Temsirolimus (CCI-779)

Name: Temsirolimus (CCI-779)
Brand: Selleck Chemicals
SKU: S1044
Rating: 5 (67 reviews)

For research use only.

Licensed by Pfizer Catalog No.S1044 Synonyms: NSC 683864

67 publications

Temsirolimus (CCI-779) Chemical Structure

CAS No. 162635-04-3

Temsirolimus (CCI-779, NSC 683864) is a specific mTOR inhibitor with IC50 of 1.76 μM in a cell-free assay. Temsirolimus induces autophagy and apoptosis.

Selleck's Temsirolimus (CCI-779) has been cited by 67 publications

Cancer Cell, 2019, 36(2):179-193

PubMed: 31378681 ( click the link to review the publication )

Cell, 2019, 36(2):179-193

PubMed: 28162770 ( click the link to review the publication )

Nat Chem Biol, 2017, 13(11):1187-1194

PubMed: 28945233 ( click the link to review the publication )

Proc Natl Acad Sci U S A, 2020, 117(49):31189-31197

PubMed: 33229547 ( click the link to review the publication )

Cancers (Basel), 2020, 17;12(1):232

PubMed: 31963500 ( click the link to review the publication )

Cell Oncol (Dordr), 2020, 8

PubMed: 32382996 ( click the link to review the publication )

Cancer Cell Int, 2020, 19;20:58

PubMed: 32099531 ( click the link to review the publication )

Cell Mol Neurobiol, 2020, 10.1007/s10571-020-00977-1

PubMed: 33025417 ( click the link to review the publication )

G3 (Bethesda), 2020, 4;10(5):1585-1597

PubMed: 32265286 ( 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 )

Hum Cell, 2020, 10.1007/s13577-020-00425-8

PubMed: 32886306 ( click the link to review the publication )

Zhongguo Fei Ai Za Zhi, 2020, 20;23(4):216-222

PubMed: 32209188 ( click the link to review the publication )

Int J Nanomedicine, 2020, 15:81-95

PubMed: 32021166 ( click the link to review the publication )

Neoplasia, 2020, 22(10):470-483

PubMed: 32818841 ( click the link to review the publication )

Nat Chem Biol, 2019, 15(3):232-240

PubMed: 30692684 ( click the link to review the publication )

Cell Rep, 2019, 28(8):1971-1980

PubMed: 31433975 ( click the link to review the publication )

Cancer Discov, 2019, 9(5):605-616

PubMed: 30877085 ( click the link to review the publication )

J Dent Res, 2019, 98(3):304-312

PubMed: 30513244 ( click the link to review the publication )

Sci Rep, 2019, 9(1):1897

PubMed: 30760778 ( click the link to review the publication )

Mol Carcinog, 2019, 58(3):358-365

PubMed: 30362635 ( click the link to review the publication )

Biomed Pharmacother, 2019, 112:108692

PubMed: 30798122 ( click the link to review the publication )

Anal Biochem, 2019, 568:65-72

PubMed: 30605633 ( click the link to review the publication )

Exp Ther Med, 2019, 18(3):2278-2284

PubMed: 31410178 ( click the link to review the publication )

Cancers (Basel), 2018, 10(10)E365

PubMed: 30274248 ( click the link to review the publication )
Glia, 2018, 66(5):999-1015

PubMed: 29392777 ( click the link to review the publication )

Cancer Manag Res, 2018, 10:3483-3500

PubMed: 30254491 ( click the link to review the publication )

BMC Cancer, 2018, 18(1):922

PubMed: 30253737 ( click the link to review the publication )

Oncotarget, 2018,

PubMed: 29423101 ( click the link to review the publication )

Oncogene, 2017, 36(6):787-796

PubMed: 27399335 ( click the link to review the publication )

Oncol Lett, 2017,

PubMed: 29113237 ( click the link to review the publication )

Oncotarget, 2017, 8(18):30151-30161

PubMed: 28404914 ( click the link to review the publication )

Oncotarget, 2017, 9(4):5111-5124

PubMed: 29435166 ( click the link to review the publication )

Integr Biol (Camb), 2017,

PubMed: 29159332 ( click the link to review the publication )

Genome Biol, 2016, 17:80

PubMed: 27139883 ( click the link to review the publication )

Clin Cancer Res, 2016, 22(4):1018-27

PubMed: 26490311 ( click the link to review the publication )

Cell Rep, 2016, 17(6):1584-1594

PubMed: 27806297 ( click the link to review the publication )

Sci Rep, 2016,

PubMed: 27849011 ( click the link to review the publication )

BMC Genomics, 2016, 17(1):879

PubMed: 27821074 ( click the link to review the publication )

Anticancer Res, 2016, 36(11):5849-5858

PubMed: 27793908 ( click the link to review the publication )

Gynecol Oncol, 2015, 138(1):165-73

PubMed: 25933683 ( click the link to review the publication )

Int J Oncol, 2015, 47(1):71-80

PubMed: 25955301 ( click the link to review the publication )

Cancer Biol Ther, 2015,

PubMed: 25692408 ( click the link to review the publication )

BMC Cancer, 2015, 15(1):241

PubMed: 25884680 ( click the link to review the publication )

Oncotarget, 2015, 6(29):27227-38

PubMed: 26317900 ( click the link to review the publication )

Leukemia, 2014, 28(4):739-48

PubMed: 23892718 ( click the link to review the publication )

Leukemia, 2014, 28(3):543-53

PubMed: 24253024 ( click the link to review the publication )

Proc Natl Acad Sci U S A, 2014, 111(40):E4214-23

PubMed: 25246577 ( click the link to review the publication )

Cancer Res, 2014, 74(14):3947-58

PubMed: 24986516 ( click the link to review the publication )
Mol Cancer, 2014, 13(1):159

PubMed: 24972933 ( click the link to review the publication )

Mol Oncol, 2014, 10.1016/j.molonc.2014.05.005

PubMed: 24908424 ( click the link to review the publication )

Mol Cancer Res, 2014, 12(5):703-13

PubMed: 24554781 ( click the link to review the publication )

BMC Cancer, 2014, 14:325

PubMed: 24885093 ( click the link to review the publication )

Microbes Infect, 2014, 19(9):2368-80

PubMed: 23633458 ( click the link to review the publication )

PLoS One, 2014, 9(10):e111146

PubMed: 25343454 ( click the link to review the publication )

Head Neck, 2014, 10.1002/hed.23822.

PubMed: 24986420 ( click the link to review the publication )

Clin Cancer Res, 2013, 19(9):2368-80

PubMed: 23633458 ( click the link to review the publication )

Mol Cancer Ther, 2013, 12(11):2581-90

PubMed: 23979920 ( click the link to review the publication )

Cancer Cell Int, 2013, 13(1):30

PubMed: 23537100 ( click the link to review the publication )

Int J Oncol, 2013, 44(3):959-69

PubMed: 24366069 ( click the link to review the publication )

Mol Pain, 2013, 9:50

PubMed: 24099268 ( click the link to review the publication )

PLoS One, 2013, 8(5):e62104

PubMed: 23690929 ( click the link to review the publication )

Mol Biosyst, 2013, 10(3):605-12

PubMed: 24413303 ( click the link to review the publication )

Curr Cancer Drug Targets, 2013, 13(2):175-87

PubMed: 23215724 ( click the link to review the publication )

Hum Pathol, 2012, 43(12):2197-206

PubMed: 22705003 ( click the link to review the publication )

Tuberc Respir Dis, 2012, 72(4):343-51

PubMed: 23227075 ( click the link to review the publication )

Autophagy, 2011, 7(2):176-87

PubMed: 21081844 ( click the link to review the publication )

Mol Genet Metab, 2010, 100(4):309-15

PubMed: 20554235 ( click the link to review the publication )

Purity & Quality Control

Choose Selective mTOR Inhibitors

Biological Activity

Description

Temsirolimus (CCI-779, NSC 683864) is a specific mTOR inhibitor with IC50 of 1.76 μM in a cell-free assay. Temsirolimus induces autophagy and apoptosis.

Targets

mTOR ^[1]
(Cell-free assay)

1.76 μM

In vitro

In the absence of FKBP12, Temsirolimus potently inhibits mTOR kinase activity with IC50 of 1.76 μM, similar to that of rapamycin with IC50 of 1.74 μM. Temsirolimus treatment at nanomolar concentrations (10 nM to <5 μM) displays a modest and selective antiproliferative activity via FKBP12-dependent mechanism, but can completely inhibit the proliferation of a broad panel of tumor cells at low micromolar concentrations (5-15 μM), involving FKBP12-independent suppression of mTOR signaling. Temsirolimus treatment at micromolar but not nanomolar concentrations (20 μM) causes a marked decline in global protein synthesis and disassembly of polyribosomes, accompanied by rapid increase in the phosphorylation of translation elongation factor eEF2 and the translation initiation factor eIF2A. ^[1] Temsirolimus inhibits the phosphorylation of ribosomal protein S6, more potently in PTEN-positive DU145 cells than in PTEN-negative PC-3 cells, and inhibits cell growth and clonogenic survival of both cells in a concentration-dependent manner. ^[2] Temsirolimus (100 ng/mL) potently inhibits proliferation and induces apoptosis in primary human lymphoblastic leukemia (ALL) cells. ^[3]

Cell Data

Cell Lines	Assay Type	Incubation Time	Activity Description	PMID
human MDA468 cells	MYPQdo9tcW[ncnH0bY9vKGG\|c3H5	M4m1eVMh\GG7cx?=	NEW1OHdCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3ERVQ3QCClZXzsd{Bi\nSncjCzJIRigXNiYomgUXRUKGG\|c3H5MEBKSzVyPUigcm0>	NX7XfG5IRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG0N\|g2PzlpPkKxOFM5PTd7PD;hQi=>
human LNCAP cells	M2XITXBzd2yrZnXyZZRqd25iYYPzZZk>	MkXTN{Bl[Xm\|	MUXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEyQQ1HQJINmdGy\|IHHmeIVzKDNiZHH5d{BjgSCPVGOgZZN{[XluIFnDOVA:OC53IH7N	MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTR\|OEW3PUc,OjF2M{i1O\|k9N2F-
A498	MkT1R5l1d3SxeHnjbZR6KGG\|c3H5	MkDtO\|IhcHK\|	NVG0Xnk5S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSTR7ODDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwJF0hOC5\|NTFOwG0v	MnTQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVzMkSxNVQoRjJ3MUK0NVE1RC:jPh?=
A498	MWTDfZRwfG:6aXPpeJkh[XO\|YYm=	NUDvdnFPPiCmYYnz	NXnuNo5uS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSTR7ODDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGOnbHygeoli[mmuaYT5JIFnfGW{IE[g[IF6eyCkeTDNWHQh[XO\|YYmsJGlEPTBiPTCwMlUh\|ryPLh?=	MnP5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN\|NkCxNFQoRjJ\|M{[wNVA1RC:jPh?=
HEK293	M3XycWZ2dmO2aX;uJIF{e2G7		M4HRUGlvcGmkaYTpc44hd2ZiRlvCVFEzNWmwZHXw[Y5l\W62IHj1cYFvKHKnY3;tZolv[W62IH3UU3Ih\XiycnXzd4VlKGmwIFjFT\|I6OyClZXzsd{B2e2mwZzDIbZM3NVN4S{GgZZMh[SC\|dXLzeJJifGViYomgSGVNTkmDIHHzd4F6NCCLQ{WwJF0hOS55NjFOwG0v	NUPWVFBsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG0N\|g2PzlpPkKxOFM5PTd7PD;hQi=>
HSC-4	NUftb2F5T3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=		MU\Jcohq[mm2aX;uJI9nKGi3bXHuJGhUSy12IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTBiPTCwMlAxODFzM{Sg{txONg>?	M3i3N\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzODFzOEKvK\|5USU6JRWK8M4E,
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Ramos-2G6-4C10	Ml7IS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		Mmf3TY5pcWKrdHnvckBw\iCqdX3hckBT[W2xcz2yS\|YuPENzMDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyIE2gNE4xODB\|NEG5JO69VS5?	M17BUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzODFzOEKvK\|5USU6JRWK8M4E,
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HH	NGLxSHJIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		MnvuTY5pcWKrdHnvckBw\iCqdX3hckBJUCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR\|UxKD1iMD6wNFA3PjR2IN88UU4>	M17mXlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzODFzOEKvK\|5USU6JRWK8M4E,
TYK-nu	Mln1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		NUjKbXR{UW6qaXLpeIlwdiCxZjDoeY1idiCWWVutcpUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NEA:KDBwMECwO\|c5OSEQvF2u	M{PVfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzODFzOEKvK\|5USU6JRWK8M4E,
H4	NGn6SmRIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		NV;rWIxUUW6qaXLpeIlwdiCxZjDoeY1idiCKNDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyIE2gNE4xODFyN{Og{txONg>?	M2DVS\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzODFzOEKvK\|5USU6JRWK8M4E,
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SK-NEP-1	MmnVS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		M3fFfGlvcGmkaYTpc44hd2ZiaIXtZY4hW0tvTlXQMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NEA:KDBwMECxOFkh\|ryPLh?=	MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlAyOTh{Lze+V2FPT0WUPD;hQi=>
697	NUnO[2lDT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=		NV;PcpFLUW6qaXLpeIlwdiCxZjDoeY1idiB4OUegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFAvODBzNzFOwG0v	MmDTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVIxOTF6Mj:nQnNCVkeHUkyvZV4>
CTB-1	NHXZclFIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		NWDOcIFwUW6qaXLpeIlwdiCxZjDoeY1idiCFVFKtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwJF0hOC5yMEK5N\|Qh\|ryPLh?=	M2TldlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzODFzOEKvK\|5USU6JRWK8M4E,
DB	MkTvS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		MVfJcohq[mm2aX;uJI9nKGi3bXHuJGRDKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVAhRSByLkCwN\|EzOyEQvF2u	MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlAyOTh{Lze+V2FPT0WUPD;hQi=>
MLMA	NI\wUHdIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		NYTUOFZSUW6qaXLpeIlwdiCxZjDoeY1idiCPTF3BJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUCgQUAxNjByM{OxN{DPxE1w	NGfrbIs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyOjBzMUiyM{c,W0GQR1XSQE9iRg>?
GAMG	NGDmSYpIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		NXTadVNMUW6qaXLpeIlwdiCxZjDoeY1idiCJQV3HJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUCgQUAxNjByM{iyN{DPxE1w	MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlAyOTh{Lze+V2FPT0WUPD;hQi=>
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NCI-H2009	NHHoTG5Iem:5dHigbY5pcWKrdHnvckBie3OjeR?=		M3HYTGlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyNFA6KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVAhRSBzOD63PFE2KM7:TT6=	MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlAyOTh{Lze+V2FPT0WUPD;hQi=>
HT-29	MkLoS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		MUfJcohq[mm2aX;uJI9nKGi3bXHuJGhVNTJ7IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTBiPTCxPE45QDd2IN88UU4>	MlrUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVIxOTF6Mj:nQnNCVkeHUkyvZV4>
CW-2	NFTRRlZIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		MVXJcohq[mm2aX;uJI9nKGi3bXHuJGNYNTJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OCB;IEKxMlQyOzdizszNMi=>	NYn0NGlYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJyMUG4Nk8oRlODTlfFVlww[T5?
HCC1187	MWLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?		NVTsOIlXUW6qaXLpeIlwdiCxZjDoeY1idiCKQ1OxNVg4KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVAhRSB{ND62NVY5KM7:TT6=	M3:1eVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzODFzOEKvK\|5USU6JRWK8M4E,
SK-LMS-1	M4rTZmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7		NIL0PZhKdmirYnn0bY9vKG:oIHj1cYFvKFONLVzNV{0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVAhRSB{Nz60OFc3KM7:TT6=	MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNlAyOTh{Lze+V2FPT0WUPD;hQi=>
SJRH30	MmjqS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		MUDJcohq[mm2aX;uJI9nKGi3bXHuJHNLWkh\|MDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyIE2gN\|YvPjFyOTFOwG0v	M2HkNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzODFzOEKvK\|5USU6JRWK8M4E,
HUTU-80	NWm4Roh2T3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=		MnHQTY5pcWKrdHnvckBw\iCqdX3hckBJXVSXLUiwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUCgQUA1Oy55OUC1JO69VS5?	NXXPbpNtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJyMUG4Nk8oRlODTlfFVlww[T5?

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	p-mTOR / mTOR / p-S6 / S6 / p-4E-BP1 / 4E-BP1 ; PubMed: 23291985 Cancer Biol Ther The mTOR inhibitor temsirolimus inhibits the activation of mTOR and its downstream molecules in esophageal cancer cells. Three esophageal cancer cell lines (TE-1, TE-8, and TE-10) were treated with different concentrations of temsirolimus (0–1000nM) and western blot was performed with appropriate antibodies to detect the expression of mTOR and its downstream effectors. β-actin was served as an internal control. p-rS6 / rS6 / p-AKT /AKT ; PubMed: 22039466 PLoS One C, D, Phosphorylation of rS6 (P-rS6) and Akt (P-Akt T308 and P-Akt S473) after treatment with indicated doses of temsirolimus for 72 hrs in temsirolimus-sensitive (C) or temsirolimus-resistant (D) cells was determined by Western blotting. Expression of total rS6 and Akt protein serves as loading controls.	23291985 22039466
Immunofluorescence	NRF2; PubMed: 22848625 PLoS One Ectopic expression of Nrf2 (red) and nuclear staining with Dapi (blue) after a 6 hour drug incubation. Yellow numbers represent the percent of cells with nuclear Nrf2 +/− the standard deviation. Scale bar = 10 µM.	22848625
Growth inhibition assay	Cell growth (HGC-3 cells) ; PubMed: 30866995 J Exp Clin Cancer Res Effect of temsirolimus on the growth of HGC-3 and -20 cells in primary culture. Cell viability ; PubMed: 22039466 PLoS One A, B, Endometrial cancer cells were treated with increasing doses of temsirolimus for 72 hrs. Results are separated by (A) sensitivity or (B) resistance as determined by cell viability.	30866995 22039466

In vivo

In the NOD/SCID xenograft models with human ALL, Temsirolimus treatment at 10 mg/kg/day produces a decrease in peripheral blood blasts and in splenomegaly ^[3] Administration of Temsirolimus (20 mg/kg i.p. 5 days/week) significantly delays the growth of DAOY xenografts by 160% after 1 week and 240% after 2 weeks, compared with controls. Single high-dose of Temsirolimus (100 mg/kg i.p) treatment induces 37% regression of tumor volume within 1 week. Temsirolimus treatment for 2 weeks also delays the growth of rapamycin-resistant U251 xenografts by 148%. ^[4] Inhibition of mTOR by Temsirolimus improves performance on four different behavioral tasks and decreases aggregate formation in a mouse model of Huntington disease. ^[5] Administration of Temsirolimus induces significant dose-dependent, antitumor responses against subcutaneous growth of 8226, OPM-2, and U266 xenografts with ED50 of 20 mg/kg and 2 mg/kg for 8226 and OPM-2, respectively, which are associated with inhibited proliferation and angiogenesis, induction of apoptosis, and reduction in tumor cell size. ^[6]

Protocol

Kinase Assay: ^[1]	- Collapse In vitro assay of mTOR catalytic activity: The Flag-tagged wild-type human mTOR (Flag-mTOR) DNA constructs are transiently transfected into HEK293 cells. Protein extraction and purification of Flag-mTOR are carried out 48 hours later. In vitro kinase assays of purified Flag-mTOR in the presence of various concentrations of Temsirolimus without FKBP12 are performed in 96-well plate and detected by dissociation-enhanced lanthanide fluorescent immunoassay (DELFIA) using His6-S6K1 as the substrate. Enzymes is first diluted in kinase assay buffer (10 mM Hepes (pH 7.4), 50 mM NaCl, 50 mM β-glycerophosphate, 10 mM MnCl₂, 0.5 mM DTT, 0.25 μM microcystin LR, and 100 μg/mL BSA). To each well, 12 μL of the diluted enzyme is mixed briefly with 0.5 μL Temsirolimus. The kinase reaction is initiated by adding 12.5 μL kinase assay buffer containing ATP and His6-S6K to give a final reaction volume of 25 μL containing 800 ng/mL FLAG-mTOR, 100 μM ATP, and 1.25 μM His6-S6K. The reaction plate is incubated for 2 hours (linear at 1-6 hours) at room temperature with gentle shaking and then terminated by adding 25 μL Stop buffer (20 mM Hepes (pH 7.4), 20 mM EDTA, and 20 mM EGTA). The DELFIA detection of the phosphorylated (Thr-389) His6-S6K is performed at room temperature using a monoclonal anti-P(T389)-p70S6K antibody labeled with Europium-N1-ITC (Eu) (10.4 Eu per antibody). 45 μL of the terminated kinase reaction mixture is transferred to a MaxiSorp plate containing 55 μL PBS. The His6-S6K is allowed to attach for 2 hours after which the wells are aspirated and washed once with PBS. 100 μL of DELFIA buffer with 40 ng/mL Eu-P(T389)-S6K antibody is added. The antibody binding is continued for 1 hour with gentle agitation. The wells are then aspirated and washed four times with PBS containing 0.05% Tween 20 (PBST). 100 μL of DELFIA Enhancement solution is added to each well and the plates are read in a PerkinElmer Victor model plate reader.
Cell Research: ^[1]	- Collapse Cell lines: A549, H157, H460, H446, HCT116, HT29, SW480, DLD1, Caco2, LNCap, DU145, MDA468, MDA231, HEK293, and PC3-MM2 Concentrations: Dissolved in DMSO, final concentrations ~20 μM Incubation Time: 72 hours Method: Cells are exposed to various concentrations of Temsirolimus for 72 hours. After treatment, viable cell densities are determined by MTS dye conversion using CellTiter AQ assay kit. (Only for Reference)
Animal Research: ^[4]	- Collapse Animal Models: Female athymic nude mice injected s.c. with DAOY, or U251 cells Dosages: 20 mg/kg Administration: Injection daily 5 times per week (Only for Reference)

References

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Solubility (25°C)

In vitro	Ethanol	75 mg/mL (72.79 mM)
	DMSO	67 mg/mL (65.03 mM)
	Water	Insoluble
In vivo	Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 2% DMSO+30% PEG 300 +2% Tween 80+ddH2O For best results, use promptly after mixing.	7mg/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 Download Temsirolimus (CCI-779) SDF

Molecular Weight	1030.29
Formula	C₅₆H₈₇NO₁₆
CAS No.	162635-04-3
Storage	3 years-20°C powder 2 years-80°C in solvent
Synonyms	NSC 683864
Smiles	CC1CCC2CC(C(=CC=CC=CC(CC(C(=O)C(C(C(=CC(C(=O)CC(OC(=O)C3CCCCN3C(=O)C(=O)C1(O2)O)C(C)CC4CCC(C(C4)OC)OC(=O)C(C)(CO)CO)C)C)O)OC)C)C)C)OC

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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.
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Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2020-01-06)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT01653067	Unknown status	Drug: Rituximab Temsirolimus DHAP intravenous	Diffuse Large B-Cell Lymphoma	Mathias Witzens-Harig\|Johannes Gutenberg University Mainz\|Technische Universität München\|Ludwig-Maximilians - University of Munich\|University Hospital Ulm\|University Hospital Erlangen\|Charite University Berlin Germany\|University Hospital Freiburg\|Johann Wolfgang Goethe University Hospital\|University Hospital Heidelberg	September 2012	Phase 2
NCT02093598	Completed	Drug: Temsirolimus	Carcinoma Endometrioid\|mTOR Protein	MedSIR	May 2012	Phase 2

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mTOR Signaling Pathway Map

mTOR Inhibitors with Unique Features

Pan mTOR inhibitor

KU-0063794 : mTORC1 and mTORC2, IC50=~10 nM.
Most Potent mTOR Inhibitor

Rapamycin (Sirolimus) : mTOR, IC50=~0.1 nM.
FDA-approved mTOR Inhibitor

Everolimus (RAD001) : Approved by FDA for Rejection of organ transplants as well as renal cell cancer and other tumors.
Newest mTOR Inhibitor

XL388 ^New : Highly potent, selective, ATP-competitive inhibitor of mTOR with IC50 of 9.9 nM, 1000-fold selectivity over the closely related PI3K kinases.

Related mTOR Products

MHY1485 ^New

MHY1485 is a potent, and cell-permeable mTOR activator, and also potently inhibits autophagy.
CHIR-99021 (CT99021) ^New

CHIR-99021 (CT99021) is a GSK-3α and GSK-3β inhibitor with IC50 of 10 nM and 6.7 nM, respectively. CHIR99201 does not exhibit cross-reactivity against cyclin-dependent kinases (CDKs) and shows a 350-fold selectivity toward GSK-3β compared to CDKs. CHIR99021 functions as a Wnt/β-catenin activator and induces autophagy.
Dorsomorphin (Compound C) ^New

Dorsomorphin (Compound C, BML-275) is a potent, reversible, selective AMPK inhibitor with K_i of 109 nM in cell-free assays, exhibiting no significant inhibition of several structurally related kinases including ZAPK, SYK, PKCθ, PKA, and JAK3. Dorsomorphin selectively inhibits the BMP type I receptors ALK2, ALK3 and ALK6. Dorsomorphin is used in promoting specific cell differentiation and inducing cancer cell line autophagy.
Rapamycin (Sirolimus)

Rapamycin (Sirolimus, AY 22989, NSC-2260804) is a specific mTOR inhibitor with IC50 of ~0.1 nM HEK293 cells.
Everolimus (RAD001)

Everolimus (RAD001) is an mTOR inhibitor of FKBP12 with IC50 of 1.6-2.4 nM in a cell-free assay. Everolimus induces cell apoptosis and autophagy and inhibits tumor cells proliferation.
AZD8055

AZD8055 is a novel ATP-competitive mTOR inhibitor with IC50 of 0.8 nM in MDA-MB-468 cells with excellent selectivity (∼1,000-fold) against PI3K isoforms and ATM/DNA-PK. AZD8055 induces caspase-dependent apoptosis and also induces autophagy. Phase 1.

Features:First drug to inhibit both types of mTOR protein.
Torin 1

Torin 1 is a potent inhibitor of mTORC1/2 with IC50 of 2 nM/10 nM in cell-free assays; exhibits 1000-fold selectivity for mTOR than PI3K.
Sapanisertib (MLN0128)

Sapanisertib (MLN0128, INK 128, TAK-228) is a potent and selective mTOR inhibitor with IC50 of 1 nM in cell-free assays; >200-fold less potent to class I PI3K isoforms, superior in blocking mTORC1/2 and sensitive to pro-invasion genes (vs Rapamycin). Phase 1.
Tacrolimus (FK506)

Tacrolimus (FK506, FR900506, Fujimycin, Prograf) is a 23-membered macrolide lactone, it reduces peptidyl-prolyl isomerase activity in T cells by binding to the immunophilin FKBP12 (FK506 binding protein) creating a new complex. Tacrolimus also inhibits the phosphatase activity of calcineurin. Tacrolimus induces vascular endothelial autophagy.
KU-0063794

KU-0063794 is a potent and highly specific dual-mTOR inhibitor of mTORC1 and mTORC2 with IC50 of ~10 nM in cell-free assays; no effect on PI3Ks.

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Temsirolimus (CCI-779)