Entrectinib (RXDX-101)

Catalog No.S7998 Synonyms: NMS-E628

For research use only.

Entrectinib (RXDX-101, NMS-E628) is an orally bioavailable pan-TrkA/B/C, ROS1 and ALK inhibitor with IC50 ranging between 0.1 and 1.7 nM. Entrectinib (RXDX-101) induces autophagy. Phase 2.

Entrectinib (RXDX-101) Chemical Structure

CAS No. 1108743-60-7

Selleck's Entrectinib (RXDX-101) has been cited by 29 publications

Purity & Quality Control

Choose Selective Trk receptor Inhibitors

Biological Activity

Description Entrectinib (RXDX-101, NMS-E628) is an orally bioavailable pan-TrkA/B/C, ROS1 and ALK inhibitor with IC50 ranging between 0.1 and 1.7 nM. Entrectinib (RXDX-101) induces autophagy. Phase 2.
Targets
TrkA [1] TrkB [1] TrkC [1] ROS1 [1] ALK [1]
In vitro

Entrectinib selectively blocks proliferation of ALK-dependent cell lines and potently inhibits ALK‐dependent signaling. Entrectinib also highly inhibits cell growth of the NSCLC cell line NCI‐H2228 bearing the EML4-ALK rearrangement. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
BAF3 NVe4Z3NuTnWwY4Tpc44h[XO|YYm= M3jRcVczKGi{cx?= MmfxTY5pcWKrdHnvckBw\iCqdX3hckBVTUxiKEOzOkBz\XOrZIXld{kh\nW|ZXStWHJMSiBqNEW1JJRwKDh{MjDy[ZNq\HWnczmgLJVvc26xd36gc5Jq\2mwKTDlfJBz\XO|ZXSgbY4hdW:3c3WgRmFHOyClZXzsd{Bie3Onc4Pl[EBieyClZXzsJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IEeyJIhzeyCkeTDj[YxtKHSrdHXyMYdtdyCjc4PhfUwhUUN3MDC9JFAvODB|IN88UU4> NGC4NVc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{CwN|c3OSd-MkewNFM4PjF:L3G+
BAF3 NYXzPHpoTnWwY4Tpc44h[XO|YYm= MVe3NkBpenN? NULST4VVUW6qaXLpeIlwdiCxZjDoeY1idiCWRVygLFM{PiC{ZYPp[JVmeyliZoXz[YQuXFKNQTCoOFQxKHSxIEe5OkBz\XOrZIXld{khMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5ibX;1d4UhSkGIMzDj[YxteyCjc4Pld5Nm\CCjczDj[YxtKGe{b4f0bEBqdmirYnn0bY9vKGGodHXyJFczKGi{czDifUBk\WyuIITpeIVzNWeubzDhd5NigSxiSVO1NEA:KDBwMECzJO69VS5? M{[1UFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MECzO|YyLz5{N{CwN|c3OTxxYU6=
BAF3 M2PaV2Z2dmO2aX;uJIF{e2G7 MX63NkBpenN? MXPJcohq[mm2aX;uJI9nKGi3bXHuJHRGVCBqM{O2JJJme2mmdXXzLUBnfXOnZD3UVmtEKCh2NUSgeI8hQDJ3IILld4llfWW|KTCoeY5sdm:5bjDvdolocW5rIHX4dJJme3OnZDDpckBud3W|ZTDCRWY{KGOnbHzzJIF{e2W|c3XkJIF{KGOnbHyg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiN{KgbJJ{KGK7IHPlcIwhfGm2ZYKt[4xwKGG|c3H5MEBKSzVyIE2gNE4xODNizszNMi=> M4i0VFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MECzO|YyLz5{N{CwN|c3OTxxYU6=
BAF3 M{j4XmZ2dmO2aX;uJIF{e2G7 M3HrVVczKGi{cx?= M4X3[mlvcGmkaYTpc44hd2ZiaIXtZY4hXEWOIDizN|YhemW|aXT1[ZMqKG[3c3XkMXJQWzFiKEG4PVEhfG9iMkO0O{Bz\XOrZIXld{khMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5ibX;1d4UhSkGIMzDj[YxteyCjc4Pld5Nm\CCjczDj[YxtKGe{b4f0bEBqdmirYnn0bY9vKGGodHXyJFczKGi{czDifUBk\WyuIITpeIVzNWeubzDhd5NigSxiSVO1NEA:KDBwMEC1JO69VS5? M3[zRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MECzO|YyLz5{N{CwN|c3OTxxYU6=
KM12 M4THU2FvfGmycn;sbYZmemG2aY\lJIF{e2G7 MVS3NkBpenN? MlHaRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCNTUGyJINmdGy|IHX4dJJme3OrbnegWHJMSSCycn;0[YlvKGmwY4XiZZRm\CCob4KgO|IhcHK|IHL5JINmdGxidHn0[ZIu\2yxIHHzd4F6NCCLQ{WwJF0hOC5yMUeg{txONg>? NYC0cnM{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewNFM4PjFpPkK3NFA{PzZzPD;hQi=>
SU-DHL1 MX7BcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NWG4XIFtPzJiaILz MmjJRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVVT3ETGwyKGOnbHzzJIV5eHKnc4PpcochSUyNIIDyc5RmcW5iaX7jeYJifGWmIH\vdkA4OiCqcoOgZpkh[2WubDD0bZRmei2pbH:gZZN{[XluIFnDOVAhRSByLkCyOEDPxE1w MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzByM{e2NUc,OjdyMEO3OlE9N2F-
BAF3 NIXaV5dHfW6ldHnvckBie3OjeR?= MVW3NkBpenN? M1vzVGlvcGmkaYTpc44hd2Zid3ns[EB1gXCnIFXNUFQuSUyNIDj1cotvd3ewIH;ybYdqdiliZYjwdoV{e2WmIHnuJI1wfXOnIFLBSlMh[2WubIOgZZN{\XO|ZXSgZZMh[2WubDDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB5MjDodpMh[nliY3XscEB1cXSncj3ncI8h[XO|YYmsJGlEPTBiPTCwMlAzQCEQvF2u NFjmcHg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{CwN|c3OSd-MkewNFM4PjF:L3G+
KARPAS299 NIPOUYhCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MkfiO|IhcHK| M4XkUGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iS1HSVGFUOjl7IHPlcIx{KGmwY4XiZZRm\CCob4KgO|IhcHK|IHL5JINmdGxidHn0[ZIu\2yxIHHzd4F6NCCLQ{WwJF0hOC5yM{Gg{txONg>? M4r2UFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MECzO|YyLz5{N{CwN|c3OTxxYU6=
SUP-M2 M{jsSmFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NUXkb|JtPzJiaILz MYPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOXUD3NNkBk\WyuczDlfJBz\XO|aX7nJGFNUyCycn;0[YlvKGmwY4XiZZRm\CCob4KgO|IhcHK|IHL5JINmdGxidHn0[ZIu\2yxIHHzd4F6NCCLQ{WwJF0hOC5yNEGg{txONg>? Mn7KQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyMEO3OlEoRjJ5MECzO|YyRC:jPh?=
BAF3 M1XXbmZ2dmO2aX;uJIF{e2G7 NHXRU5g4OiCqcoO= NFHk[FBKdmirYnn0bY9vKG:oIFXNUFQuSUyNIFyxNVk3VSCvdYThcpQhMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5ibX;1d4UhSkGIMzDj[YxteyCjc4Pld5Nm\CCjczDj[YxtKGe{b4f0bEBqdmirYnn0bY9vKGGodHXyJFczKGi{czDifUBk\WyuIITpeIVzNWeubzDhd5NigSxiSVO1NEA:KDBwME[3JO69VS5? NYHJfFF4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewNFM4PjFpPkK3NFA{PzZzPD;hQi=>
NCI-H2228 NFHLRo5CdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NGC3S|M4OiCqcoO= M{LlS2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTlPJMWgzOjJ6IHPlcIx{KGW6cILld5NqdmdiQVzLJJBzd3SnaX6gbY5kfWKjdHXkJIZweiB5MjDodpMh[nliY3XscEB1cXSncj3ncI8h[XO|YYmsJGlEPTBiPTCwMlA3QCEQvF2u NIrsbGI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{CwN|c3OSd-MkewNFM4PjF:L3G+
MV411 Mn\LRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MX63NkBpenN? NIjxRYNCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3WOFEyKGOnbHzzJIlv[3WkYYTl[EBnd3JiN{KgbJJ{KGK7IHPlcIwhfGm2ZYKt[4xwKGG|c3H5MEBKSzVyIE2gNE4xQDFizszNMi=> MmXFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyMEO3OlEoRjJ5MECzO|YyRC:jPh?=
SR786 MlnrRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NGLQOmE4OiCqcoO= NXe5O4FQSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTVlc5PiClZXzsd{BmgHC{ZYPzbY5oKEGOSzDwdo91\WmwIHnuZ5Vj[XSnZDDmc5IhPzJiaILzJIJ6KGOnbHygeIl1\XJvZ3zvJIF{e2G7LDDJR|UxKD1iMD6wPFEh|ryPLh?= MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzByM{e2NUc,OjdyMEO3OlE9N2F-
BAF3 NXXsZ481TnWwY4Tpc44h[XO|YYm= MVi3NkBpenN? MVLJcohq[mm2aX;uJI9nKEWPTEStRWxMKEdzMkCyVkBufXSjboSgLJVvc26xd36gc5Jq\2mwKTDlfJBz\XO|ZXSgbY4hdW:3c3WgRmFHOyClZXzsd{Bie3Onc4Pl[EBieyClZXzsJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IEeyJIhzeyCkeTDj[YxtKHSrdHXyMYdtdyCjc4PhfUwhUUN3MDC9JFAvQDl5IN88UU4> MlTsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyMEO3OlEoRjJ5MECzO|YyRC:jPh?=
BA/F3 NHzvNYFEgXSxdH;4bYNqfHliYYPzZZk> M4GyUVczKGi{cx?= MUfDfZRwfG:6aXPpeJkh[WejaX7zeEBud3W|ZTDJUE0{KGSncHXu[IVvfCCEQT;GN{Bk\WyuczDpcoN2[mG2ZXSg[o9zKDd{IHjyd{BjgSClZXzsJJRqfGW{LXfsc{Bie3OjeTygTWM2OCB;IEKuNVA1KM7:TT6= M2jafVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MECzO|YyLz5{N{CwN|c3OTxxYU6=
KM12 Mn[1SpVv[3Srb36gZZN{[Xl? MkXlNkBpenN? MWTJcohq[mm2aX;uJI9nKFSSTUOtWHJMSSCyaH;zdIhwenmuYYTpc44hcW5iaIXtZY4hU01zMjDj[YxteyCjdDDsc5ch[2:wY3XueJJifGmxbjDh[pRmeiB{IHjyd{BjgSCZZYP0[ZJvKGKub4SgZY5idHm|aYO= NHG5eXI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{CwN|c3OSd-MkewNFM4PjF:L3G+
KM12 MWXGeY5kfGmxbjDhd5NigQ>? MWWyJIhzew>? MX\Jcohq[mm2aX;uJI9nKFSSTUOtWHJMSSCyaH;zdIhwenmuYYTpc44hcW5iaIXtZY4hU01zMjDj[YxteyCjc4Pld5Nm\CCjczDzeZBxemW|c3nvckBw\iCPQWDLJJBpd3OyaH;yfYxifGmxbjDheEBtd3diY3;uZ4VvfHKjdHnvckBi\nSncjCyJIhzeyCkeTDX[ZN1\XKwIHLsc5Qh[W6jbInzbZM> MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzByM{e2NUc,OjdyMEO3OlE9N2F-
KM12 NXLTTpB5TnWwY4Tpc44h[XO|YYm= MojyNkBpenN? NGLSS2lKdmirYnn0bY9vKG:oIGTQUVMuXFKNQTDwbI9{eGixconsZZRqd25iaX6gbJVu[W5iS12xNkBk\WyuczDhd5Nme3OnZDDhd{B{fXCycnXzd4lwdiCxZjDQUGNo[W2vYUGgdIhwe3Cqb4L5cIF1cW:wIHH0JIxwfyClb37j[Y51emG2aX;uJIFnfGW{IEKgbJJ{KGK7IGfld5Rmem5iYnzveEBidmGueYPpdy=> NH;GNYg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{CwN|c3OSd-MkewNFM4PjF:L3G+
KM12 NF\WbVNHfW6ldHnvckBie3OjeR?= MVqyJIhzew>? M4D0PWlvcGmkaYTpc44hd2ZiVGDNN{1VWkuDIIDoc5NxcG:{eXzheIlwdiCrbjDoeY1idiCNTUGyJINmdGy|IHHzd4V{e2WmIHHzJJN2eHC{ZYPzbY9vKG:oIFHLWEBxcG:|cHjvdplt[XSrb36gZZQhdG:5IHPvcoNmdnS{YYTpc44h[W[2ZYKgNkBpenNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{ NVPJc5FNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewNFM4PjFpPkK3NFA{PzZzPD;hQi=>
KM12 NHzjfGxHfW6ldHnvckBie3OjeR?= NHXIN3gzKGi{cx?= NU[4ZY1SUW6qaXLpeIlwdiCxZjDUVG0{NVSUS1GgdIhwe3Cqb4L5cIF1cW:wIHnuJIh2dWGwIFvNNVIh[2WubIOgZZN{\XO|ZXSgZZMhe3WycILld5Nqd25ib3[gV|YheGixc4Doc5J6dGG2aX;uJIF1KGyxdzDjc45k\W62cnH0bY9vKGGodHXyJFIhcHK|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>? Mnq3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyMEO3OlEoRjJ5MECzO|YyRC:jPh?=
KARPAS299 MkOwSpVv[3Srb36gZZN{[Xl? NUHjXpJTPjBibXevb4c> NXnRRppoOTJiaILz M2HFeWV5KH[rdn:gbY5pcWKrdHnvckBw\iCQUF2tRWxMKHCqb4PwbI9zgWyjdHnvckBqdiCVQ1nEJI1wfXOnIIjlco9oemGodHXkJJdqfGhiaIXtZY4hU0GUUFHTNlk6KGOnbHzzJIF1KDZyIH3nM4toNCCybzDh[I1qdmm|dHXy[YQh[XNic3nu[4xmKGSxc3WgcYVie3W{ZXSgZYZ1\XJiMUKgbJJ{KGK7IGfld5Rmem5iYnzveEBidmGueYPpdy=> M1T5flxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MECzO|YyLz5{N{CwN|c3OTxxYU6=
KARPAS299 NVvwXWxyTnWwY4Tpc44h[XO|YYm= NE\hR2w3OCCvZz;r[y=> M3[2SlE5KGi{cx?= MVPFfEB3cX[xIHnubIljcXSrb36gc4YhVlCPLVHMT{BxcG:|cHjvdplt[XSrb36gbY4hW0OLRDDtc5V{\SC6ZX7v[5Ji\nSnZDD3bZRpKGi3bXHuJGtCWlCDU{K5PUBk\WyuczDheEA3OCCvZz;r[{wheG9iYXTtbY5qe3SncnXkJIF{KHOrbnfs[UBld3OnIH3lZZN2emWmIHHmeIVzKDF6IHjyd{BjgSCZZYP0[ZJvKGKub4SgZY5idHm|aYO= M1XublxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MECzO|YyLz5{N{CwN|c3OTxxYU6=
KARPAS299 NVewOXpJTnWwY4Tpc44h[XO|YYm= NVjUTlVvPjBibXevb4c> NYrwR5VYOTJiaILz NG\pXZBGgCC4aY\vJIlvcGmkaYTpc44hd2ZiTmDNMWFNUyCyaH;zdIhwenmuYYTpc44hcW5iU1PJSEBud3W|ZTD4[Y5w\3KjZoTl[EB4cXSqIHj1cYFvKEuDUmDBV|I6QSClZXzsd{Bie3Onc4Pl[EBieyC|dYDwdoV{e2mxbjDv[kBUXEGWMzDwbI9{eGixconsZZRqd25iYYSgOlAhdWdxa3esJJBwKGGmbXnubZN1\XKnZDDhd{B{cW6pbHWg[I9{\SCvZXHzeZJm\CCjZoTldkAyOiCqcoOgZpkhX2W|dHXyckBjdG:2IHHuZYx6e2m| MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzByM{e2NUc,OjdyMEO3OlE9N2F-
KARPAS299 MYLGeY5kfGmxbjDhd5NigQ>? NIW0dFM3OCCvZz;r[y=> MWKxPEBpenN? MYXJckB3cX[xIHnubIljcXSrb36gc4YhVlCPLVHMT{BxcG:|cHjvdplt[XSrb36gbY4hW0OLRDDtc5V{\SC6ZX7v[5Ji\nSnZDD3bZRpKGi3bXHuJGtCWlCDU{K5PUBk\WyuczDhd5Nme3OnZDDhd{B{fXCycnXzd4lwdiCxZjDTWGFVOyCyaH;zdIhwenmuYYTpc44h[XRiNkCgcYcwc2duIIDvJIFldWmwaYP0[ZJm\CCjczDzbY5odGViZH;z[UBu\WG|dYLl[EBi\nSncjCxPEBpenNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{ MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzByM{e2NUc,OjdyMEO3OlE9N2F-
NCI-H2228 MkKzRY51cXS3bX;yJIF{e2G7 M3H4WFMxKHSxIE[wJI1oN2up NUPZTY1oOTBiZHH5dy=> NH;tVmlCdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2kuUDJ{MkigZ4VtdHNieHXuc4dz[W[2ZXSgbY4h[XSqeX3pZ{BvfS:wdTDtc5V{\SCjc4Pld5Nm\CCjczD0eY1weiCpcn;3eIghcW6qaXLpeIlwdiCjdDCzNEB1dyB4MDDt[{9s\yxicH:gZollKGGmbXnubZN1\XKnZDDmc5IhOTBiZHH5dy=> NUf4WJlnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewNFM4PjFpPkK3NFA{PzZzPD;hQi=>
NCI-H2228 MWnGeY5kfGmxbjDhd5NigQ>? MnvKOlAhdWdxa3e= M2nJb|EzKGi{cx?= NUXMb4xkTXhidnn2c{BqdmirYnn0bY9vKG:oIFXNUFQuSUyNIIDoc5NxcG:{eXzheIlwdiCrbjDheIh6dWmlIH71M452KG2xdYPlJJhmdm:pcnHmeIVlKHerdHigbJVu[W5iTlPJMWgzOjJ6IHPlcIx{KGG2IE[wJI1oN2upLDDwc{Bi\G2rbnnzeIVz\WRiYYOgd4lv\2ynIHTvd4UhdWWjc4Xy[YQh[W[2ZYKgNVIhcHK|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>? NYCzSnhpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewNFM4PjFpPkK3NFA{PzZzPD;hQi=>
NCI-H2228 MV;GeY5kfGmxbjDhd5NigQ>? MUK2NEBu\y:tZx?= NF25UZoyQCCqcoO= M3;YOWV5KH[rdn:gbY5pcWKrdHnvckBw\iCHTVy0MWFNUyCyaH;zdIhwenmuYYTpc44hcW5iYYTofY1q[yCwdT;ueUBud3W|ZTD4[Y5w\3KjZoTl[EB4cXSqIHj1cYFvKE6FST3INlIzQCClZXzsd{BifCB4MDDt[{9s\yxicH:gZYRucW6rc4TldoVlKGG|IIPpcodt\SCmb4PlJI1m[XO3cnXkJIFnfGW{IEG4JIhzeyCkeTDX[ZN1\XKwIHLsc5Qh[W6jbInzbZM> Moe1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyMEO3OlEoRjJ5MECzO|YyRC:jPh?=
NCI-H2228 NEHnT4VHfW6ldHnvckBie3OjeR?= MoS4OlAhdWdxa3e= M2S3XVEzKGi{cx?= NYDEPIp2TXhidnn2c{BqdmirYnn0bY9vKG:oIFXNUFQuSUyNIIDoc5NxcG:{eXzheIlwdiCrbjDheIh6dWmlIH71M452KG2xdYPlJJhmdm:pcnHmeIVlKHerdHigbJVu[W5iTlPJMWgzOjJ6IHPlcIx{KGG|c3Xzd4VlKGG|IIP1dJBz\XO|aX;uJI9nKEGNVDDwbI9{eGixconsZZRqd25iYYSgOlAhdWdxa3esJJBwKGGmbXnubZN1\XKnZDDhd{B{cW6pbHWg[I9{\SCvZXHzeZJm\CCjZoTldkAyOiCqcoOgZpkhX2W|dHXyckBjdG:2IHHuZYx6e2m| Mo\jQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyMEO3OlEoRjJ5MECzO|YyRC:jPh?=
NCI-H2228 M4rnfmZ2dmO2aX;uJIF{e2G7 Mlz4OlAhdWdxa3e= M2j1[|E5KGi{cx?= M{e1dWV5KH[rdn:gbY5pcWKrdHnvckBw\iCHTVy0MWFNUyCyaH;zdIhwenmuYYTpc44hcW5iYYTofY1q[yCwdT;ueUBud3W|ZTD4[Y5w\3KjZoTl[EB4cXSqIHj1cYFvKE6FST3INlIzQCClZXzsd{Bie3Onc4Pl[EBieyC|dYDwdoV{e2mxbjDv[kBCU1RicHjvd5Bpd3K7bHH0bY9vKGG2IE[wJI1oN2upLDDwc{Bi\G2rbnnzeIVz\WRiYYOgd4lv\2ynIHTvd4UhdWWjc4Xy[YQh[W[2ZYKgNVghcHK|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>? M3mwZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MECzO|YyLz5{N{CwN|c3OTxxYU6=
KARPAS299 NXroe3h{SW62aYT1cY9zKGG|c3H5 NE\mR5U{OCC2bzC2NEBu\y:tZx?= MlfKNVAh\GG7cx?= MmruRY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iS1HSVGFUOjl7IHPlcIx{KHinbn;ndoFnfGWmIHnuJHNEUURibX;1d4Uh[XO|ZYPz[YQh[XNidIXtc5Ih\3Kxd4ToJIlvcGmkaYTpc44h[XRiM{CgeI8hPjBibXevb4ctKHCxIHLp[EBi\G2rbnnzeIVz\WRiZn;yJFExKGSjeYO= MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzByM{e2NUc,OjdyMEO3OlE9N2F-
KARPAS299 MWTBcpRqfHWvb4KgZZN{[Xl? M2P2[lMxKHSxIE[wJI1oN2up MmfXNVAh\GG7cx?= NGK1[FdCdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBpfW2jbjDLRXJRSVN{OUmgZ4VtdHNieHXuc4dz[W[2ZXSgbY4hW0OLRDDtc5V{\SCjc4Pld5Nm\CCjczD0eY1weiCocnXlJIN2emWmIH3veZNmKGG2IEOwJJRwKDZyIH3nM4toNCCybzDibYQh[WSvaX7pd5RmemWmIH\vdkAyOCCmYYnzJI1m[XO3cnXkJI9vKGSjeTC5NC=> NILteFA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{CwN|c3OSd-MkewNFM4PjF:L3G+
KARPAS299 NG\oOXdHfW6ldHnvckBie3OjeR?= MXeyJIhzew>? NY\Cd3dvUW6qaXLpeIlwdiCxZjDOVG0wSUyNIHH1eI9xcG:|cHjvdplt[XSrb36gbY4hcHWvYX6gT2FTWEGVMkm5JINmdGy|IHH0JJZmenlibH;3JINwdmOnboTyZZRqd25iYX\0[ZIhOiCqcoOgZpkhX2W|dHXyckBjdG:2IHHuZYx6e2m| NHfTd5Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{CwN|c3OSd-MkewNFM4PjF:L3G+
NCI-H2228 MX\GeY5kfGmxbjDhd5NigQ>? NWrUbpZTOiCqcoO= NYjqd3lyUW6qaXLpeIlwdiCxZjDOVG0wSUyNIHH1eI9xcG:|cHjvdplt[XSrb36gbY4hcHWvYX6gUmNKNUh{MkK4JINmdGy|IHH0JJZmenlibH;3JINwdmOnboTyZZRqd25iYX\0[ZIhOiCqcoOgZpkhX2W|dHXyckBjdG:2IHHuZYx6e2m| NXK1U45rRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewNFM4PjFpPkK3NFA{PzZzPD;hQi=>
Assay
Methods Test Index PMID
Western blot Cyclin A1 / Cyclin E1 / p27 / p21 ; p-ALK / ALK / p-ERK / ERK / p-STAT3 / STAT3 ; pTrkA-Y490 / TrkA / p-PLCγ-Y783 / PLCγ ; pAKT / AKT 26735175 28903424 26172300
Growth inhibition assay Cell viability 26172300
In vivo In mice bearing Karpas-299 and SR-786 xenografts, Entrectinib (p.o.) induces complete tumor regression. In NPM-ALK transgenic mice, Entrectinib induces complete regression of tumor masses observed in the thymus and in lymph nodes. [2] In the NB xenograft model, Entrectinib cotreatment enhanced the efficacy of conventional chemotherapy. [3]

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 560.64
Formula

C31H34F2N6O2

CAS No. 1108743-60-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN1CCN(CC1)C2=CC(=C(C=C2)C(=O)NC3=NNC4=C3C=C(C=C4)CC5=CC(=CC(=C5)F)F)NC6CCOCC6

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

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

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04551495 Recruiting Drug: Entrectinib|Drug: Letrozole|Drug: Goserelin Invasive Lobular Breast Carcinoma|ER+ Breast Cancer|HER2-negative Breast Cancer Jules Bordet Institute|Hoffmann-La Roche January 14 2021 Phase 2
NCT04226833 Completed Drug: entrectinib Hepatic Insufficiency Hoffmann-La Roche February 11 2020 Phase 1
NCT03796013 Completed Drug: Entrectinib Form A|Drug: Entrectinib Form C Healthy Volunteers Genentech Inc. January 10 2019 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Entrectinib (RXDX-101) | Entrectinib (RXDX-101) supplier | purchase Entrectinib (RXDX-101) | Entrectinib (RXDX-101) cost | Entrectinib (RXDX-101) manufacturer | order Entrectinib (RXDX-101) | Entrectinib (RXDX-101) distributor