- 抑制劑
- 研究領(lǐng)域
- PI3K/Akt/mTOR信號(hào)通路
- 表觀遺傳
- 甲基化
- 免疫&炎癥
- 酪氨酸蛋白激酶
- 血管生成
- 凋亡
- 自噬
- 內(nèi)質(zhì)網(wǎng)應(yīng)激&UPR響應(yīng)
- JAK/STAT信號(hào)通路
- MAPK信號(hào)通路
- 細(xì)胞骨架
- 細(xì)胞周期
- TGF-beta/Smad信號(hào)通路
- DNA損傷/DNA修復(fù)
- 化合物庫
- 抗體
- 生物試劑
- qPCR
- 2x SYBR Green qPCR Master Mix
- 2x SYBR Green qPCR Master Mix(Low ROX)
- 2x SYBR Green qPCR Master Mix(High ROX)
- 蛋白實(shí)驗(yàn)
- Protein A/G免疫沉淀磁珠
- Anti-DYKDDDDK Tag免疫磁珠
- Anti-DYKDDDDK Tag親和凝膠
- Anti-Myc免疫磁珠
- Anti-HA免疫磁珠
- 磁力架
- Poly DYKDDDDK Tag多肽
- 細(xì)胞核與細(xì)胞漿蛋白抽提試劑盒
- 免疫磁珠
- 蛋白酶抑制劑Cocktail
- 蛋白酶抑制劑Cocktail(DMSO儲(chǔ)液)
- 磷酸酶抑制劑Cocktail
- 細(xì)胞實(shí)驗(yàn)
- Cell Counting Kit-8 (CCK-8)
- 動(dòng)物實(shí)驗(yàn)
- 鼠尾直接PCR試劑盒(快速基因型鑒定)
- 小鼠CD3+ T細(xì)胞分選試劑盒
- 小鼠CD4+ T細(xì)胞分選試劑盒
- 小鼠CD8+ T細(xì)胞分選試劑盒
- 新產(chǎn)品
- 聯(lián)系我們
Sapanisertib (MLN0128)
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(xì)胞試驗(yàn)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) Chemical Structure
CAS: 1224844-38-5
產(chǎn)品質(zhì)控
批次：
純度：
99.94%
99.94
Sapanisertib (MLN0128)相關(guān)產(chǎn)品
| 相關(guān)靶點(diǎn) | mTORC1 mTORC2 | 點(diǎn)擊展開 |
|---|---|---|
| 相關(guān)產(chǎn)品 | AZD8055 Torin 1 Ridaforolimus (Deforolimus, MK-8669) Torkinib (PP242) Vistusertib (AZD2014) MHY1485 KU-0063794 Torin 2 OSI-027 WYE-354 WYE-125132 (WYE-132) 3BDO Palomid 529 (P529) Zotarolimus (ABT-578) Salidroside WAY-600 GDC-0349 Onatasertib (CC 223) WYE-687 XL388 | 點(diǎn)擊展開 |
| 相關(guān)化合物庫 | 激酶抑制劑庫 PI3K/Akt 抑制劑庫 凋亡分子化合物庫 細(xì)胞周期化合物庫 NF-κB信號(hào)通路庫 | 點(diǎn)擊展開 |
相關(guān)信號(hào)通路圖
細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例
| 細(xì)胞系 | 實(shí)驗(yàn)類型 | 給藥濃度 | 孵育時(shí)間 | 活性描述 | 文獻(xiàn)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 |
| 點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù) | |||||
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(xì)胞試驗(yàn)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(diǎn) |
|
| 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。[1] 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(xì)胞株的有效抑制效應(yīng)。[2] |
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| 實(shí)驗(yàn)圖片 | 檢測方法 | 檢測指標(biāo) | 實(shí)驗(yàn)圖片 | PMID | ||
| Western blot |
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