Afuresertib (GSK2110183)
中文名称：阿氟色替
Afuresertib (GSK2110183)是一种有效的，口服生物可利用的 Akt 抑制剂，对Akt1，Akt2，和 Akt3 的 Ki 分别为 0.08 nM，2 nM，和 2.6 nM。Phase 2。
Afuresertib (GSK2110183) Chemical Structure
CAS: 1047644-62-1
客户使用Selleck的Afuresertib (GSK2110183)发表文献31篇
产品质控
批次：
纯度：
99.61%
99.61
Afuresertib (GSK2110183)相关产品
相关信号通路图
Akt抑制剂选择性比较
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| Sf9 | Function assay | 40 mins | Inhibition of full length human AKT1 expressed in Sf9 cells assessed as reduction in substrate phosphorylation using biotin-ahx-ARKRERAYSFGHHA-amide substrate and [gamma-33P]ATP incubated for 40 mins by top count microplate scintillation counting method, IC50 = 0.001 μM. | ChEMBL | |
| Sf9 | Function assay | 40 mins | Inhibition of full length human AKT3 expressed in Sf9 cells assessed as reduction in substrate phosphorylation using biotin-ahx-ARKRERAYSFGHHA-amide substrate and [gamma-33P]ATP incubated for 40 mins by top count microplate scintillation counting method, IC50 = 0.001585 μM. | ChEMBL | |
| COLO205 | Growth inhibition assay | 72 hrs | Growth inhibition of human COLO205 cells at 1:10 molar ratio of compound in presence of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl- 2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide incubated for 72 hrs , IC50 = 0.009 μM. | ChEMBL | |
| Sf9 | Function assay | 40 mins | Inhibition of full length human AKT2 expressed in Sf9 cells assessed as reduction in substrate phosphorylation using biotin-ahx-ARKRERAYSFGHHA-amide substrate and [gamma-33P]ATP incubated for 40 mins by top count microplate scintillation counting method, IC50 = 0.01 μM. | ChEMBL | |
| MV522 | Growth inhibition assay | 72 hrs | Growth inhibition of human MV522 cells at 1:10 molar ratio of compound in presence of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl- 2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide incubated for 72 hrs, IC50 = 0.012 μM. | ChEMBL | |
| HT-29 | Growth inhibition assay | 72 hrs | Growth inhibition of human HT-29 cells at 1:10 molar ratio of compound in presence of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl- 2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide incubated for 72 hrs, IC50 = 0.015 μM. | ChEMBL | |
| NCI-H727 | Growth inhibition assay | 72 hrs | Growth inhibition of human NCI-H727 cells at 1:10 molar ratio of compound in presence of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl- 2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide incubated for 72 hrs, IC50 = 0.019 μM. | ChEMBL | |
| SW1417 | Growth inhibition assay | 72 hrs | Growth inhibition of human SW1417 cells at 1:10 molar ratio of compound in presence of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl- 2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide incubated for 72 hrs, IC50 = 0.03 μM. | ChEMBL | |
| Calu6 | Growth inhibition assay | 72 hrs | Growth inhibition of human Calu6 cells at 1:10 molar ratio of compound in presence of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl- 2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide incubated for 72 hrs, IC50 = 0.031 μM. | ChEMBL | |
| LS1034 | Growth inhibition assay | 72 hrs | Growth inhibition of human LS1034 cells at 1:10 molar ratio of compound in presence of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl- 2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide incubated for 72 hrs, IC50 = 0.04 μM. | ChEMBL | |
| SW1463 | Growth inhibition assay | 72 hrs | Growth inhibition of human SW1463 cells at 1:10 molar ratio of compound in presence of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl- 2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide incubated for 72 hrs, IC50 = 0.041 μM. | ChEMBL | |
| RKO | Growth inhibition assay | 72 hrs | Growth inhibition of human RKO cells at 1:10 molar ratio of compound in presence of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl- 2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide incubated for 72 hrs, IC50 = 0.054 μM. | ChEMBL | |
| NCI-H508 | Growth inhibition assay | 72 hrs | Growth inhibition of human NCI-H508 cells at 1:10 molar ratio of compound in presence of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl- 2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide incubated for 72 hrs, IC50 = 0.08 μM. | ChEMBL | |
| NCI-H1155 | Growth inhibition assay | 72 hrs | Growth inhibition of human NCI-H1155 cells at 1:10 molar ratio of compound in presence of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl- 2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide incubated for 72 hr, IC50 = 0.101 μM. | ChEMBL | |
| A427 | Growth inhibition assay | 72 hrs | Growth inhibition of human A427 cells at 1:10 molar ratio of compound in presence of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl- 2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide incubated for 72 hrs, IC50 = 0.103 μM. | ChEMBL | |
| KM12 | Growth inhibition assay | 72 hrs | Growth inhibition of human KM12 cells at 1:10 molar ratio of compound in presence of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl- 2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide incubated for 72 hrs, IC50 = 0.104 μM. | ChEMBL | |
| HCT8 | Growth inhibition assay | 72 hrs | Growth inhibition of human HCT8 cells at 1:10 molar ratio of compound in presence of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl- 2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide incubated for 72 hrs, IC50 = 0.143 μM. | ChEMBL | |
| MDA-MB-175-VII | Growth inhibition assay | 72 hrs | Growth inhibition of human MDA-MB-175-VII cells at 1:10 molar ratio of compound in presence of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl- 2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide incubated for 72 hrs, IC50 = 0.155 μM. | ChEMBL | |
| A549 | Growth inhibition assay | 72 hrs | Growth inhibition of human A549 cells at 1:10 molar ratio of compound in presence of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl- 2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide incubated for 72 hrs, IC50 = 0.164 μM. | ChEMBL | |
| NCI-H23 | Growth inhibition assay | 72 hrs | Growth inhibition of human NCI-H23 cells at 1:10 molar ratio of compound in presence of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl- 2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide incubated for 72 hrs , IC50 = 0.199 μM. | ChEMBL | |
| SW837 | Growth inhibition assay | 72 hrs | Growth inhibition of human SW837 cells at 1:10 molar ratio of compound in presence of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl- 2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide incubated for 72 hrs, IC50 = 0.248 μM. | ChEMBL | |
| SW480 | Growth inhibition assay | 72 hrs | Growth inhibition of human SW480 cells at 1:10 molar ratio of compound in presence of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl- 2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide incubated for 72 hrs, IC50 = 0.259 μM. | ChEMBL | |
| NCI-H1355 | Growth inhibition assay | 72 hrs | Growth inhibition of human NCI-H1355 cells at 1:10 molar ratio of compound in presence of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl- 2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide incubated for 72 hr, IC50 = 0.268 μM. | ChEMBL | |
| EFM19 | Growth inhibition assay | 72 hrs | Growth inhibition of human EFM19 cells at 1:10 molar ratio of compound in presence of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl- 2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide incubated for 72 hrs, IC50 = 0.3 μM. | ChEMBL | |
| T84 | Growth inhibition assay | 72 hrs | Growth inhibition of human T84 cells at 1:10 molar ratio of compound in presence of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl- 2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide incubated for 72 hrs, IC50 = 0.304 μM. | ChEMBL | |
| COR-L23 | Growth inhibition assay | 72 hrs | Growth inhibition of human COR-L23 cells at 1:10 molar ratio of compound in presence of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl- 2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide incubated for 72 hrs , IC50 = 0.368 μM. | ChEMBL | |
| NCI-H1792 | Growth inhibition assay | 72 hrs | Growth inhibition of human NCI-H1792 cells at 1:10 molar ratio of compound in presence of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl- 2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide incubated for 72 hr, IC50 = 0.374 μM. | ChEMBL | |
| SW1573 | Growth inhibition assay | 72 hrs | Growth inhibition of human SW1573 cells at 1:10 molar ratio of compound in presence of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl- 2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide incubated for 72 hrs, IC50 = 0.382 μM. | ChEMBL | |
| Calu3 | Growth inhibition assay | 72 hrs | Growth inhibition of human Calu3 cells at 1:10 molar ratio of compound in presence of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl- 2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide incubated for 72 hrs, IC50 = 0.392 μM. | ChEMBL | |
| HCC827 | Growth inhibition assay | 72 hrs | Growth inhibition of human HCC827 cells at 1:10 molar ratio of compound in presence of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl- 2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide incubated for 72 hrs, IC50 = 0.401 μM. | ChEMBL | |
| EFM19 | Growth inhibition assay | 72 hrs | Growth inhibition of human EFM19 cells incubated for 72 hrs by Cell-titer-Glo reagent based assay, IC50 = 0.43 μM. | ChEMBL | |
| HOP62 | Growth inhibition assay | 72 hrs | Growth inhibition of human HOP62 cells at 1:10 molar ratio of compound in presence of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl- 2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide incubated for 72 hrs, IC50 = 0.498 μM. | ChEMBL | |
| NCI-H508 | Growth inhibition assay | 72 hrs | Growth inhibition of human NCI-H508 cells incubated for 72 hrs by Cell-titer-Glo reagent based assay, IC50 = 0.522 μM. | ChEMBL | |
| SW900 | Growth inhibition assay | 72 hrs | Growth inhibition of human SW900 cells at 1:10 molar ratio of compound in presence of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl- 2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide incubated for 72 hrs, IC50 = 0.719 μM. | ChEMBL | |
| MDA-MB-175-VII | Growth inhibition assay | 72 hrs | Growth inhibition of human MDA-MB-175-VII cells incubated for 72 hrs by Cell-titer-Glo reagent based assay, IC50 = 0.794 μM. | ChEMBL | |
| NCI-H1155 | Growth inhibition assay | 72 hrs | Growth inhibition of human NCI-H1155 cells incubated for 72 hrs by Cell-titer-Glo reagent based assay, IC50 = 0.865 μM. | ChEMBL | |
| DLD1 | Growth inhibition assay | 72 hrs | Growth inhibition of human DLD1 cells at 1:10 molar ratio of compound in presence of N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl- 2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide incubated for 72 hrs, IC50 = 0.932 μM. | ChEMBL | |
| HT-29 | Growth inhibition assay | 72 hrs | Growth inhibition of human HT-29 cells incubated for 72 hrs by Cell-titer-Glo reagent based assay, IC50 = 1.383 μM. | ChEMBL | |
| HCT8 | Growth inhibition assay | 72 hrs | Growth inhibition of human HCT8 cells incubated for 72 hrs by Cell-titer-Glo reagent based assay, IC50 = 1.541 μM. | ChEMBL | |
| RKO | Growth inhibition assay | 72 hrs | Growth inhibition of human RKO cells incubated for 72 hrs by Cell-titer-Glo reagent based assay, IC50 = 1.806 μM. | ChEMBL | |
| Calu6 | Growth inhibition assay | 72 hrs | Growth inhibition of human Calu6 cells incubated for 72 hrs by Cell-titer-Glo reagent based assay, IC50 = 2.154 μM. | ChEMBL | |
| KM12 | Growth inhibition assay | 72 hrs | Growth inhibition of human KM12 cells incubated for 72 hrs by Cell-titer-Glo reagent based assay, IC50 = 2.247 μM. | ChEMBL | |
| COLO205 | Growth inhibition assay | 72 hrs | Growth inhibition of human COLO205 cells incubated for 72 hrs by Cell-titer-Glo reagent based assay, IC50 = 2.567 μM. | ChEMBL | |
| MV522 | Growth inhibition assay | 72 hrs | Growth inhibition of human MV522 cells incubated for 72 hrs by Cell-titer-Glo reagent based assay, IC50 = 3.044 μM. | ChEMBL | |
| LS1034 | Growth inhibition assay | 72 hrs | Growth inhibition of human LS1034 cells incubated for 72 hrs by Cell-titer-Glo reagent based assay, IC50 = 4.339 μM. | ChEMBL | |
| NCI-H727 | Growth inhibition assay | 72 hrs | Growth inhibition of human NCI-H727 cells incubated for 72 hrs by Cell-titer-Glo reagent based assay, IC50 = 4.799 μM. | ChEMBL | |
| COR-L23 | Growth inhibition assay | 72 hrs | Growth inhibition of human COR-L23 cells incubated for 72 hrs by Cell-titer-Glo reagent based assay, IC50 = 5.373 μM. | ChEMBL | |
| A549 | Growth inhibition assay | 72 hrs | Growth inhibition of human A549 cells incubated for 72 hrs by Cell-titer-Glo reagent based assay, IC50 = 5.993 μM. | ChEMBL | |
| NCI-H1355 | Growth inhibition assay | 72 hrs | Growth inhibition of human NCI-H1355 cells incubated for 72 hrs by Cell-titer-Glo reagent based assay, IC50 = 6.685 μM. | ChEMBL | |
| NCI-H23 | Growth inhibition assay | 72 hrs | Growth inhibition of human NCI-H23 cells incubated for 72 hrs by Cell-titer-Glo reagent based assay, IC50 = 7.124 μM. | ChEMBL | |
| NCI-H1792 | Growth inhibition assay | 72 hrs | Growth inhibition of human NCI-H1792 cells incubated for 72 hrs by Cell-titer-Glo reagent based assay, IC50 = 7.307 μM. | ChEMBL | |
| SW1463 | Growth inhibition assay | 72 hrs | Growth inhibition of human SW1463 cells incubated for 72 hrs by Cell-titer-Glo reagent based assay, IC50 = 9.725 μM. | ChEMBL | |
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Afuresertib (GSK2110183)是一种有效的，口服生物可利用的 Akt 抑制剂，对Akt1，Akt2，和 Akt3 的 Ki 分别为 0.08 nM，2 nM，和 2.6 nM。Phase 2。 | ||||||
|---|---|---|---|---|---|---|---|
| 靶点 |
|
| 体外研究(In Vitro) | ||||
| 体外研究活性 | Afuresertib抑制E17K AKT1突变蛋白的激酶活性，EC50为0.2 nM。Afuresertib对多重AKT底物磷酸化水平，包括GSK3b，PRAS40，FOXO和Caspase 9，表现出浓度依赖性作用。总体65%的血液学细胞系对afuresertib (EC50 < 1 μM)敏感。在测试的实体肿瘤细胞系中，21%对afuresertib的响应具有< 1 μM 的EC50 。[1] | |||
|---|---|---|---|---|
| 激酶实验 | Afuresertib的效力(Ki*)测定 | |||
| 抑制剂的真实效力(Ki*)首先在较低酶浓度(0.1 nM AKT1，0.7 nM AKT2，和0.2 nM AKT3)下使用过滤结合分析法测定，然后通过反应发展曲线分析证实。在过滤结合分析法中，酶的预混合物加抑制剂培养1小时，然后加入GSKα多肽 (Ac-KKGGRARTSS-FAEPG-amide)和 [γ33P] ATP。2小时后，反应终止，放射性标记的AKT多肽产物在磷酸纤维素过滤板上捕获。反应进展曲线分析利用连续实时荧光检测Sox-AKT-tide底物(Ac-ARKRERAYSF-d-Pro-Sox-Gly-NH2)生成的产品。 | ||||
| 细胞实验 | 细胞系 | 血液病细胞系和实体肿瘤癌细胞系 | ||
| 浓度 | 30 μM | |||
| 孵育时间 | 72 h | |||
| 方法 | 为期3天的增殖试验使用CellTiter-Glo进行，以测量0-30 μM化合物引起的生长抑制，细胞生长情况相对于未处理的(DMSO)对照组测定。EC50值根据抑制曲线使用Assay Client application中4或6参数拟合算法计算。 | |||
| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | p-GSK3 / GSK3 / p-PRAS40 / PRAS40 / p-FOXO / p-Casp9 / p-AKT / AKT / p-MEK / p-ERK / Erk ATG3 / ATG12 / LC3B |
|
24978597 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | 负荷BT474乳腺肿瘤异种移植物的小鼠，afuresertib (p.o.)以每天10，30或100 mg/kg的剂量给药，分别导致8，37和61% TGI。负荷SKOV3卵巢肿瘤异种移植物的小鼠用10，30和100 mg/kg afuresertib处理，分别导致23，37 和97% TGI。[1] | |
|---|---|---|
| 动物实验 | Animal Models | 负荷SKOV3或BT474肿瘤的雌性无胸腺裸鼠和 SCID小鼠 |
| Dosages | 100 mg/kg | |
| Administration | p.o. | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT05489744 | Completed | Healthy Volunteer |
Laekna Limited |
August 6 2022 | Phase 1 |
| NCT04374630 | Active not recruiting | Platinum-resistant Ovarian Cancer |
Laekna Limited |
June 9 2020 | Phase 2 |
| NCT04060394 | Active not recruiting | Metastatic Castration-resistant Prostate Cancer |
Laekna Limited |
September 13 2019 | Phase 1|Phase 2 |
| NCT02235740 | Terminated | Cancer |
Novartis|Amgen |
November 2014 | Phase 1 |
化学信息&溶解度
| 分子量 | 427.32 | 分子式 | C18H17Cl2FN4OS |
| CAS号 | 1047644-62-1 | SDF | Download Afuresertib (GSK2110183) SDF |
| Smiles | CN1C(=C(C=N1)Cl)C2=C(SC(=C2)C(=O)NC(CC3=CC(=CC=C3)F)CN)Cl | ||
| 储存条件(自收到货起) | |||
|
体外溶解度 |
DMSO : 85 mg/mL ( (198.91 mM)； DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Ethanol : 85 mg/mL Water : Insoluble |
摩尔浓度计算器 |
|
体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
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，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
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。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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