Entrectinib (RXDX-101)

For research use only.

Catalog No.S7998 Synonyms: NMS-E628

20 publications

Entrectinib (RXDX-101) Chemical Structure

CAS No. 1108743-60-7

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.

Selleck's Entrectinib (RXDX-101) has been cited by 20 publications

Cell, 2020, 183(5):1420-1435.e21

PubMed: 33159857 ( click the link to review the publication )

Hum Cell, 2021, 10.1007/s13577-021-00579-z

PubMed: 34304386 ( click the link to review the publication )

Journal of Cancer, 2021, 12(21): 6356-6362

PubMed: None ( click the link to review the publication )

Clin Cancer Res, 2020, clincanres.2585.2020

PubMed: 33229458 ( click the link to review the publication )

Clin Cancer Res, 2020, 8

PubMed: 32269053 ( click the link to review the publication )

Cancer Discov, 2020, 1 pii: CD-19-1030

PubMed: 32238360 ( click the link to review the publication )

Lung Cancer, 2020, 144:20-29

PubMed: 32353632 ( click the link to review the publication )

Hum Cell, 2020, 10.1007/s13577-020-00420-z

PubMed: 32870449 ( click the link to review the publication )

J Pers Med, 2020, 10(4)E290

PubMed: 33353026 ( click the link to review the publication )

NPJ Precis Oncol, 2020, 4:21

PubMed: 32802958 ( click the link to review the publication )

CU Digital Repository, 2020, N/A

PubMed: N/A ( click the link to review the publication )

Clin Cancer Res, 2019, 10.1158/1078-0432.CCR-19-1104

PubMed: 31585938 ( click the link to review the publication )

Mol Cancer Ther, 2019, 18(6):1137-1148

PubMed: 30926633 ( click the link to review the publication )

J Drug Target, 2019, 27(4):442-450

PubMed: 30301369 ( click the link to review the publication )

Nat Commun, 2018, 9(1):1466

PubMed: 29654229 ( click the link to review the publication )

Clin Cancer Res, 2018, 24(10):2357-2369

PubMed: 29463555 ( click the link to review the publication )

Clin Cancer Res, 2018, 10.1158/1078-0432.CCR-18-1574

PubMed: 30279230 ( click the link to review the publication )

Mol Cancer Ther, 2018, 17(1):222-231

PubMed: 29054983 ( click the link to review the publication )

Cancer Med, 2017, 6(12):2972-2983

PubMed: 29125233 ( click the link to review the publication )

Oncotarget, 2017, 8(43):73871-73883

PubMed: 29088753 ( click the link to review the publication )

Purity & Quality Control

Choose Selective Trk receptor Inhibitors

Biological Activity

Description

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	Activity Description	PMID
BAF3	NYX2[pJITnWwY4Tpc44h[XO\|YYm=		MmDTO\|IhcHK\|	MmHWTY5pcWKrdHnvckBw\iCqdX3hckBVTUxiKEOzOkBz\XOrZIXld{kh\nW\|ZXStWHJMSiBqNEW1JJRwKDh{MjDy[ZNq\HWnczmgLJVvc26xd36gc5Jq\2mwKTDlfJBz\XO\|ZXSgbY4hdW:3c3WgRmFHOyClZXzsd{Bie3Onc4Pl[EBieyClZXzsJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IEeyJIhzeyCkeTDj[YxtKHSrdHXyMYdtdyCjc4PhfUwhUUN3MDC9JFAvODB\|IN88UU4>	NYqwXphrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewNFM4PjFpPkK3NFA{PzZzPD;hQi=>
BAF3	NUHrVW5zTnWwY4Tpc44h[XO\|YYm=		NHjxXoE4OiCqcoO=	MXTJcohq[mm2aX;uJI9nKGi3bXHuJHRGVCBqM{O2JJJme2mmdXXzLUBnfXOnZD3UVmtCKCh2NECgeI8hPzl4IILld4llfWW\|KTCoeY5sdm:5bjDvdolocW5rIHX4dJJme3OnZDDpckBud3W\|ZTDCRWY{KGOnbHzzJIF{e2W\|c3XkJIF{KGOnbHyg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiN{KgbJJ{KGK7IHPlcIwhfGm2ZYKt[4xwKGG\|c3H5MEBKSzVyIE2gNE4xODNizszNMi=>	MnnBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyMEO3OlEoRjJ5MECzO\|YyRC:jPh?=
BAF3	NVjDUJVMTnWwY4Tpc44h[XO\|YYm=		MkPKO\|IhcHK\|	NHzRVpJKdmirYnn0bY9vKG:oIHj1cYFvKFSHTDCoN\|M3KHKnc3nkeYV{MSCodYPl[E1VWkuFIDi0OVQhfG9iOEK1JJJme2mmdXXzLUApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCvb4Xz[UBDSUZ\|IHPlcIx{KGG\|c3Xzd4VlKGG\|IHPlcIwh\3Kxd4ToJIlvcGmkaYTpc44h[W[2ZYKgO\|IhcHK\|IHL5JINmdGxidHn0[ZIu\2yxIHHzd4F6NCCLQ{WwJF0hOC5yMEOg{txONg>?	NFjqRW09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{CwN\|c3OSd-MkewNFM4PjF:L3G+
BAF3	NHjjZmpHfW6ldHnvckBie3OjeR?=		MnjZO\|IhcHK\|	MVXJcohq[mm2aX;uJI9nKGi3bXHuJHRGVCBqM{O2JJJme2mmdXXzLUBnfXOnZD3SU3MyKChzOEmxJJRwKDJ\|NEegdoV{cWS3ZYOpJEh2dmuwb4fuJI9zcWerbjmg[ZhxemW\|c3XkJIlvKG2xdYPlJGJCTjNiY3XscJMh[XO\|ZYPz[YQh[XNiY3XscEBoem:5dHigbY5pcWKrdHnvckBi\nSncjC3NkBpenNiYomgZ4VtdCC2aYTldk1odG9iYYPzZZktKEmFNUCgQUAxNjByNTFOwG0v	MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzByM{e2NUc,OjdyMEO3OlE9N2F-
KM12	MWDBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?		M1ywT\|czKGi{cx?=	MWHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEuPMUKgZ4VtdHNiZYjwdoV{e2mwZzDUVmtCKHC{b4TlbY4hcW6ldXLheIVlKG[xcjC3NkBpenNiYomgZ4VtdCC2aYTldk1odG9iYYPzZZktKEmFNUCgQUAxNjBzNzFOwG0v	NV;VUlBIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewNFM4PjFpPkK3NFA{PzZzPD;hQi=>
SU-DHL1	M2n0ZmFvfGmycn;sbYZmemG2aY\lJIF{e2G7		Mke4O\|IhcHK\|	NWT1R41USW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTWU1FUExzIHPlcIx{KGW6cILld5NqdmdiQVzLJJBzd3SnaX6gbY5kfWKjdHXkJIZweiB5MjDodpMh[nliY3XscEB1cXSncj3ncI8h[XO\|YYmsJGlEPTBiPTCwMlAzPCEQvF2u	MmPBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyMEO3OlEoRjJ5MECzO\|YyRC:jPh?=
BAF3	NXP5ZW5WTnWwY4Tpc44h[XO\|YYm=		MoXIO\|IhcHK\|	NFHhZZBKdmirYnn0bY9vKG:oIIfpcIQhfHmyZTDFUWw1NUGOSzCoeY5sdm:5bjDvdolocW5rIHX4dJJme3OnZDDpckBud3W\|ZTDCRWY{KGOnbHzzJIF{e2W\|c3XkJIF{KGOnbHyg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiN{KgbJJ{KGK7IHPlcIwhfGm2ZYKt[4xwKGG\|c3H5MEBKSzVyIE2gNE4xOjhizszNMi=>	NYXUOXNDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewNFM4PjFpPkK3NFA{PzZzPD;hQi=>
KARPAS299	NEL6TGFCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=		MWC3NkBpenN?	Mn7WRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCNQWLQRXMzQTliY3XscJMhcW6ldXLheIVlKG[xcjC3NkBpenNiYomgZ4VtdCC2aYTldk1odG9iYYPzZZktKEmFNUCgQUAxNjB\|MTFOwG0v	NF7abHc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{CwN\|c3OSd-MkewNFM4PjF:L3G+
SUP-M2	MmrQRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?		NW\sRll2PzJiaILz	MWXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOXUD3NNkBk\WyuczDlfJBz\XO\|aX7nJGFNUyCycn;0[YlvKGmwY4XiZZRm\CCob4KgO\|IhcHK\|IHL5JINmdGxidHn0[ZIu\2yxIHHzd4F6NCCLQ{WwJF0hOC5yNEGg{txONg>?	M4Pa[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MECzO\|YyLz5{N{CwN\|c3OTxxYU6=
BAF3	M1HTXmZ2dmO2aX;uJIF{e2G7		NU\lZXRNPzJiaILz	NFrCfm1KdmirYnn0bY9vKG:oIFXNUFQuSUyNIFyxNVk3VSCvdYThcpQhMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5ibX;1d4UhSkGIMzDj[YxteyCjc4Pld5Nm\CCjczDj[YxtKGe{b4f0bEBqdmirYnn0bY9vKGGodHXyJFczKGi{czDifUBk\WyuIITpeIVzNWeubzDhd5NigSxiSVO1NEA:KDBwME[3JO69VS5?	M1zyN\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MECzO\|YyLz5{N{CwN\|c3OTxxYU6=
NCI-H2228	NIj4O41CdnSrcILvcIln\XKjdHn2[UBie3OjeR?=		MkjkO\|IhcHK\|	NV;rSGdMSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2kuUDJ{MkigZ4VtdHNiZYjwdoV{e2mwZzDBUGsheHKxdHXpckBqdmO3YnH0[YQh\m:{IEeyJIhzeyCkeTDj[YxtKHSrdHXyMYdtdyCjc4PhfUwhUUN3MDC9JFAvODZ6IN88UU4>	M1fCXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MECzO\|YyLz5{N{CwN\|c3OTxxYU6=
MV411	MU\BcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?		NEHu[4s4OiCqcoO=	M2rVRmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTW[0NVEh[2WubIOgbY5kfWKjdHXkJIZweiB5MjDodpMh[nliY3XscEB1cXSncj3ncI8h[XO\|YYmsJGlEPTBiPTCwMlA5OSEQvF2u	NV\JdXZPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewNFM4PjFpPkK3NFA{PzZzPD;hQi=>
SR786	NGnE[XpCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=		NHX6Xo44OiCqcoO=	Mnf2RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCVUke4OkBk\WyuczDlfJBz\XO\|aX7nJGFNUyCycn;0[YlvKGmwY4XiZZRm\CCob4KgO\|IhcHK\|IHL5JINmdGxidHn0[ZIu\2yxIHHzd4F6NCCLQ{WwJF0hOC5yOEGg{txONg>?	NFT3e2g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{CwN\|c3OSd-MkewNFM4PjF:L3G+
BAF3	NF23cVRHfW6ldHnvckBie3OjeR?=		MlLDO\|IhcHK\|	MWHJcohq[mm2aX;uJI9nKEWPTEStRWxMKEdzMkCyVkBufXSjboSgLJVvc26xd36gc5Jq\2mwKTDlfJBz\XO\|ZXSgbY4hdW:3c3WgRmFHOyClZXzsd{Bie3Onc4Pl[EBieyClZXzsJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IEeyJIhzeyCkeTDj[YxtKHSrdHXyMYdtdyCjc4PhfUwhUUN3MDC9JFAvQDl5IN88UU4>	NFyybHQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{CwN\|c3OSd-MkewNFM4PjF:L3G+
BA/F3	MXvDfZRwfG:6aXPpeJkh[XO\|YYm=		NEm3PJU4OiCqcoO=	NV;SS5NkS3m2b4TvfIlkcXS7IHHnZYlve3RibX;1d4UhUUxvMzDk[ZBmdmSnboSgRmEwTjNiY3XscJMhcW6ldXLheIVlKG[xcjC3NkBpenNiYomgZ4VtdCC2aYTldk1odG9iYYPzZZktKEmFNUCgQUAzNjFyNDFOwG0v	MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzByM{e2NUc,OjdyMEO3OlE9N2F-
KM12	NIrqVldHfW6ldHnvckBie3OjeR?=		MXGyJIhzew>?	MkTQTY5pcWKrdHnvckBw\iCWUF2zMXRTU0FicHjvd5Bpd3K7bHH0bY9vKGmwIHj1cYFvKEuPMUKgZ4VtdHNiYYSgcI94KGOxbnPlcpRz[XSrb36gZYZ1\XJiMjDodpMh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz	MnroQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyMEO3OlEoRjJ5MECzO\|YyRC:jPh?=
KM12	MkTzSpVv[3Srb36gZZN{[Xl?		M3mySlIhcHK\|	M{O0NGlvcGmkaYTpc44hd2ZiVGDNN{1VWkuDIIDoc5NxcG:{eXzheIlwdiCrbjDoeY1idiCNTUGyJINmdGy\|IHHzd4V{e2WmIHHzJJN2eHC{ZYPzbY9vKG:oIF3BVGsheGixc4Doc5J6dGG2aX;uJIF1KGyxdzDjc45k\W62cnH0bY9vKGGodHXyJFIhcHK\|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>?	NW\hU3pQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewNFM4PjFpPkK3NFA{PzZzPD;hQi=>
KM12	Mm\ySpVv[3Srb36gZZN{[Xl?		NYrCcHYzOiCqcoO=	MVjJcohq[mm2aX;uJI9nKFSSTUOtWHJMSSCyaH;zdIhwenmuYYTpc44hcW5iaIXtZY4hU01zMjDj[YxteyCjc4Pld5Nm\CCjczDzeZBxemW\|c3nvckBw\iCSTFPnZY1u[TFicHjvd5Bpd3K7bHH0bY9vKGG2IHzve{Bkd26lZX70doF1cW:wIHHmeIVzKDJiaILzJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrcx?=	NVzVeW1yRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewNFM4PjFpPkK3NFA{PzZzPD;hQi=>
KM12	M{jwVmZ2dmO2aX;uJIF{e2G7		MnTWNkBpenN?	NEPD[GJKdmirYnn0bY9vKG:oIGTQUVMuXFKNQTDwbI9{eGixconsZZRqd25iaX6gbJVu[W5iS12xNkBk\WyuczDhd5Nme3OnZDDhd{B{fXCycnXzd4lwdiCxZjDBT3QheGixc4Doc5J6dGG2aX;uJIF1KGyxdzDjc45k\W62cnH0bY9vKGGodHXyJFIhcHK\|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>?	MlXjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyMEO3OlEoRjJ5MECzO\|YyRC:jPh?=
KM12	M3i1UGZ2dmO2aX;uJIF{e2G7		NFHweVczKGi{cx?=	NXT4eoZTUW6qaXLpeIlwdiCxZjDUVG0{NVSUS1GgdIhwe3Cqb4L5cIF1cW:wIHnuJIh2dWGwIFvNNVIh[2WubIOgZZN{\XO\|ZXSgZZMhe3WycILld5Nqd25ib3[gV\|YheGixc4Doc5J6dGG2aX;uJIF1KGyxdzDjc45k\W62cnH0bY9vKGGodHXyJFIhcHK\|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>?	M1LHTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MECzO\|YyLz5{N{CwN\|c3OTxxYU6=
KARPAS299	M1fUbGZ2dmO2aX;uJIF{e2G7	NX;RS41ZPjBibXevb4c>	NHXNe5MyOiCqcoO=	NUK2dVlJTXhidnn2c{BqdmirYnn0bY9vKG:oIF7QUU1CVEticHjvd5Bpd3K7bHH0bY9vKGmwIGPDTWQhdW:3c3WgfIVvd2e{YX\0[YQhf2m2aDDoeY1idiCNQWLQRXMzQTliY3XscJMh[XRiNkCgcYcwc2duIIDvJIFldWmwaYP0[ZJm\CCjczDzbY5odGViZH;z[UBu\WG\|dYLl[EBi\nSncjCxNkBpenNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{	NYfhSnU4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewNFM4PjFpPkK3NFA{PzZzPD;hQi=>
KARPAS299	MkXFSpVv[3Srb36gZZN{[Xl?	MXq2NEBu\y:tZx?=	MUixPEBpenN?	NF;0Xm9GgCC4aY\vJIlvcGmkaYTpc44hd2ZiTmDNMWFNUyCyaH;zdIhwenmuYYTpc44hcW5iU1PJSEBud3W\|ZTD4[Y5w\3KjZoTl[EB4cXSqIHj1cYFvKEuDUmDBV\|I6QSClZXzsd{BifCB4MDDt[{9s\yxicH:gZYRucW6rc4TldoVlKGG\|IIPpcodt\SCmb4PlJI1m[XO3cnXkJIFnfGW{IEG4JIhzeyCkeTDX[ZN1\XKwIHLsc5Qh[W6jbInzbZM>	NESwfpQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{CwN\|c3OSd-MkewNFM4PjF:L3G+
KARPAS299	NXXaOJp2TnWwY4Tpc44h[XO\|YYm=	NX\BPZYzPjBibXevb4c>	NYnGVmFEOTJiaILz	M2TnO2V5KH[rdn:gbY5pcWKrdHnvckBw\iCQUF2tRWxMKHCqb4PwbI9zgWyjdHnvckBqdiCVQ1nEJI1wfXOnIIjlco9oemGodHXkJJdqfGhiaIXtZY4hU0GUUFHTNlk6KGOnbHzzJIF{e2W\|c3XkJIF{KHO3cIDy[ZN{cW:wIH;mJHNVSVR\|IIDoc5NxcG:{eXzheIlwdiCjdDC2NEBu\y:tZzygdI8h[WSvaX7pd5RmemWmIHHzJJNqdmeuZTDkc5NmKG2nYYP1doVlKGGodHXyJFEzKGi{czDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN?	M1X2cFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MECzO\|YyLz5{N{CwN\|c3OTxxYU6=
KARPAS299	NEfFOIpHfW6ldHnvckBie3OjeR?=	NYf0c4d[PjBibXevb4c>	M3T2eFE5KGi{cx?=	NGD1WmNKdiC4aY\vJIlvcGmkaYTpc44hd2ZiTmDNMWFNUyCyaH;zdIhwenmuYYTpc44hcW5iU1PJSEBud3W\|ZTD4[Y5w\3KjZoTl[EB4cXSqIHj1cYFvKEuDUmDBV\|I6QSClZXzsd{Bie3Onc4Pl[EBieyC\|dYDwdoV{e2mxbjDv[kBUXEGWMzDwbI9{eGixconsZZRqd25iYYSgOlAhdWdxa3esJJBwKGGmbXnubZN1\XKnZDDhd{B{cW6pbHWg[I9{\SCvZXHzeZJm\CCjZoTldkAyQCCqcoOgZpkhX2W\|dHXyckBjdG:2IHHuZYx6e2m\|	Ml\YQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyMEO3OlEoRjJ5MECzO\|YyRC:jPh?=
NCI-H2228	MlzmRY51cXS3bX;yJIF{e2G7	NIW1OGs{OCC2bzC2NEBu\y:tZx?=	NWLsPZV3OTBiZHH5dy=>	NVjqOlZFSW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gUmNKNUh{MkK4JINmdGy\|IIjlco9oemGodHXkJIlvKGG2aIntbYMhdnVxboWgcY92e2ViYYPz[ZN{\WRiYYOgeJVud3JiZ4Lve5RpKGmwaHnibZRqd25iYYSgN\|AhfG9iNkCgcYcwc2duIIDvJIJq\CCjZH3pcol{fGW{ZXSg[o9zKDFyIHThfZM>	MoPiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyMEO3OlEoRjJ5MECzO\|YyRC:jPh?=
NCI-H2228	NIrZVldHfW6ldHnvckBie3OjeR?=	MnXaOlAhdWdxa3e=	Mn\MNVIhcHK\|	Mk\5SZghfmm4bzDpcohq[mm2aX;uJI9nKEWPTEStRWxMKHCqb4PwbI9zgWyjdHnvckBqdiCjdHj5cYlkKG63L371JI1wfXOnIIjlco9oemGodHXkJJdqfGhiaIXtZY4hVkOLLViyNlI5KGOnbHzzJIF1KDZyIH3nM4toNCCybzDh[I1qdmm\|dHXy[YQh[XNic3nu[4xmKGSxc3WgcYVie3W{ZXSgZYZ1\XJiMUKgbJJ{KGK7IGfld5Rmem5iYnzveEBidmGueYPpdy=>	MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzByM{e2NUc,OjdyMEO3OlE9N2F-
NCI-H2228	M3LmW2Z2dmO2aX;uJIF{e2G7	M4HjV\|YxKG2pL3vn	MYCxPEBpenN?	M{HQXGV5KH[rdn:gbY5pcWKrdHnvckBw\iCHTVy0MWFNUyCyaH;zdIhwenmuYYTpc44hcW5iYYTofY1q[yCwdT;ueUBud3W\|ZTD4[Y5w\3KjZoTl[EB4cXSqIHj1cYFvKE6FST3INlIzQCClZXzsd{BifCB4MDDt[{9s\yxicH:gZYRucW6rc4TldoVlKGG\|IIPpcodt\SCmb4PlJI1m[XO3cnXkJIFnfGW{IEG4JIhzeyCkeTDX[ZN1\XKwIHLsc5Qh[W6jbInzbZM>	MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzByM{e2NUc,OjdyMEO3OlE9N2F-
NCI-H2228	NHTzVpNHfW6ldHnvckBie3OjeR?=	NVvOcWJYPjBibXevb4c>	NH7iO\|MyOiCqcoO=	NGLT[mJGgCC4aY\vJIlvcGmkaYTpc44hd2ZiRV3MOE1CVEticHjvd5Bpd3K7bHH0bY9vKGmwIHH0bJlucWNiboWvcpUhdW:3c3WgfIVvd2e{YX\0[YQhf2m2aDDoeY1idiCQQ1mtTFIzOjhiY3XscJMh[XO\|ZYPz[YQh[XNic4XwdJJme3Orb36gc4YhSUuWIIDoc5NxcG:{eXzheIlwdiCjdDC2NEBu\y:tZzygdI8h[WSvaX7pd5RmemWmIHHzJJNqdmeuZTDkc5NmKG2nYYP1doVlKGGodHXyJFEzKGi{czDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN?	MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzByM{e2NUc,OjdyMEO3OlE9N2F-
NCI-H2228	MojSSpVv[3Srb36gZZN{[Xl?	MYG2NEBu\y:tZx?=	NGniUmkyQCCqcoO=	NIfVV2xGgCC4aY\vJIlvcGmkaYTpc44hd2ZiRV3MOE1CVEticHjvd5Bpd3K7bHH0bY9vKGmwIHH0bJlucWNiboWvcpUhdW:3c3WgfIVvd2e{YX\0[YQhf2m2aDDoeY1idiCQQ1mtTFIzOjhiY3XscJMh[XO\|ZYPz[YQh[XNic4XwdJJme3Orb36gc4YhSUuWIIDoc5NxcG:{eXzheIlwdiCjdDC2NEBu\y:tZzygdI8h[WSvaX7pd5RmemWmIHHzJJNqdmeuZTDkc5NmKG2nYYP1doVlKGGodHXyJFE5KGi{czDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN?	MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzByM{e2NUc,OjdyMEO3OlE9N2F-
KARPAS299	NI\zPHVCdnSrdIXtc5Ih[XO\|YYm=	MnjGN\|AhfG9iNkCgcYcwc2d?	NUDXXlhtOTBiZHH5dy=>	NGTwXW5CdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBpfW2jbjDLRXJRSVN{OUmgZ4VtdHNieHXuc4dz[W[2ZXSgbY4hW0OLRDDtc5V{\SCjc4Pld5Nm\CCjczD0eY1weiCpcn;3eIghcW6qaXLpeIlwdiCjdDCzNEB1dyB4MDDt[{9s\yxicH:gZollKGGmbXnubZN1\XKnZDDmc5IhOTBiZHH5dy=>	NVPpSmhORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewNFM4PjFpPkK3NFA{PzZzPD;hQi=>
KARPAS299	NYmw[FFISW62aYT1cY9zKGG\|c3H5	NGrQNIw{OCC2bzC2NEBu\y:tZx?=	M{KxUFExKGSjeYO=	MoHYRY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iS1HSVGFUOjl7IHPlcIx{KHinbn;ndoFnfGWmIHnuJHNEUURibX;1d4Uh[XO\|ZYPz[YQh[XNidIXtc5Ih\nKnZTDjeZJm\CCvb4Xz[UBifCB\|MDD0c{A3OCCvZz;r[{wheG9iYnnkJIFldWmwaYP0[ZJm\CCob4KgNVAh\GG7czDt[YF{fXKnZDDvckBl[XliOUC=	NVXRNlZKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewNFM4PjFpPkK3NFA{PzZzPD;hQi=>
KARPAS299	MVTGeY5kfGmxbjDhd5NigQ>?		NHrOVnYzKGi{cx?=	NHjY[m1KdmirYnn0bY9vKG:oIF7QUU9CVEtiYYX0c5Bpd3OyaH;yfYxifGmxbjDpckBpfW2jbjDLRXJRSVN{OUmgZ4VtdHNiYYSgeoVzgSCub4egZ49v[2WwdILheIlwdiCjZoTldkAzKGi{czDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN?	NWTGRWNHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewNFM4PjFpPkK3NFA{PzZzPD;hQi=>
NCI-H2228	MY\GeY5kfGmxbjDhd5NigQ>?		M3racVIhcHK\|	NYT5RpZ1UW6qaXLpeIlwdiCxZjDOVG0wSUyNIHH1eI9xcG:\|cHjvdplt[XSrb36gbY4hcHWvYX6gUmNKNUh{MkK4JINmdGy\|IHH0JJZmenlibH;3JINwdmOnboTyZZRqd25iYX\0[ZIhOiCqcoOgZpkhX2W\|dHXyckBjdG:2IHHuZYx6e2m\|	MnLLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyMEO3OlEoRjJ5MECzO\|YyRC:jPh?=

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	Cyclin A1 / Cyclin E1 / p27 / p21; PubMed: 26735175 Oncotarget Expression of cell cycle regulatory proteins (p21, p27, Cyclin A1, and Cyclin E1) was validated by Western Blot 24h after treatment with entrectinib. Gapdh was used as a control of proper protein loading. Numbers indicate concentration of entrectinib (e; 䲧疝Ỵ疞㧀疜膉痘  p-ALK / ALK / p-ERK / ERK / p-STAT3 / STAT3; PubMed: 26735175 Oncotarget Using entrectinib (e) IC50 defined for 48h, Eventual change of ALK downstream pathway after treatment with entrectinib was validated by Western blot. pTrkA-Y490 / TrkA / p-PLCγ-Y783 / PLCγ ; PubMed: 28903424 Oncotarget Western blot analysis of the changes in phosphorylation levels of TRKA and its downstream transducer PLCγ 2 hours post entrectinib and crizotinib treatment in Ba/F3-SCYL3-NTRK1 cells. pAKT / AKT; PubMed: 26172300 Oncotarget Western blot demonstrating Inhibition of the phosphorylation of the ALK protein and other downstream signal molecules in the EML4-ALK CRC patient tumor derived cell line after inhibition by crizotinib or entrectinib.	26735175 28903424 26172300
Growth inhibition assay	Cell viability ; PubMed: 26172300 Oncotarget Inhibition of the growth of the EML4-ALK CRC patient derived tumor cells with 1 μM crizotinib or 1 μM entrectinib.	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

References

Solubility (25°C)

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

* 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 Entrectinib (RXDX-101) SDF

Molecular Weight	560.64
Formula	C₃₁H₃₄F₂N₆O₂
CAS No.	1108743-60-7
Storage	3 years-20°C powder 2 years-80°C in solvent
Synonyms	NMS-E628
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)

Dosage

mg/kg

Average weight of animals

Dosing volume per animal

Number of animals

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

Calculate Reset

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):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
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)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2021-09-06)

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	Recruiting	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

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

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Entrectinib (RXDX-101)