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- 2026年01月19日
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- 详细信息
- 文献和实验
- 技术资料
- 保存条件：
Powder:-20℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:-20℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
OSI-027
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
936890-98-1
- 规格：
100mg/50mg/25mg/10mg/5mg/1mg
| 规格： | 100mg | 产品价格： | ￥6980.0 |
|---|---|---|---|
| 规格： | 50mg | 产品价格： | ￥3890.0 |
| 规格： | 25mg | 产品价格： | ￥2550.0 |
| 规格： | 10mg | 产品价格： | ￥1480.0 |
| 规格： | 5mg | 产品价格： | ￥780.0 |
| 规格： | 1mg | 产品价格： | ￥300.0 |
| 基本信息 | |
| CAS | No.936890-98-1 |
| 英文名称 | OSI-027 |
| 别名 | ASP7486 |
| 分子式 | C21H22N6O3 |
| 分子量 | 406.44 |
| 溶解性 | Soluble in DMSO ≥10mg/mL(Need ultrasonic) |
| 纯度 | ≥98% |
| 外观(性状) | Light yellow to yellow Solid |
| 储存条件 | Powder:-20℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| MDL | MFCD20275101 |
| SMILES | COC1=CC=CC2=C1NC(=C2)C3=C4C(=NC=NN4C(=N3)C5CCC(CC5)C(=O)O)N |
| InChIKey | JROFGZPOBKIAEW-UHFFFAOYSA-N |
| InChI | InChI=1S/C21H22N6O3/c1-30-15-4-2-3-13-9-14(25-16(13)15)17-18-19(22)23-10-24-27(18)20(26-17)11-5-7-12(8-6-11)21(28)29/h2-4，9-12，25H，5-8H2，1H3，(H，28，29)(H2，22，23，24) |
| PubChem CID | 135398516 |
| 靶点 | mTOR |
| 通路 | PI3K/Akt/mTOR |
| 背景说明 | OSI-027 是一种 ATP 竞争性的 mTOR 激酶活性抑制剂。 |
| 生物活性 | OSI-027 (ASP7486) is a potent， selective， orally active and ATP-competitive mTOR kinase activity inhibitor with an IC50 of 4 nM. OSI-027 targets both mTORC1 and mTORC2 with IC50s of 22 nM and 65 nM， respectively.[1-4] |
| In Vitro | OSI-027 is an ATP-competitive inhibitor， which targets both mTORC1 and mTORC2 with IC50s of 22 nM and 65 nM. OSI-027 also inhibits PI3K-α， PI3K-γ and DNA-PK with IC50s of 1.3 μM， 0.42 μM and 1.0 μM. OSI-027 inhibits mTOR signaling of phospho-4E-BP1 with an IC50 of 1 μM[1]. |
| 细胞实验 | Effects on GEO colorectal xenograft growth treated with Rapamycin or OSI-027 for 12 days are consistent with our in vitro experiments. Treatment with Rapamycin (20 mg/kg) inhibits phospho-S6 and phospho-4E-BP1， while Akt phosphorylation is increased by 29%. In contrast， OSI-027 (65 mg/kg) inhibits both mTORC1 and mTORC2 effectors. After 2 hours， decreased 4E-BP1， Akt， and S6 phosphorylation is observed and inhibition of S6 and Akt is sustained for 24 hours. The plasma drug concentration of OSI-027 inversely correlated with these effects on mTORC1 and mTORC2 signaling. The median plasma drug concentration with OSI-027 is 21.3 μM at 2 hours and 14.9 μM at 8 hours. The in vivo efficacy of OSI-027 plus Sunitinib is tested in H292 human lung and Ovcar-5 human ovarian xenograft tumors. H292 tumors， treated with OSI-027 (50 mg/kg) for 21 days have 61% median tumor growth inhibition for the duration of treatment (TGI). Sunitinib (40 mg/kg) for 21 days had 47% median TGI. Combining OSI-027 with Sunitinib， however， has a median TGI of 100% with 59% maximal tumor regression， a statistically significant improvement over either agent alone. Ovcar-5 xenograft tumors treated with OSI-027 or Sunitinib have a 55% and 68% median TGI， respectively. OSI-027 administered with Sunitinib has a significantly better median TGI of 100% with 38% maximal tumor regression[1]. In the Rapamycin (RAPA) group， three rats exhibit symptoms typical of LTx-aGVHD and die 27 to 35 days after liver transplantation (LT); the remaining five rats do not develop LTx-aGVHD symptoms and survive for more than 100 days. In contrast， seven rats in the OSI-027 group survive for more than 100 days without symptoms of LTx-aGVHD， and only one rat exhibits LTx-aGVHD symptoms and dies on day 33 after LT[3]. |
| 细胞实验 | To study the effect of drug treatment on cellular signaling， Ovcar-3 cells are plated in normal growth medium. After 24 hours， serum is removed and cells are serum-starved overnight. Rapamycin， OSI-027 and OXA-01 are solubilized in DMSO and added to cells at varying concentrations. After a two-hour incubation cells are growth factor stimulated with 10 ng/mL Insulin for 3 to 5 minutes， then rinsed with cold PBS and lysed[1]. |
| 动物实验 | Mice[1] For xenograft models， cells are harvested， implanted s.c. in the right flank of nu/nu CD-1 mice and tumor growth is analyzed. Mice bearing GEO xenografts are treated for 12 days with OSI-027 (65mg/kg) or vehicle and tumors collected at 2， 8， and 24 hours. Tumor growth inhibition and regression calculations are included. Rats[2]Specific pathogen-free female Lewis rats， male BN rats， male Lew-Tg(CAG-EGFP)YsRrrc rats and male Lew-TgYsRrrc rats are used. Orthotopic LT is undertaken. No antibiotics were used. Freshly prepared splenocytes (4×108， suspended in 500 μL PBS) of Lew-Tg YsRrrc rats are infused into each recipient via the dorsal penile vein immediately after LT (within 30 min). LTx-aGVHD model rats are divided into three experimental groups: RAPA (1 mg/kg)， OSI-027 (1 mg/kg) or control (equal quantity of vehicle) groups; treatments are administered via the vena caudalis from day 7 to day 15. |
| 激酶实验 | Assays of a panel of 40 other recombinant kinases including both protein and lipid kinases are performed at 100 mM ATP concentration by SelectScreen profiling service. A broad panel of kinases is tested at a single concentration of OSI-027 or OXA-01 (3 μM) to evaluate percent inhibition of each kinase or mutant variant， using the Ambit KinomeScan platform[1]. |
| 数据来源文献 | [1]. Falcon BL， et al. Reduced VEGF production， angiogenesis， and vascular regrowth contribute to the antitumor properties of dual mTORC1/mTORC2 inhibitors. Cancer Res. 2011 Mar 1;71(5):1573-83. [2]. Mateo J， et al. A first in man， dose-finding study of the mTORC1/mTORC2 inhibitor OSI-027 in patients with advanced solid malignancies. Br J Cancer. 2016;114(8):889-896. [3]. Zhang Y， et al. PP2AC Level Determines Differential Programming of p38-TSC-mTOR Signaling and Therapeutic Response to p38-Targeted Therapy in Colorectal Cancer. EBioMedicine. 2015 Nov 19;2(12):1944-56. [4]. Zhi X， et al. OSI-027 modulates acute graft-versus-host disease after liver transplantation in a rat model. Liver Transpl. 2017 Sep;23(9):1186-1198. |
| 单位 | 瓶 |
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