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My CartCAS：1224844-38-5
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to off-white Solid
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| CAS | 1224844-38-5 |
| Name | Sapanisertib |
| Molecular Formula | C15H15N7O |
| Molecular Weight | 309.33 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD22124893 |
| SMILES | CC(C)N1C2=NC=NC(=C2C(=N1)C3=CC4=C(C=C3)OC(=N4)N)N |
| Target Point | mTOR |
| Passage | PI3K/Akt/mTOR |
| Background | It is an orally active ATP-dependent mTOR1/2 inhibitor. |
| Biological Activity | Sapanisertib (INK-128) 是ATP依赖性的 mTOR1/2 抑制剂，抑制mTOR激酶的IC50 值为1 nM。[1-2] |
| In Vitro | Sapanisertib(INK-128)对mTOR具有酶抑制活性，对PI3K激酶具有100倍以上的选择性[1]。 Sapanisertib(INK-128)选择性地降低蛋白质中YB1，MTA1，波形蛋白和CD44的表达，但不降低PC3细胞中的转录水平。 Sapanisertib(INK-128)降低PC3前列腺癌细胞的侵袭潜力。此外，Sapanisertib(INK-128)在治疗6小时开始抑制癌细胞迁移，与促入侵袭基因表达减少明显相关，但在细胞周期或整体全球蛋白质合成的任何变化之前[2] 。 |
| In Vivo | 在ZR-75-1乳腺癌异种移植模型中，Sapanisertib(INK-128)在0.3mg / kg /天的剂量下显示出肿瘤生长抑制功效[1]。在PtenL / L小鼠中用INK128处理后，4EBP1和p70S6K1 / 2磷酸化完全恢复到野生型水平。 Sapanisertib(INK-128)治疗导致PtenL / L小鼠前列腺上皮内瘤变(PIN)损伤减少50％，并在小鼠的多种癌细胞系中诱导程序性细胞死亡[2]。 |
| Cell Experiment | 用合适的药物处理PC3细胞48小时，并使用CellTiter-Glo发光试剂测量增殖。使用浓度范围为20.0μM至0.1nM(12点曲线)计算实现细胞生长抑制50％所需的萨潘替尼(INK-128)浓度(IC 50)。 |
| Animal Experiment | 裸鼠在右肩胛下区域皮下接种5×106个MDA-MB-361细胞。在肿瘤达到150-200mm 3的大小后，将小鼠随机分配到载体对照组或治疗组中。 Sapanisertib(INK-128)配制成5％聚乙烯丙炔，15％NMP，80％水，并通过口服强饲法以0.3mg / kg和1mg / kg每天施用。 |
| Data Literature Source | [1]. Liu A，et al. mTOR Mediated Anti-Cancer Drug Discovery. Drug Discovery Today: Therapeutic Strategies. 2009，6(2)，47-55. [2]. Hsieh AC，et al. The translational landscape of mTOR signalling steers cancer initiation and metastasis. Nature. 2012 Feb 22;485(7396):55-61 |
| Unit | Bottle |
| Specification | 5mg 10mg 25mg |
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
Note：
1. The products are all for scientific research use only. Do not use it for medical, clinical diagnosis or treatment, food and cosmetics, etc. Do not store them in ordinary residential areas.
2. For your safety and health, please wear laboratory clothes, disposable gloves and masks.
3. The experimental results may be affected by many factors, after-sale service is limited to the product itself and does not involve other compensation.
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