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 28 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 NWGwXZRXTnWwY4Tpc44h[XO|YYm= Mn62O|IhcHK| Ml\6TY5pcWKrdHnvckBw\iCqdX3hckBVTUxiKEOzOkBz\XOrZIXld{kh\nW|ZXStWHJMSiBqNEW1JJRwKDh{MjDy[ZNq\HWnczmgLJVvc26xd36gc5Jq\2mwKTDlfJBz\XO|ZXSgbY4hdW:3c3WgRmFHOyClZXzsd{Bie3Onc4Pl[EBieyClZXzsJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IEeyJIhzeyCkeTDj[YxtKHSrdHXyMYdtdyCjc4PhfUwhUUN3MDC9JFAvODB|IN88UU4> MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzByM{e2NUc,OjdyMEO3OlE9N2F-
BAF3 NXzJenhjTnWwY4Tpc44h[XO|YYm= MXm3NkBpenN? MlfUTY5pcWKrdHnvckBw\iCqdX3hckBVTUxiKEOzOkBz\XOrZIXld{kh\nW|ZXStWHJMSSBqNESwJJRwKDd7NjDy[ZNq\HWnczmgLJVvc26xd36gc5Jq\2mwKTDlfJBz\XO|ZXSgbY4hdW:3c3WgRmFHOyClZXzsd{Bie3Onc4Pl[EBieyClZXzsJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IEeyJIhzeyCkeTDj[YxtKHSrdHXyMYdtdyCjc4PhfUwhUUN3MDC9JFAvODB|IN88UU4> NHvReW89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{CwN|c3OSd-MkewNFM4PjF:L3G+
BAF3 MmjzSpVv[3Srb36gZZN{[Xl? NF[w[lM4OiCqcoO= MX;Jcohq[mm2aX;uJI9nKGi3bXHuJHRGVCBqM{O2JJJme2mmdXXzLUBnfXOnZD3UVmtEKCh2NUSgeI8hQDJ3IILld4llfWW|KTCoeY5sdm:5bjDvdolocW5rIHX4dJJme3OnZDDpckBud3W|ZTDCRWY{KGOnbHzzJIF{e2W|c3XkJIF{KGOnbHyg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiN{KgbJJ{KGK7IHPlcIwhfGm2ZYKt[4xwKGG|c3H5MEBKSzVyIE2gNE4xODNizszNMi=> NXjvUYVzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewNFM4PjFpPkK3NFA{PzZzPD;hQi=>
BAF3 M2jxeWZ2dmO2aX;uJIF{e2G7 M3vON|czKGi{cx?= NWD2UFd7UW6qaXLpeIlwdiCxZjDoeY1idiCWRVygLFM{PiC{ZYPp[JVmeyliZoXz[YQuWk:VMTCoNVg6OSC2bzCyN|Q4KHKnc3nkeYV{MSBqdX7rco94diCxcnnnbY4qKGW6cILld5Nm\CCrbjDtc5V{\SCEQV[zJINmdGy|IHHzd4V{e2WmIHHzJINmdGxiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPzJiaILzJIJ6KGOnbHygeIl1\XJvZ3zvJIF{e2G7LDDJR|UxKD1iMD6wNFUh|ryPLh?= NH62RXY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{CwN|c3OSd-MkewNFM4PjF:L3G+
KM12 M3nEUGFvfGmycn;sbYZmemG2aY\lJIF{e2G7 Ml\iO|IhcHK| NH71[JdCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFvNNVIh[2WubIOg[ZhxemW|c3nu[{BVWkuDIIDyc5RmcW5iaX7jeYJifGWmIH\vdkA4OiCqcoOgZpkh[2WubDD0bZRmei2pbH:gZZN{[XluIFnDOVAhRSByLkCxO{DPxE1w MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzByM{e2NUc,OjdyMEO3OlE9N2F-
SU-DHL1 MlXjRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NYXQcI5mPzJiaILz MWXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOXLVTIUFEh[2WubIOg[ZhxemW|c3nu[{BCVEticILveIVqdiCrbnP1ZoF1\WRiZn;yJFczKGi{czDifUBk\WyuIITpeIVzNWeubzDhd5NigSxiSVO1NEA:KDBwMEK0JO69VS5? MmDyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyMEO3OlEoRjJ5MECzO|YyRC:jPh?=
BAF3 NXXJb|dZTnWwY4Tpc44h[XO|YYm= MojTO|IhcHK| MXvJcohq[mm2aX;uJI9nKHerbHSgeJlx\SCHTVy0MWFNUyBqdX7rco94diCxcnnnbY4qKGW6cILld5Nm\CCrbjDtc5V{\SCEQV[zJINmdGy|IHHzd4V{e2WmIHHzJINmdGxiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPzJiaILzJIJ6KGOnbHygeIl1\XJvZ3zvJIF{e2G7LDDJR|UxKD1iMD6wNlgh|ryPLh?= NYjoRYJbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewNFM4PjFpPkK3NFA{PzZzPD;hQi=>
KARPAS299 MlOzRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? M37INVczKGi{cx?= MlT4RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCNQWLQRXMzQTliY3XscJMhcW6ldXLheIVlKG[xcjC3NkBpenNiYomgZ4VtdCC2aYTldk1odG9iYYPzZZktKEmFNUCgQUAxNjB|MTFOwG0v MmrmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyMEO3OlEoRjJ5MECzO|YyRC:jPh?=
SUP-M2 MYTBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? M1exclczKGi{cx?= M1uzc2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU2XQMW0zKGOnbHzzJIV5eHKnc4PpcochSUyNIIDyc5RmcW5iaX7jeYJifGWmIH\vdkA4OiCqcoOgZpkh[2WubDD0bZRmei2pbH:gZZN{[XluIFnDOVAhRSByLkC0NUDPxE1w NUHMcoNERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewNFM4PjFpPkK3NFA{PzZzPD;hQi=>
BAF3 NHH4VldHfW6ldHnvckBie3OjeR?= NWrMWphsPzJiaILz NVj6dnNwUW6qaXLpeIlwdiCxZjDFUWw1NUGOSzDMNVE6Pk1ibYX0ZY51KCi3bnvuc5dvKG:{aXfpckkh\XiycnXzd4VlKGmwIH3veZNmKEKDRkOgZ4VtdHNiYYPz[ZN{\WRiYYOgZ4VtdCCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkA4OiCqcoOgZpkh[2WubDD0bZRmei2pbH:gZZN{[XluIFnDOVAhRSByLkC2O{DPxE1w NX[1PIFDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewNFM4PjFpPkK3NFA{PzZzPD;hQi=>
NCI-H2228 NFrSblhCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MYO3NkBpenN? NXLyW5lNSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2kuUDJ{MkigZ4VtdHNiZYjwdoV{e2mwZzDBUGsheHKxdHXpckBqdmO3YnH0[YQh\m:{IEeyJIhzeyCkeTDj[YxtKHSrdHXyMYdtdyCjc4PhfUwhUUN3MDC9JFAvODZ6IN88UU4> MmjvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyMEO3OlEoRjJ5MECzO|YyRC:jPh?=
MV411 NX\ZN|VZSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= M4rVVFczKGi{cx?= NGjPWVZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3WOFEyKGOnbHzzJIlv[3WkYYTl[EBnd3JiN{KgbJJ{KGK7IHPlcIwhfGm2ZYKt[4xwKGG|c3H5MEBKSzVyIE2gNE4xQDFizszNMi=> M{naW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MECzO|YyLz5{N{CwN|c3OTxxYU6=
SR786 NEPoXG9CdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MoHyO|IhcHK| NYewV5lqSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTVlc5PiClZXzsd{BmgHC{ZYPzbY5oKEGOSzDwdo91\WmwIHnuZ5Vj[XSnZDDmc5IhPzJiaILzJIJ6KGOnbHygeIl1\XJvZ3zvJIF{e2G7LDDJR|UxKD1iMD6wPFEh|ryPLh?= MkLKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyMEO3OlEoRjJ5MECzO|YyRC:jPh?=
BAF3 MWfGeY5kfGmxbjDhd5NigQ>? MWO3NkBpenN? MWPJcohq[mm2aX;uJI9nKEWPTEStRWxMKEdzMkCyVkBufXSjboSgLJVvc26xd36gc5Jq\2mwKTDlfJBz\XO|ZXSgbY4hdW:3c3WgRmFHOyClZXzsd{Bie3Onc4Pl[EBieyClZXzsJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IEeyJIhzeyCkeTDj[YxtKHSrdHXyMYdtdyCjc4PhfUwhUUN3MDC9JFAvQDl5IN88UU4> NH[zeFY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{CwN|c3OSd-MkewNFM4PjF:L3G+
BA/F3 M{fVWmN6fG:2b4jpZ4l1gSCjc4PhfS=> MX23NkBpenN? MkXrR5l1d3SxeHnjbZR6KGGpYXnud5QhdW:3c3WgTWwuOyCmZYDlcoRmdnRiQlGvSlMh[2WubIOgbY5kfWKjdHXkJIZweiB5MjDodpMh[nliY3XscEB1cXSncj3ncI8h[XO|YYmsJGlEPTBiPTCyMlExPCEQvF2u M4qzXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MECzO|YyLz5{N{CwN|c3OTxxYU6=
KM12 MoHySpVv[3Srb36gZZN{[Xl? MnXwNkBpenN? NGPhcYlKdmirYnn0bY9vKG:oIGTQUVMuXFKNQTDwbI9{eGixconsZZRqd25iaX6gbJVu[W5iS12xNkBk\WyuczDheEBtd3diY3;uZ4VvfHKjdHnvckBi\nSncjCyJIhzeyCkeTDX[ZN1\XKwIHLsc5Qh[W6jbInzbZM> NYTT[XY4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewNFM4PjFpPkK3NFA{PzZzPD;hQi=>
KM12 M{PM[mZ2dmO2aX;uJIF{e2G7 M4D5[|IhcHK| M3Xu[GlvcGmkaYTpc44hd2ZiVGDNN{1VWkuDIIDoc5NxcG:{eXzheIlwdiCrbjDoeY1idiCNTUGyJINmdGy|IHHzd4V{e2WmIHHzJJN2eHC{ZYPzbY9vKG:oIF3BVGsheGixc4Doc5J6dGG2aX;uJIF1KGyxdzDjc45k\W62cnH0bY9vKGGodHXyJFIhcHK|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>? MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzByM{e2NUc,OjdyMEO3OlE9N2F-
KM12 MY\GeY5kfGmxbjDhd5NigQ>? M1jqWFIhcHK| NX7jfnd6UW6qaXLpeIlwdiCxZjDUVG0{NVSUS1GgdIhwe3Cqb4L5cIF1cW:wIHnuJIh2dWGwIFvNNVIh[2WubIOgZZN{\XO|ZXSgZZMhe3WycILld5Nqd25ib3[gVGxE\2GvbXGxJJBpd3OyaH;yfYxifGmxbjDheEBtd3diY3;uZ4VvfHKjdHnvckBi\nSncjCyJIhzeyCkeTDX[ZN1\XKwIHLsc5Qh[W6jbInzbZM> MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzByM{e2NUc,OjdyMEO3OlE9N2F-
KM12 Mm\ESpVv[3Srb36gZZN{[Xl? Mor4NkBpenN? NF\RR3lKdmirYnn0bY9vKG:oIGTQUVMuXFKNQTDwbI9{eGixconsZZRqd25iaX6gbJVu[W5iS12xNkBk\WyuczDhd5Nme3OnZDDhd{B{fXCycnXzd4lwdiCxZjDBT3QheGixc4Doc5J6dGG2aX;uJIF1KGyxdzDjc45k\W62cnH0bY9vKGGodHXyJFIhcHK|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>? NIL5dI89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{CwN|c3OSd-MkewNFM4PjF:L3G+
KM12 MWXGeY5kfGmxbjDhd5NigQ>? MofBNkBpenN? MWDJcohq[mm2aX;uJI9nKFSSTUOtWHJMSSCyaH;zdIhwenmuYYTpc44hcW5iaIXtZY4hU01zMjDj[YxteyCjc4Pld5Nm\CCjczDzeZBxemW|c3nvckBw\iCVNjDwbI9{eGixconsZZRqd25iYYSgcI94KGOxbnPlcpRz[XSrb36gZYZ1\XJiMjDodpMh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz NU\rN3g{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewNFM4PjFpPkK3NFA{PzZzPD;hQi=>
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KARPAS299 M4HLeGZ2dmO2aX;uJIF{e2G7 NWrVPGJ1PjBibXevb4c> NUCzOYtkOThiaILz NFryZZBGgCC4aY\vJIlvcGmkaYTpc44hd2ZiTmDNMWFNUyCyaH;zdIhwenmuYYTpc44hcW5iU1PJSEBud3W|ZTD4[Y5w\3KjZoTl[EB4cXSqIHj1cYFvKEuDUmDBV|I6QSClZXzsd{BifCB4MDDt[{9s\yxicH:gZYRucW6rc4TldoVlKGG|IIPpcodt\SCmb4PlJI1m[XO3cnXkJIFnfGW{IEG4JIhzeyCkeTDX[ZN1\XKwIHLsc5Qh[W6jbInzbZM> NXXGUWdsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewNFM4PjFpPkK3NFA{PzZzPD;hQi=>
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NCI-H2228 MWDGeY5kfGmxbjDhd5NigQ>? NEHtPIM3OCCvZz;r[y=> NXGwfJBQOTJiaILz NH7EeWVGgCC4aY\vJIlvcGmkaYTpc44hd2ZiRV3MOE1CVEticHjvd5Bpd3K7bHH0bY9vKGmwIHH0bJlucWNiboWvcpUhdW:3c3WgfIVvd2e{YX\0[YQhf2m2aDDoeY1idiCQQ1mtTFIzOjhiY3XscJMh[XO|ZYPz[YQh[XNic4XwdJJme3Orb36gc4YhSUuWIIDoc5NxcG:{eXzheIlwdiCjdDC2NEBu\y:tZzygdI8h[WSvaX7pd5RmemWmIHHzJJNqdmeuZTDkc5NmKG2nYYP1doVlKGGodHXyJFEzKGi{czDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN? NIH6[JY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{CwN|c3OSd-MkewNFM4PjF:L3G+
NCI-H2228 Mn\OSpVv[3Srb36gZZN{[Xl? MYW2NEBu\y:tZx?= M3TVSVE5KGi{cx?= NXrFNGx2TXhidnn2c{BqdmirYnn0bY9vKG:oIFXNUFQuSUyNIIDoc5NxcG:{eXzheIlwdiCrbjDheIh6dWmlIH71M452KG2xdYPlJJhmdm:pcnHmeIVlKHerdHigbJVu[W5iTlPJMWgzOjJ6IHPlcIx{KGG|c3Xzd4VlKGG|IIP1dJBz\XO|aX;uJI9nKEGNVDDwbI9{eGixconsZZRqd25iYYSgOlAhdWdxa3esJJBwKGGmbXnubZN1\XKnZDDhd{B{cW6pbHWg[I9{\SCvZXHzeZJm\CCjZoTldkAyQCCqcoOgZpkhX2W|dHXyckBjdG:2IHHuZYx6e2m| MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzByM{e2NUc,OjdyMEO3OlE9N2F-
KARPAS299 M4PMOmFvfGm2dX3vdkBie3OjeR?= MnO4N|AhfG9iNkCgcYcwc2d? M37kclExKGSjeYO= NWP4N4NOSW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gT2FTWEGVMkm5JINmdGy|IIjlco9oemGodHXkJIlvKFOFSVSgcY92e2ViYYPz[ZN{\WRiYYOgeJVud3JiZ4Lve5RpKGmwaHnibZRqd25iYYSgN|AhfG9iNkCgcYcwc2duIIDvJIJq\CCjZH3pcol{fGW{ZXSg[o9zKDFyIHThfZM> M1;FZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MECzO|YyLz5{N{CwN|c3OTxxYU6=
KARPAS299 M{\KZ2FvfGm2dX3vdkBie3OjeR?= MVOzNEB1dyB4MDDt[{9s\w>? Mn:0NVAh\GG7cx?= MX;BcpRqfHWvb4KgZYN1cX[rdImgZYdicW6|dDDoeY1idiCNQWLQRXMzQTliY3XscJMhgGWwb3fyZYZ1\WRiaX6gV2NKTCCvb4Xz[UBie3Onc4Pl[EBieyC2dX3vdkBnemWnIHP1doVlKG2xdYPlJIF1KDNyIITvJFYxKG2pL3vnMEBxdyCkaXSgZYRucW6rc4TldoVlKG[xcjCxNEBl[Xm|IH3lZZN2emWmIH;uJIRigSB7MB?= M4DVXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MECzO|YyLz5{N{CwN|c3OTxxYU6=
KARPAS299 Mo\1SpVv[3Srb36gZZN{[Xl? NFXIS2EzKGi{cx?= MnO3TY5pcWKrdHnvckBw\iCQUF2vRWxMKGG3dH;wbI9{eGixconsZZRqd25iaX6gbJVu[W5iS1HSVGFUOjl7IHPlcIx{KGG2II\ldpkhdG:5IHPvcoNmdnS{YYTpc44h[W[2ZYKgNkBpenNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{ M{nNV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MECzO|YyLz5{N{CwN|c3OTxxYU6=
NCI-H2228 MWHGeY5kfGmxbjDhd5NigQ>? NWr3em1EOiCqcoO= M2fhOWlvcGmkaYTpc44hd2ZiTmDNM2FNUyCjdYTvdIhwe3Cqb4L5cIF1cW:wIHnuJIh2dWGwIF7DTU1JOjJ{ODDj[YxteyCjdDD2[ZJ6KGyxdzDjc45k\W62cnH0bY9vKGGodHXyJFIhcHK|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>? MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzByM{e2NUc,OjdyMEO3OlE9N2F-
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

DMSO 100 mg/mL
(178.36 mM)
Ethanol 75 mg/mL
(133.77 mM)
Water Insoluble

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 2022-01-17)

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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