
PC3 M{niemFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NXO1THJwPSCmYYnz M2\kW2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iUFOzJINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiClZXzsJJZq[WKrbHn0fUBqdmO3YnH0[YQh\m:{IEWg[IF6eyCkeTDD[YxtNXSrdHXyJGdtdyC{ZXHn[Y51KGKjc3XkJIF{e2G7LDDJR|UxRTBwMEC0OO69VQ>? MkTIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh4MUC5PFQoRjJ6NkGwPVg1RC:jPh?=
TC32 NXnsRlBMeUiWUzDhd5NigQ>? MnHSdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFSFM{KgZ4VtdHN? M37NVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
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SJ-GBM2 NFHWXIJyUFSVIHHzd4F6 NVXQPYx1eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPKMWdDVTJiY3XscJM> MojPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
A673 MnHCdWhVWyCjc4PhfS=> NV\BVldVeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFG2O|Mh[2WubIO= NXK1dodQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
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NB1643 MXvxTHRUKGG|c3H5 NV3DUXBxeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF7CNVY1OyClZXzsdy=> Ml3CQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
LAN-5 MXzxTHRUKGG|c3H5 Mn7xdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEyDTj21JINmdGy| MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
BT-12 NVPLVod2eUiWUzDhd5NigQ>? M4C0UpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCEVD2xNkBk\Wyucx?= NIDBZ2M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
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OHS-50 MYfxTHRUKGG|c3H5 MoDGdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE:KUz21NEBk\Wyucx?= Ml3yQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
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MG 63 (6-TG R) M1jrNpFJXFNiYYPzZZk> NUPRN|BneUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF3HJFY{KCh4LWTHJHIqKGOnbHzz M2SybFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
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DAOY NUG5WZlIeUiWUzDhd5NigQ>? MYrxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDERW9[KGOnbHzz MkHEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
NB-EBc1 MXrxTHRUKGG|c3H5 NX3kXoF3eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhVkJvRVLjNUBk\Wyucx?= NEDpcVE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
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BT-37 MkfFdWhVWyCjc4PhfS=> MUPxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDCWE0{PyClZXzsdy=> NUKwSZozRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
TC32 NWLJWIpneUiWUzDhd5NigQ>? NHzBSnRyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBVSzN{IHPlcIx{ MnPGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
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RD MXvxTHRUKGG|c3H5 Mlu1dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgVmQh[2WubIO= NVT5cFJRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
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Rh30 NGq3VGNyUFSVIHHzd4F6 NE\ldGJyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBTcDNyIHPlcIx{ M1[0N|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Saos-2 M4PoNZFJXFNiYYPzZZk> MYPxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDTZY9{NTJiY3XscJM> MnnaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
4T1 NFOwbXFCdnSrdIXtc5Ih[XO|YYm= NEnPO5gyOCCvZz;r[y=> MoK3NVIh\GG7cx?= MXnBcpRqfHWvb4KgZYN1cX[rdImgZYdicW6|dDDtc5V{\SB2VEGgZ4VtdHNiaX3wcIFvfGWmIHnuJGJCVEJxYzDtc5V{\SCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4hfHWvb4XyJJZwdHWvZTDheEAyOCCvZz;r[{whcXBiYnnkJIZweiBzMjDkZZl{KGK7II\ldo5q\XJiY3HsbZBmeiCvZYToc4Q> M3riSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzNECwO|A6Lz5|MUSwNFcxQTxxYU6=
4T1 MkfJRY51cXS3bX;yJIF{e2G7 M3LRcFExKG2pL3vn NV;hcot1OTJiZHH5dy=> NGe1dplCdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBud3W|ZTC0WFEh[2WubIOgbY1xdGGwdHXkJIlvKEKDTFKvZ{Bud3W|ZTDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5idIXtc5Ihf2WrZ3j0JIF1KDFyIH3nM4toNCCrcDDibYQh\m:{IEGyJIRigXN? NYTqUnF5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{G0NFA4ODlpPkOxOFAxPzB7PD;hQi=>
4T1 NVfJS45SSW62aYT1cY9zKGG|c3H5 NWXWPZpOOTBibXevb4c> Mn7tNVIh\GG7cx?= NVT0[2FTSW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhdW:3c3WgOHQyKGOnbHzzJIlueGyjboTl[EBqdiCEYXziM4MhdW:3c3WgcY92e2ViYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iC2dX3vdkBu\XSjc4Thd4l{KGG2IEGwJI1oN2upLDDpdEBjcWRiZn;yJFEzKGSjeYOgcYVie3W{ZXSgdI9{fCCuYYP0JIRwe2ViYomgZ5J6e3SjbDD2bY9t\XRic4ThbY5qdmdiYnHz[YQhfGirb3f1ZY5qdmViY3zvco9o\W6rYzDhd5NigQ>? MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{OTRyMEewPUc,OzF2MEC3NFk9N2F-
In vivo GMX1778 (250 mg/kg, p.o.) shows marked antitumoural activity against three different human neuroendocrine tumours, midgut carcinoid (GOT1), pancreatic carcinoid (BON), and medullary thyroid carcinoma (GOT2), transplanted in nude mice. [4]

Protocol (from reference)

Kinase Assay:[1]
  • In vitro coupled-enzyme NAMPT assay:

    Recombinant NAMPT activity is assessed using a coupled-enzyme assay based on the quantitation of NAD+. Reactions are performed at room temperature for 180 min using mixtures consisting of 50 mM HEPES (pH 7.4), 50 mM KCl, 5 mM MgCl2, 0.5 mM β-mercaptoethanol, 0.005% bovine serum albumin, 1% DMSO, 2.0 U/ml lactate dehydrogenase, 4 mM sodium L-lactate, 0.4 U/ml diaphorase, 6 μΜ resazurin sodium salt, 0.4 mM PRPP, 3.0 nM NMNAT1, 125 μM ATP, 50 μM NM, and 2 to 5 μM recombinant NAMPT. Fluorescence s measured with a Tecan Safire plate reader (excitation wavelength, 560 nm; emission wavelength, 590 nm). Ki values are calculated using Graphpad Prism 4.0 software and the Cheng-Prusoff equation.

Cell Research:[1]
  • Cell lines: HeLa cells
  • Concentrations: ~100 nM
  • Incubation Time: 72 h
  • Method: Serial dilutions of GMX1778 in DMSO are performed to achieve a final concentration of 0.2% DMSO. Relative ATP levels after 72 h are determined using a ViaLight HS high-sensitivity cytotoxicity and cell proliferation BioAssay kit per the manufacturer's instructions. For GMX1778 cytotoxicity rescue experiments, cells are treated with NA (10 μM) or NMN (100 μM) simultaneously with GMX1778. Sigmoidal dose-response curves are generated by nonlinear regression analysis of variable slope using GraphPad Prism version 4.00 (GraphPad Software) to calculate 50% inhibitory (IC50) values.
Animal Research:sup>[4]
  • Animal Models: Nude mice bearing midgut carcinoid (GOT1), pancreatic carcinoid (BON) and medullary thyroid cancer (GOT2) tumors
  • Dosages: ~250 mg/kg
  • Administration: p.o.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 371.86
Formula

C19H22ClN5O

CAS No. 200484-11-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=CC(=CC=C1OCCCCCCN=C(NC#N)NC2=CC=NC=C2)Cl

In vivo Formulation Calculator (Clear solution)

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

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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

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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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Frequently Asked Questions

Question 1:
Could you please suggest me the suitable formulation of S8117 for in vivo study?

Answer:
You can dissolve S8117 in 1%CMC-Na (suspension) for oral administration.

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