| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 10 mM * 1 mL in DMSO |
|
||
| 2mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| Other Sizes |
|
| 靶点 |
mTOR (IC50 = 1 nM); PI3Kα (IC50 = 219 nM); PI3Kγ (IC50 = 221 nM); PI3Kδ (IC50 = 230 nM); PI3Kβ (IC50 = 5.293 μM); mTORC1; mTORC2; Autophagy
|
|---|---|
| 体外研究 (In Vitro) |
Sapanisertib (INK-128) 对 mTOR 具有酶抑制活性，对 PI3K 激酶的选择性高于 100 倍[1]。在 PC3 细胞中，sapanisertib (INK-128) 特异性降低 YB1、MTA1、vimentin 和 CD44 的蛋白质水平表达，但不降低转录物水平。 Sapanisertib (INK-128) 降低 PC3 前列腺癌细胞的侵袭能力。此外，Sapanisertib (INK-128) 在治疗后 6 小时开始抑制癌细胞的迁移，恰好与促侵袭基因表达减少的时间一致，但在细胞周期或总体蛋白质合成发生任何改变之前。 2]。
|
| 体内研究 (In Vivo) |
Sapanisertib (INK-128) 在 ZR-75-1 乳腺癌异种移植模型中以 0.3 mg/kg/天的剂量表现出肿瘤生长抑制功效[1]。在 PtenL/L 小鼠中，INK128 治疗可将 4EBP1 和 p70S6K1/2 磷酸化完全恢复至野生型水平。使用 sapanisertib (INK-128) 治疗可将 PTENL/L 小鼠的前列腺上皮内瘤变 (PIN) 病变减少 50%，并导致许多癌细胞系发生程序性细胞死亡 [2]。
|
| 酶活实验 |
Sapanisertib (INK-128) 是一种 ATP 依赖性 mTOR1/2 抑制剂，对 mTOR 激酶的 IC50 为 1 nM。Sapanisertib (INK-128) 对 mTOR 具有酶抑制活性，对 PI3K 激酶具有超过 100 倍的选择性。细胞测定：INK 128对 mTOR 具有酶抑制活性，对 PI3K 激酶具有超过 100 倍的选择性。作为 TORC1/2 抑制剂，INK 128 抑制 TORC1 下游底物 S6 和 4EBP1 的磷酸化，并选择性抑制 TORC2 下游底物 Ser473 处的 AKT 磷酸化。此外，INK 128 还对雷帕霉素和泛 PI3K 抑制剂耐药的细胞系显示出有效的抑制作用。
|
| 细胞实验 |
用适当的药物处理 PC3 细胞 48 小时，并使用 CellTiter-Glo 发光试剂测量增殖。使用 20.0 M 至 0.1 nM 范围内的浓度（12 点曲线）确定实现 50% 细胞生长抑制 (IC50) 所需的 Sapanisertib (INK-128) 浓度。
|
| 动物实验 |
A subcutaneous inoculation of 5×106 MDA-MB-361 cells is administered to naked mice in the right subscapular region. The allocation of mice to vehicle control or treatment groups occurs once tumors have grown to a size of 150–200 mm3. Sapanisertib (INK-128) is formulated in 5% polyvinylpropyline, 15% NMP, and 80% water and is given orally by gavage at 0.3 mg/kg and 1 mg/kg daily.
|
| 参考文献 |
| 分子式 |
C15H15N7O
|
|---|---|
| 分子量 |
309.3259
|
| 精确质量 |
309.1338
|
| 元素分析 |
C, 58.24; H, 4.89; N, 31.70; O, 5.17
|
| CAS号 |
1224844-38-5
|
| 相关CAS号 |
1224844-38-5
|
| 外观&性状 |
White to off white solid powder
|
| SMILES |
CC(C)N1C2=NC=NC(=C2C(=N1)C3=CC4=C(C=C3)OC(=N4)N)N
|
| InChi Key |
GYLDXIAOMVERTK-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C15H15N7O/c1-7(2)22-14-11(13(16)18-6-19-14)12(21-22)8-3-4-10-9(5-8)20-15(17)23-10/h3-7H,1-2H3,(H2,17,20)(H2,16,18,19)
|
| 化学名 |
5-(4-amino-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-3-yl)-1,3-benzoxazol-2-amine
|
| 别名 |
MLN-0128; Sapanisertib; TAK-228; TAK 228; TAK228; INK128; INK-128; INK 128; MLN0128; MLN 0128; MLN-0128
|
| HS Tariff Code |
2934.99.9001
|
| 存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| 溶解度 (体外) |
DMSO: ~62 mg/mL (~200.4 mM)
Water: <1 mg/mL Ethanol: ~2 mg/mL (~6.5 mM) |
|---|---|
| 溶解度 (体内) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.72 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (6.72 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (6.72 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 30% PEG400+0.5% Tween80+5% propylene glycol: 30mg/mL 1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL； 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果，工作液请现配现用！ 6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
| 制备储备液 | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2328 mL | 16.1640 mL | 32.3279 mL | |
| 5 mM | 0.6466 mL | 3.2328 mL | 6.4656 mL | |
| 10 mM | 0.3233 mL | 1.6164 mL | 3.2328 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液)：对于大多数产品，InvivoChem推荐用DMSO配置母液 (比如：5、10、20mM或者10、20、50 mg/mL浓度），个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息，或者很难将产品溶解在溶液中，请联系我们;
3、建议使用下列计算器进行相关计算（摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等）;
4、母液配好之后，将其分装到常规用量，并储存在-20°C或-80°C，尽量减少反复冻融循环。
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)。如该浓度超过该批次药物DMSO溶解度，请首先与我们联系。
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。
(1) 请确保溶液澄清之后，再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶；
(2) 一定要按顺序加入溶剂 (助溶剂) 。
| NCT Number | Status | Interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03047213 | Active Recruiting |
Drug: Sapanisertib | Recurrent Bladder Carcinoma Metastatic Transitional Cell Carcinoma |
National Cancer Institute (NCI) |
August 24, 2017 | Phase 2 |
| NCT02159989 | Active Recruiting |
Drug: Sapanisertib Biological: Ziv-Aflibercept |
Ovarian Carcinoma Fibrolamellar Carcinoma |
National Cancer Institute (NCI) |
June 3, 2014 | Phase 1 |
| NCT02133183 | Active Recruiting |
Drug: Sapanisertib | Glioblastoma Gliosarcoma |
National Cancer Institute (NCI) |
May 12, 2014 | Phase 1 |
| NCT02503722 | Active Recruiting |
Drug: Sapanisertib Drug: Osimertinib |
Metastatic Lung Non-Small Cell Carcinoma Recurrent Lung Non-Small Cell Carcinoma |
National Cancer Institute (NCI) |
October 13, 2016 | Phase 1 |
| NCT02484430 | Active Recruiting |
Drug: Sapanisertib | B Acute Lymphoblastic Leukemia T Acute Lymphoblastic Leukemia |
National Cancer Institute (NCI) |
October 20, 2016 | Phase 2 |
Ribosome profiling reveals mTOR-dependent specialized translational control of the prostate cancer genome.Nature.2012 Feb 22;485(7396):55-61. |
mTOR promotes prostate cancer cell migration and invasion through a translationally regulated gene signature.
TheThe 4EBP1–eIF4E axis controls the post-transcriptional expression of mTOR-sensitive invasion genes.Nature.2012 Feb 22;485(7396):55-61 |
mTOR hyperactivation augments translation ofYB1, MTA1, CD44and vimentin mRNAs in a subset of pre-invasive prostate cancer cellsin vivo.Nature.2012 Feb 22;485(7396):55-61. |
Complete mTOR inhibition by INK128 treatment prevents prostate cancer invasion and metastasisin vivo.Nature.2012 Feb 22;485(7396):55-61. |
|
mTOR signal pathway.Drug Discov Today Ther Strateg.2009 Summer;6(2):47-55. |
Thioether-cyclized helix B peptide, CHBP TFA
mTOR inhibitor-12
mTOR inhibitor-11
mTOR inhibitor-14
InvivoChem的所有产品仅用于作科学研究，不面向患者销售
Copyright 2020 InvivoChem LLC | All Rights Reserved 粤ICP备20063088号-1
COA
粤公网安备 44011102003439号