GDC-0068(RG 7440)是泛Akt抑制剂,对Akt1/2/3的IC50分别为5 nM/18 nM/8 nM,比对PKA的抑制性高620倍。
GDC-0068 (RG7440) is a potent and selective, ATP-competitive Akt inhibitor with IC50 values of 5 to 18 nM.
~100 mg/kg/day口服处理
动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数 | |
例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。
[1] Lin K. Cancer Res, 2011, 71(8 Supplement), abstract DDT02-01.
分子式 C24H32ClN5O2 |
分子量 458 |
CAS号 1001264-89-6 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 90 mg/mL |
Water <1 mg/mL |
Ethanol 90 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT02063581 | Healthy Volunteer | Drug: ipatasertib (Capsule)|Drug: ipatasertib (Tablet) | Genentech, Inc. | Phase 1 | 2014-02-01 | 2016-11-01 |
NCT02536391 | Cancer | Drug: Ipatasertib (capsule)|Drug: Ipatasertib (tablet) | Genentech, Inc. | Phase 1 | 2015-10-01 | 2016-11-01 |
NCT02162719 | Breast Neoplasms | Drug: Ipatasertib|Drug: Paclitaxel|Drug: Placebo | Genentech, Inc. | Phase 2 | 2014-09-01 | 2016-11-03 |
NCT03072238 | Metastatic Prostate Cancer | Drug: Ipatasertib|Drug: Abiraterone|Drug: Placebo | Hoffmann-La Roche | Phase 3 | 2017-06-01 | 2017-03-02 |
NCT02390492 | Healthy Volunteer | Drug: Period 1 treatment|Drug: Period 2 treatment | Genentech, Inc. | Phase 1 | 2015-03-01 | 2016-11-01 |
NCT02301988 | Breast Cancer | Drug: Ipatasertib|Drug: Paclitaxel|Drug: Placebo | Genentech, Inc.|SOLTI Breast Cancer Research Group | Phase 2 | 2015-02-01 | 2016-11-01 |
NCT01485861 | Prostate Cancer | Drug: Abiraterone|Drug: GDC-0980|Drug: Ipatasertib|Drug: Placebo|Drug: Prednisone|Drug: Prednisolone | Genentech, Inc. | Phase 1|Phase 2 | 2012-01-11 | 2017-03-20 |
NCT01562275 | Neoplasms | Drug: Ipatasertib|Drug: Cobimetinib | Genentech, Inc. | Phase 1 | 2012-04-01 | 2016-02-25 |
NCT02430363 | Glioblastoma | Drug: MK - 3475|Biological: Suppressor of the PI3K/Akt pathways | Medical Research Council|Department of Experimental Clinical Oncology, Aarhus University Hospital|NCRI Clinical Studies Groups|ECCO - the European CanCer Organisation|Merck Sharp & Dohme Corp. | Phase 1|Phase 2 | 2013-03-01 | 2016-02-23 |
注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。
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