Sapanisertib (MLN0128)

For research use only. Not for use in humans.

目录号：S2811 别名： INK 128,TAK-228

Sapanisertib (MLN0128) Chemical Structure

CAS No. 1224844-38-5

Sapanisertib (MLN0128, INK 128, TAK-228) 是一种有效的，选择性mTOR抑制剂，在无细胞试验中IC50为1 nM；对I型PI3K亚型的作用效果低200倍以上，与Rapamycin相比，优先抑制mTORC1/2，且对促侵袭基因敏感。Phase 1。

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库存

购买数量

10mM (1mL in DMSO)	RMB 1810.73	现货
5mg	RMB 1405.88	现货
50mg	RMB 7924.38	现货
100mg	RMB 10401.3	现货
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客户使用Selleck生产的Sapanisertib (MLN0128)发表文献90篇：

Cancer Cell, 2021, S1535-6108(20)30609-7

PubMed: 33417832 ( click the link to review the publication )

Cell Metab, 2021, S1550-4131(21)00326-0

PubMed: 34348115 ( click the link to review the publication )

Cell, 2020, 182(3):685-712.e19

PubMed: 32645325 ( click the link to review the publication )

Cell Stem Cell, 2019, 10.1016/j.stem.2019.10.005

PubMed: 31786016 ( click the link to review the publication )

Cancer Discov, 2017, 7(12):1450-1463

PubMed: 28963352 ( click the link to review the publication )

Cancer Cell, 2017, 31(3):424-435

PubMed: 28292440 ( click the link to review the publication )

Cell Metab, 2017, 26(6):817-829

PubMed: 28988820 ( click the link to review the publication )

Cancer Discov, 2014, 4(5):554-63

PubMed: 24631838 ( click the link to review the publication )

Nat Chem Biol, 2021, 10.1038/s41589-021-00751-4

PubMed: 33686292 ( click the link to review the publication )

Nat Commun, 2021, 12(1):245

PubMed: 33431855 ( click the link to review the publication )

Clin Cancer Res, 2021, clincanres.3017.2020

PubMed: 33414137 ( click the link to review the publication )

Aging Cell, 2021, 20(2):e13304

PubMed: 33448083 ( click the link to review the publication )

Cancer Lett, 2021, 504:137-145

PubMed: 33571541 ( click the link to review the publication )

Cancers (Basel), 2021, 13(11)2778

PubMed: 34204960 ( click the link to review the publication )

Cell Death Discov, 2021, 7(1):179

PubMed: 34282122 ( click the link to review the publication )

Stem Cell Res Ther, 2021, 12(1):170

PubMed: 33691762 ( click the link to review the publication )

Stem Cells Transl Med, 2021, 10.1002/sctm.20-0386

PubMed: 33656802 ( click the link to review the publication )

Endocrinology, 2021, 162(3)bqaa239

PubMed: 33367617 ( click the link to review the publication )

Cell Mol Biol Lett, 2021, 26(1):18

PubMed: 34006213 ( click the link to review the publication )

Oral Dis, 2021, 10.1111/odi.13860

PubMed: 33772986 ( click the link to review the publication )

Neuro Oncol, 2020, 15;22(4):563-574

PubMed: 31841591 ( click the link to review the publication )

Theranostics, 2020, 25;10(10):4627-4643

PubMed: 32292519 ( click the link to review the publication )

Cancer Res, 2020, 10;canres.57.2020

PubMed: 32522823 ( click the link to review the publication )

Cell Rep, 2020, 31(12):107800

PubMed: 32579927 ( click the link to review the publication )
Oncogene, 2020, 10.1038/s41388-020-01552-0

PubMed: 33191406 ( click the link to review the publication )

Cell Death Dis, 2020, 11(10):925

PubMed: 33116117 ( click the link to review the publication )

Glia, 2020, 10.1002/glia.23921

PubMed: 33068318 ( click the link to review the publication )

Aging (Albany NY), 2020, 12(12):11864-11877

PubMed: 32568101 ( click the link to review the publication )

J Cell Sci, 2020, jcs.241356

PubMed: 32546533 ( click the link to review the publication )

Front Mol Biosci, 2020, 7:566291

PubMed: 33425984 ( click the link to review the publication )

J Biol Chem, 2020, jbc.RA120.014960

PubMed: 33273014 ( click the link to review the publication )

Breast Cancer Res Treat, 2020, 179(2):337-347

PubMed: 31655920 ( click the link to review the publication )

Sci Rep, 2020, 10(1):12644

PubMed: 32724089 ( click the link to review the publication )

Int J Biol Markers, 2020, 1724600820943610

PubMed: 32686562 ( click the link to review the publication )

Mol Oncol, 2020, 10.1002/1878-0261.12673

PubMed: 32191822 ( click the link to review the publication )

Proc Natl Acad Sci U S A, 2019, 10.1073/pnas.1911393116

PubMed: 31732667 ( click the link to review the publication )

Cancer Res, 2019, 79(1):209-219

PubMed: 30389701 ( click the link to review the publication )

Mol Syst Biol, 2019, 15(3):e8323

PubMed: 30858180 ( click the link to review the publication )

Cancer Res, 2019, 10.1158/0008-5472.CAN-18-2808

PubMed: 31806641 ( click the link to review the publication )

MBio, 2019, 10(1)

PubMed: 30782662 ( click the link to review the publication )

Sci Signal, 2019, 12(570)

PubMed: 30808819 ( click the link to review the publication )

Cancers (Basel), 2019, 11(12)

PubMed: 31795447 ( click the link to review the publication )

Stem Cells, 2019, 37(7):888-898

PubMed: 30913328 ( click the link to review the publication )

Mol Cancer Ther, 2019, 18(11):1985-1996

PubMed: 31308077 ( click the link to review the publication )

Biochim Biophys Acta Mol Basis Dis, 2019, 1865(1):1-13

PubMed: 30292636 ( click the link to review the publication )

J Cell Physiol, 2019, 234(2):1618-1629

PubMed: 30132862 ( click the link to review the publication )

Front Oncol, 2019, 9:1119

PubMed: 31750239 ( click the link to review the publication )

J Bone Oncol, 2019, 15:100222

PubMed: 30766792 ( click the link to review the publication )
JCI Insight, 2019, 4(18)

PubMed: 31534053 ( click the link to review the publication )

Oncotarget, 2019, 10(49):5011-5019

PubMed: 31489111 ( click the link to review the publication )

Clin Cancer Res, 2018, 24(22):5658-5672

PubMed: 30087143 ( click the link to review the publication )

Mol Cancer Ther, 2018, 17(2):347-354

PubMed: 28958992 ( click the link to review the publication )

Mol Cancer Res, 2018, 16(11):1773-1784

PubMed: 29967110 ( click the link to review the publication )

Int J Biol Sci, 2018, 14(10):1221-1231

PubMed: 30123071 ( click the link to review the publication )

Mol Carcinog, 2018, 57(11):1445-1457

PubMed: 29963728 ( click the link to review the publication )

J Chromatogr B Analyt Technol Biomed Life Sci, 2018,

PubMed: 29195143 ( click the link to review the publication )

Acta Biochim Biophys Sin (Shanghai), 2018, 10.1093/abbs/gmy088

PubMed: 30060081 ( click the link to review the publication )

Oncotarget, 2018, 9(86):35676-35686

PubMed: 30479697 ( click the link to review the publication )

J Exp Med, 2018, 215(1):159-175

PubMed: 29141866 ( click the link to review the publication )

Hepatology, 2017, 66(6):1920-1933

PubMed: 28732118 ( click the link to review the publication )

Nat Commun, 2017, 8(1):2207

PubMed: 29263324 ( click the link to review the publication )

Nucleic Acids Res, 2017, 45(16):9654-9678

PubMed: 28934469 ( click the link to review the publication )

Neuro-oncology, 2017,

PubMed: 28582547 ( click the link to review the publication )

Clin Cancer Res, 2017, 23(12):3045-3052

PubMed: 28007777 ( click the link to review the publication )

Dev Cell, 2017, 43(6):673-688

PubMed: 29103956 ( click the link to review the publication )

Proc Natl Acad Sci U S A, 2017, 114(12):3186-3191

PubMed: 28270607 ( click the link to review the publication )

Cancer Discov, 2017, 7(12):1450-1463

PubMed: 28963352 ( click the link to review the publication )

Sci Rep, 2017, 7(1):1876

PubMed: 28500298 ( click the link to review the publication )

J Biol Chem, 2017, 292(9):3947-3957

PubMed: 28100775 ( click the link to review the publication )

J Pharm Biomed Anal, 2017, 145:473-481

PubMed: 28743078 ( click the link to review the publication )

Biomed Chromatogr, 2017, 31(3)

PubMed: 27554984 ( click the link to review the publication )

Oncotarget, 2017, 8(21):34552-34564

PubMed: 28388555 ( click the link to review the publication )
Oncotarget, 2017, 8(4):5992-6002

PubMed: 27863413 ( click the link to review the publication )

Sci Rep, 2017, 7(1):6529

PubMed: 28747804 ( click the link to review the publication )

Int J Cancer, 2016, 138(5):1246-55

PubMed: 26422827 ( click the link to review the publication )

Antimicrobial Agents and Chemotherapy, 2016, 10.1128/AAC.02921-15

PubMed: 26976874 ( click the link to review the publication )

Front Microbiol, 2016, 7:1658

PubMed: 27812353 ( click the link to review the publication )

Int J Oncol, 2016, 48(1):253-60

PubMed: 26549638 ( click the link to review the publication )

Cancer Res, 2015, 75(22):4910-22

PubMed: 26574479 ( click the link to review the publication )

Cell Rep, 2015, 11(3):446-59

PubMed: 25865887 ( click the link to review the publication )

Cell Commun Signal, 2015, 13:15

PubMed: 25849580 ( click the link to review the publication )

Cell Communication and Signaling, 2015, 13:15

PubMed: ( click the link to review the publication )

Sci Rep, 2015, 5:18251

PubMed: 26671574 ( click the link to review the publication )

Apoptosis, 2015, 20(1):50-62

PubMed: 25425103 ( click the link to review the publication )

Cancer Biol Ther, 2015,

PubMed: 25692620 ( click the link to review the publication )

Oncology, 2015, 88(5):309-19

PubMed: 25591719 ( click the link to review the publication )

Oncotarget, 2015, 6(31):32089-103

PubMed: 26392332 ( click the link to review the publication )

Tumour Biol, 2015, 36(10):8177-84

PubMed: 25990456 ( click the link to review the publication )

Biochem Biophys Res Commun, 2014, 450(2):973-8

PubMed: 24971544 ( click the link to review the publication )

Biochem Biophys Res Commun, 2013, 440(4):701-6

PubMed: 24103749 ( click the link to review the publication )

产品安全说明书

mTOR抑制剂选择性比较

生物活性

产品描述

靶点

mTOR ^[3] (Cell-free assay)	mTOR ^[3] (Cell-free assay)	PI3Kα ^[3] (Cell-free assay)	PI3Kγ ^[3] (Cell-free assay)	PI3Kδ ^[3] (Cell-free assay)	点击更多
1.4 nM(Ki)	1.4 nM(Ki)	219 nM	221 nM	230 nM	点击更多

体外研究

INK 128 表现对mTOR酶的抑制活性并对PI3K激酶的选择性超过100倍。^[1] 作为TORC1/2抑制剂，INK 128抑制TORC1的下游底物S6和4EBP1的磷酸化。此外，INK 128也显示了对雷帕霉素和泛PI3K抑制剂耐受的细胞株的有效抑制效应。^[2]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
PANC-1	MUfGeY5kfGmxbjDBd5NigQ>?	NYXoU\|kzOTBibl2=	M2\1cFczKGh?	MWTpcoNz\WG\|ZYOg[4Vu[2m2YXLpcoUhe2Wwc3n0bZZqfHl?	NUjhSpB{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5O\|E2PDRpPkK0PVcyPTR2PD;hQi=>
PANC-1	NWDDRmR1TnWwY4Tpc44hSXO\|YYm=	NVXzTlBGPTBibl2=	MYm0PEBp	NYTrV4p6\Gm\|coXweJMh[2WubDDjfYNt\SCycn;ndoV{e2mxbh?=	M1rVNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUexOVQ1Lz5{NEm3NVU1PDxxYU6=
PANC-1	M2HvOmZ2dmO2aX;uJGF{e2G7	M2Hae\|ExNzVyIH7N	Mon3NlQhcA>?	Mlvt[JJidWG2aXPhcIx6KGmwaHnibZR{KHCqb4PwbI9zgWyjdHnvckBw\iB2RT3CVFEuWz[NMTCocXRQWkNzIHHjeIl3[XSrb36gbY5lcWOjdH;yd{kh[W6mIFHreEBifCCVZYKgOFc{KCi2aHWgcXRQWkN{IHHjeIl3[XSrb36gbY5lcWOjdH;yLS=>	MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDl5MUW0OEc,OjR7N{G1OFQ9N2F-
PANC-1	MlvxRZBweHSxc3nzJGF{e2G7	NEf1TXUyOC1zMECgcm0>	MUC3NkBp	MUXpcoR2[2W\|IHHwc5B1d3OrczDkc5NmKGSncHXu[IVvfGy7	NYHTTnYyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5O\|E2PDRpPkK0PVcyPTR2PD;hQi=>
MIA PaCa-2	NXn0Z4x5S2WubDDWbYFjcWyrdImgRZN{[Xl?	M3HaWFEuOTByIH7N	MlLvO\|IhcA>?	NV7n[JVEcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?=	MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDl5MUW0OEc,OjR7N{G1OFQ9N2F-
PANC-1	M4W4W2NmdGxiVnnhZoltcXS7IFHzd4F6	MlTyOVAhdk1?	M{njfVI1NTl4IHi=	NYS0SYtwcW6qaXLpeJMh[2WubDD2bYFjcWyrdImgeIlu\SCmZYDlcoRmdnSueR?=	MnHyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7N{G1OFQoRjJ2OUexOVQ1RC:jPh?=
PANC-1	MWDD[YxtKF[rYXLpcIl1gSCDc4PhfS=>	NGfkS3QyNTFyMDDuUS=>	MUG3NkBp	NEnY[nRqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7	NWewdldmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5O\|E2PDRpPkK0PVcyPTR2PD;hQi=>
TC32	M37Ie5FJXFNiYYPzZZk>			MX7xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhXEN\|MjDj[Yxtew>?	M3rDelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
U-2 OS	M{fwbJFJXFNiYYPzZZk>			MYHxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhXS1{IF;TJINmdGy\|	MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
A673	MmfDdWhVWyCjc4PhfS=>			M{DCfJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCDNkezJINmdGy\|	MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
DAOY	M4LRSpFJXFNiYYPzZZk>			MoS2dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKESDT2mgZ4VtdHN?	NGD4OZA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
Saos-2	M4\1RZFJXFNiYYPzZZk>			MVvxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW2Gxcz2yJINmdGy\|	NFjsdIQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
BT-37	MojIdWhVWyCjc4PhfS=>			M3H5WpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCEVD2zO{Bk\Wyucx?=	MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
RD	MnezdWhVWyCjc4PhfS=>			M2rEbpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCURDDj[Yxtew>?	MlTsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
SK-N-SH	M2S0W5FJXFNiYYPzZZk>			MkTEdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tV2gh[2WubIO=	MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
BT-12	NFzFXmhyUFSVIHHzd4F6			M{iwWpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCEVD2xNkBk\Wyucx?=	NFrkOXQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
MG 63 (6-TG R)	NWnBRXhIeUiWUzDhd5NigQ>?			NXnwVWJqeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IF3HJFY{KCh4LWTHJHIqKGOnbHzz	NUmyVW1zRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
BT-12	MXzxTHRUKGG\|c3H5			MkK2dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgRnQuOTJiY3XscJM>	NWXTUYR1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
OHS-50	MnfudWhVWyCjc4PhfS=>			MnLadWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKE:KUz21NEBk\Wyucx?=	NIL3doI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
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SKOV3	NFK5NmRHfW6ldHnvckBie3OjeR?=		MVSxJIhz	MV3Jcohq[mm2aX;uJI9nKFSRUlOyJIlvKGi3bXHuJHNMV1Z\|IHPlcIx{KGG\|c3Xzd4VlKGG\|IHTlZ5Jm[XOnIHnuJHBMSi:Da4SgdIhwe3Cqb4L5cIF1cW:wIHH0JHNmejR5MzDh[pRmeiBzIHjyJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrcx?=	MkLNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB\|NUmwNFMoRjNyM{W5NFA{RC:jPh?=
PC3	MkTjRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?		MmLwO\|IhcHK\|	NUjSZmZzSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDQR\|Mh[2WubIOgcYVie3W{ZXSgZYZ1\XJiN{KgbJJ{KGK7IFHsZY1ieiCkbIXlJIR6\S2kYYPl[EBndHWxcnXzZ4Vv[2ViYX7hcJl{cXNuIFXDOVAhRSByLkGg{txONg>?	NEK1NYk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw{PTR3MEm3M{c,S2iHTVLMQE9iRg>?
U87	NWDieWlkTnWwY4Tpc44h[XO\|YYm=			MX7Jcohq[mm2aX;uJI9nKG2WT2KgbY4hcHWvYX6gWVg4KGOnbHzzJIF{e2W\|c3XkJIF{KHKnZIXjeIlwdiCrbjDwRWtVKHCqb4PwbI9zgWyjdHnvckBifCC{ZYPp[JVmKDR5IHL5JHdme3Sncn6gZoxwfCCvZYToc4Q>	MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyzOVQ2ODl5Lze+R4hGVUKOPD;hQi=>
U87	MVXGeY5kfGmxbjDhd5NigQ>?			NV;4TXNGUW6qaXLpeIlwdiCxZjDtWG9TKGmwIHj1cYFvKFV6NzDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4heDSHQmCxJJBpd3OyaH;yfYxifGmxbjDifUBY\XO2ZYLuJIJtd3RibXX0bI9l	M1zmcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFM2PDVyOUevK\|5EcEWPQly8M4E,
U87	MWjGeY5kfGmxbjDhd5NigQ>?			M2jFfmlvcGmkaYTpc44hd2ZibWTPVkBxWz[NIHnuJIh2dWGwIGW4O{Bk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIETFRnAyKHCqb4PwbI9zgWyjdHnvckBjgSCZZYP0[ZJvKGKub4SgZY5idHm\|aYO=	M1e3[\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFM2PDVyOUevK\|5EcEWPQly8M4E,
U87	NG\u[Y9HfW6ldHnvckBie3OjeR?=			NIrMOYlKdmirYnn0bY9vKG:oIH3UU3IhcW5iaIXtZY4hXTh5IHPlcIx{KGG\|c3Xzd4VlKGG\|IILl[JVkfGmxbjDpckBxWkGVNECgdIhwe3Cqb4L5cIF1cW:wIHL5JHdme3Sncn6gZoxwfCCvZYToc4Q>	NX3mcXJ7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOzV2NUC5O{8oRkOqRV3CUFww[T5?
U87	NUj3UYNnTnWwY4Tpc44h[XO\|YYm=			M1GwcGlvcGmkaYTpc44hd2ZibWTPVkBxWz[NIHnuJIh2dWGwIGW4O{Bk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIGLBV\|QxKHCqb4PwbI9zgWyjdHnvckBjgSCZZYP0[ZJvKGKub4SgZY5idHm\|aYO=	MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyzOVQ2ODl5Lze+R4hGVUKOPD;hQi=>
U87	MnXBRY51cXS3bX;yJIF{e2G7	MXmwMlMhfG9iMzDt[{9s\w>?	MoPVNVQh\GG7cx?=	MoLzRY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iVUi3JINmdGy\|IIjlco9oemGodHXkJIlvKG2xdYPlJIF{e2W\|c3XkJIF{KHS3bX;yJIdzd3e2aDDpcohq[mm2aX;uJIF1KDBwMzD0c{A{KG2pL3vnJI1m[XO3cnXkJIFnfGW{IEG0JIRigXN?	NVjxcWVFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOzV2NUC5O{8oRkOqRV3CUFww[T5?

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	FKBP1 / MARS / CDC25A / TCL1A; PubMed: 25849580 Cell Commun Signal SUDHL-2 and SUDHL-4 cells are treated with EtOH (20 mM) for 48 h or INK128 (40 nM) for 24 h. Protein levels of validated genes were analyzed by western blotting. p-mTOR(Ser2448) / mTOR / p-p70S6K(Thr389) / p70S6K / p-RPS / RPS6; PubMed: 25849580 Cell Commun Signal SUDHL-2 and SUDHL-4 cells were treated with either EtOH for 24 h, INK128 for 3 h at the concentrations as indicated, or 20 nM rapamycin (Rap.) for 3 h. Cell lysates were analyzed by western blotting for phosphorylation states and total levels of indicated䲧疝Ỵ疞㧀疜 c-Jun; PubMed: 27462815 Nature Representative western blot of 293T cells after 24 h treatment with INK128. The results are representative of three independent experiments. CD44 / Vimentin; PubMed: 29899840 Oncotarget CD44 (high) SNU423 cells were treated with increasing concentrations of INK128 for 48 h. CD44, vimentin and downstream effectors of mTOR pathway were evaluated by immunoblotting. p-4EBP1 / 4EBP1 / p-S6 / S6 / p-Akt-S473 / p-Akt-T308 / Akt; PubMed: 25425103 Apoptosis INK128 inhibits mTOR signaling in neuroblastoma cells. A panel of six neuroblastoma cell lines was treated with 0.2 μM INK128 for 0 hr, 4 hrs, and 6 hrs, lysed, subjected to SDS-PAGE and immunoblotted with indicated antibodies. β-Actin was detected as a l䲧疝Ỵ疞㧀疜膉痘 瘿뙠ෆᾰƌෆĀ	25849580 27462815 29899840 25425103
Growth inhibition assay	Cell viability ; PubMed: 25425103 Apoptosis Six neuroblastoma cell lines were treated with the indicated concentrations of INK128 for 48 hrs. Cell viability was then measured by adding the mixture of 10 μL of CCK-8 and 190 μL of RPMI 1640 and reading the absorbance at 450 nm. Data were represented 䲧疝Ỵ疞㧀疜膉痘 瘿뙠ෆᾰƌෆĀ 㺣痖帉痖Ѐ瑖堘𢡄빢᎒ෆĀ鑸᎒彿堙奋堙巫堙᎒ﻺ᎒彿堙ﻮ᎒塚堙ﻺ	25425103

体内研究

在ZR-75-1乳腺癌异种移植模型中，INK 128（0.3 mg/kg/day）的处理表现了肿瘤生长抑制效果。^[1] 在多种移植体模型中，每日口服给药INK 128抑制血管生成和肿瘤生长。^[2]

参考文献

溶解度 (25°C)

体外	DMSO	62 mg/mL (200.43 mM)
	Ethanol	2 mg/mL (6.46 mM)
	Water	Insoluble
体内	从左到右依次将纯溶剂加入产品，现配现用(数据来自Selleck实验检测而非文献)： 30% PEG400+0.5% Tween80+5% propylene glycol	30 mg/mL

* 溶解度检测是由Selleck技术部门检测的，可能会和文献中提供的溶解度有所差异，这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据 Download Sapanisertib (MLN0128) SDF

分子量	309.33
化学式	C₁₅H₁₅N₇O
CAS号	1224844-38-5
储存条件	3年-20°C 粉状 2年-80°C 溶于溶剂
别名	INK 128,TAK-228

动物体内配方计算器 (澄清溶液)

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量

mg/kg

动物平均体重

每只动物给药体积

动物数量

只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO+ % + % Tween 80+ % ddH₂O

计算重置

计算结果:

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

质量

浓度

体积

分子量
=

×

×

*在配置溶液时，请务必参考Selleck产品标签上、SDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。

稀释计算器

用本工具协助配置特定浓度的溶液，使用的计算公式为：

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入输出 )

C1

V1

C2

V2
×

=

×

在配置溶液时，请务必参考Selleck产品标签上、SDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。.

连续稀释计算器方程

连续稀释
初始浓度:
稀释倍数:

计算结果

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):

分子量计算器

通过输入化合物的化学式来计算其分子量：

注：化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×
计算

临床试验信息 (data from https://clinicaltrials.gov, updated on 2021-09-06)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04250545	Recruiting	Drug: Sapanisertib\|Drug: Telaglenastat Hydrochloride	Leptomeningeal Neoplasm\|Metastatic Lung Non-Small Cell Carcinoma\|Metastatic Malignant Neoplasm in the Brain\|Recurrent Lung Non-Small Cell Carcinoma\|Stage IV Lung Cancer AJCC v8\|Stage IVA Lung Cancer AJCC v8\|Stage IVB Lung Cancer AJCC v8	National Cancer Institute (NCI)	November 9 2020	Phase 1
NCT02575339	Active not recruiting	Drug: MLN0128\|Drug: MLN0128 (RP2D)\|Drug: Sorafenib	Hepatocellular Carcinoma\|Liver Cancer\|HCC	Kathy Miller\|Millennium Pharmaceuticals Inc.\|Big Ten Cancer Research Consortium	July 2016	Phase 1\|Phase 2
NCT02719691	Completed	Drug: Alisertib\|Drug: MLN0128	Metastatic Breast Cancer\|Solid Tumors	University of Colorado Denver	May 13 2016	Phase 1
NCT02514824	Completed	Drug: MLN0128	Merkel Cell Carcinoma	Dana-Farber Cancer Institute\|Millennium Pharmaceuticals Inc.	October 2015	Phase 1\|Phase 2
NCT02244463	Active not recruiting	Drug: MLN0128	Anaplastic Thyroid Cancer\|Thyroid Cancer	Dana-Farber Cancer Institute\|Millennium Pharmaceuticals Inc.	July 2015	Phase 2

技术支持

在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题，请给我们留言。

常见问题及建议解决方法

问题 1：
What is the recommendation method to formulate S2811 INK 128 (MLN0128) for oral administration?
回答：
You can try this vehicle for oral administration: 30% PEG400+0.5% Tween80 +5% Propylene glycol.

mTOR Signaling Pathway Map

mTOR Inhibitors with Unique Features

选择性强的mTOR抑制剂

Rapamycin (Sirolimus) : mTORC1-selective, IC50=~0.1 nM.
活性最高的mTOR抑制剂

Rapamycin (Sirolimus) : mTOR, IC50=~0.1 nM.
FDA批准的mTOR抑制剂

Temsirolimus (CCI-779, NSC 683864) : Approved by FDA for Renal Cell Carcinoma (RCC).
最新的mTOR抑制剂

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.

研究领域

产品类型

定制您的化合物库

Sapanisertib (MLN0128)

客户使用Selleck生产的Sapanisertib (MLN0128)发表文献90篇：

产品安全说明书

mTOR抑制剂选择性比较

生物活性

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

参考文献

溶解度 (25°C)

化学数据 Download Sapanisertib (MLN0128) SDF

动物体内配方计算器 (澄清溶液)

计算器

摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

稀释计算器

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

连续稀释计算器方程

连续稀释

计算结果

分子量计算器

总分子量：g/mol

摩尔浓度计算器

临床试验信息 (data from https://clinicaltrials.gov, updated on 2021-09-06)

技术支持

常见问题及建议解决方法

mTOR Signaling Pathway Map

mTOR Inhibitors with Unique Features

相关mTOR产品