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Sapanisertib (MLN0128, INK-128)

別名: INK 128,TAK-228

Sapanisertib (MLN0128, INK 128, TAK-228) 是一種有效的，選擇性mTOR抑制劑，在無細胞試驗中IC50為1 nM；對I型PI3K亞型的作用效果低200倍以上，與Rapamycin相比，優(yōu)先抑制mTORC1/2，且對促侵襲基因敏感。Phase 1。

Sapanisertib (MLN0128, INK-128) Chemical Structure

Sapanisertib (MLN0128, INK-128) Chemical Structure

CAS: 1224844-38-5

規(guī)格 價格 庫存 購買數(shù)量
10mM (1mL in DMSO) 1810.73 現(xiàn)貨
5mg 1405.88 現(xiàn)貨
50mg 7924.38 現(xiàn)貨
100mg 10401.3 現(xiàn)貨
1g 32678.1 現(xiàn)貨
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細胞實驗數(shù)據(jù)示例

細胞系 實驗類型 給藥濃度 孵育時間 活性描述 文獻信息(PMID)
U87 Function assay Inhibition of mTOR in human U87 cells assessed as reduction in pRAS40 phosphorylation by Western blot method ChEMBL
U87 Function assay Inhibition of mTOR pS6K in human U87 cells assessed as inhibition of 4EBP1 phosphorylation by Western blot analysis ChEMBL
PANC-1? Function Assay 50 nM 48 h disrupts cell cycle progression 24971544
PANC-1? Function Assay 10 nM 72 h increases LY 188011 sensitivity 24971544
PANC-1? Function Assay 10/50 nM 24 h dramatically inhibits phosphorylation of 4E-BP1-S6K1 (mTORC1 activation indicators) and Akt at Ser 473 (the mTORC2 activation indicator) 24971544
PANC-1? Apoptosis Assay 10-100 nM 72 h induces apoptosis dose dependently 24971544
MIA PaCa-2 Cell Viability Assay 1-100 nM 72 h inhibits cell viability dose dependently 24971544
PANC-1? Cell Viability Assay 50 nM 24-96 h inhibits cell viability time dependently 24971544
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells 29435139
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells 29435139
U-2 OS qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells 29435139
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells 29435139
A2058 Function assay 1 hr Inhibition of TORC2 in human A2058 cells assessed as decrease in PKB/Akt phosphorylation at Ser473 after 1 hr by Western blot analysis 30359003
A2058 Function assay 1 hr Inhibition of TORC1 in human A2058 cells assessed as decrease in S6 phosphorylation at Ser235/236 after 1 hr by Western blot analysis 30359003
A2058 Function assay 1 hr Inhibition of TORC1 in human A2058 cells assessed as decrease in 4E-BP1 phosphorylation after 1 hr by Western blot analysis 30359003
SKOV3 Function assay 1 hr Inhibition of TORC1 in human SKOV3 cells assessed as decrease in S6 phosphorylation at Ser235/236 after 1 hr by Western blot analysis 30359003
SKOV3 Function assay 1 hr Inhibition of TORC1 in human SKOV3 cells assessed as decrease in S6K phosphorylation after 1 hr by Western blot analysis 30359003
A2058 Function assay 1 hr Inhibition of TORC1 in human A2058 cells assessed as decrease in S6K phosphorylation after 1 hr by Western blot analysis 30359003
SKOV3 Function assay 1 hr Inhibition of TORC2 in human SKOV3 cells assessed as decrease in PKB/Akt phosphorylation at Ser473 after 1 hr by Western blot analysis 30359003
U87 Function assay Inhibition of mTOR in human U87 cells assessed as reduction in pAKT phosphorylation at residue 47 by Western blot method ChEMBL
PANC-1? Cell Viability Assay 1-100 nM 72 h inhibits cell viability dose dependently 24971544
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells 29435139
U-2 OS qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells 29435139
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells 29435139
SKOV3 Function assay 1 hr Inhibition of TORC1 in human SKOV3 cells assessed as decrease in 4E-BP1 phosphorylation after 1 hr by Western blot analysis 30359003
PC3 Antiproliferative assay 72 hrs Antiproliferative activity against human PC3 cells measured after 72 hrs by Alamar blue dye-based fluorescence analysis, EC50 = 0.1 μM. ChEMBL
U87 Function assay Inhibition of mTOR in human U87 cells assessed as reduction in p4EBP1 phosphorylation by Western blot method ChEMBL
U87 Function assay Inhibition of mTOR pS6K in human U87 cells assessed as inhibition of RAS40 phosphorylation by Western blot analysis ChEMBL
U87 Antitumor assay 0.3 to 3 mg/kg 14 days Antitumor activity against human U87 cells xenografted in mouse assessed as tumor growth inhibition at 0.3 to 3 mg/kg measured after 14 days ChEMBL
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生物活性

產(chǎn)品描述 Sapanisertib (MLN0128, INK 128, TAK-228) 是一種有效的，選擇性mTOR抑制劑，在無細胞試驗中IC50為1 nM；對I型PI3K亞型的作用效果低200倍以上，與Rapamycin相比，優(yōu)先抑制mTORC1/2，且對促侵襲基因敏感。Phase 1。
靶點
mTOR
(Cell-free assay)		 mTOR
(Cell-free assay)		 PI3Kα
(Cell-free assay)		 PI3Kγ
(Cell-free assay)		 PI3Kδ
(Cell-free assay)		 點擊更多
1.4 nM(Ki) 1.4 nM(Ki) 219 nM 221 nM 230 nM
體外研究(In Vitro)
體外研究活性

INK 128 表現(xiàn)對mTOR酶的抑制活性并對PI3K激酶的選擇性超過100倍。

作為TORC1/2抑制劑，INK 128抑制TORC1的下游底物S6和4EBP1的磷酸化。此外，INK 128也顯示了對雷帕霉素和泛PI3K抑制劑耐受的細胞株的有效抑制效應。
實驗圖片 檢測方法 檢測指標 實驗圖片 PMID
Western blot

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