GDC-0068

98.30%

GDC-0068

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品牌：源叶(MedMol)

产品编号：S80002 一键复制产品信息

CAS号：1001264-89-6

分子式：C₂₄H₃₂ClN₅O₂

分子量：458

别名：(S)-2-(4-chlorophenyl)-1-(4-((5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazin-1-yl)-3-(isopropylamino)propan-1-one

货号	规格	价格	上海	北京	珠海	重庆	武汉
S80002-1mg	98.30%	￥200.00 S80002-1mg ￥200.00 现货	8 8	-	-	-	-
S80002-5mg	98.30%	￥544.00 S80002-5mg ￥544.00 现货	4 4	-	-	-	-
S80002-10mg	98.30%	￥748.00 S80002-10mg ￥748.00 现货	5 5	-	-	-	-
S80002-25mg	98.30%	￥1360.00 S80002-25mg ￥1360.00 现货	3 0 3	-	-	-	-
S80002-50mg	≥98%	￥2240.00 S80002-50mg ￥2240.00 2-3天	0 货期：2-3天	-	-	-	-
S80002-100mg	≥98%	￥4210.00 S80002-100mg ￥4210.00 2-3天	0 货期：2-3天	-	-	-	-

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产品介绍参考文献质检证书(COA) 摩尔浓度计算器相关产品

产品描述：

Ipatasertib (GDC-0068) is a highly selective and ATP-competitive pan-Akt inhibitor with IC50s of 5, 18 and 8 nM for Akt1, Akt2 and Akt3, respectively.

靶点：

Akt1:5 nM (IC50);Akt2:18 nM (IC50);Akt3:8 nM (IC50);PKA:3100 nM (IC50);Akt

体内研究：

Ipatasertib (GDC-0068) is typically efficacious in xenograft models in which Akt is activated because of genetic alterations including PTEN loss, PIK3CA mutations/amplifications, or HER2 overexpression. In these models, tumor growth delay, stasis, or regression is achieved at or below 100 mg/kg daily oral dose, which is the maximum dose tested in immunocompromised mice that is well tolerated. When tested in vivo, daily dosing of Ipatasertib (GDC-0068) in combination with RP-56976 induces tumor regression and stasis in the PC-3 and MCF7-neo/HER2 xenograft models, at doses where each single agent is ineffective or only causes modest tumor growth delay. Similarly, increased TGI is observed in the OVCAR3 ovarian cancer xenograft model when Ipatasertib (GDC-0068) is combined with NSC 241240. The combination of Ipatasertib (GDC-0068) with RP-56976 or NSC 241240 is tolerated with less than 5% body weight loss when compared with treatment with each chemotherapeutic agent alone

参考文献：

1. Blake JF, et al. Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors. J Med Chem. 2012 Sep 27;55(18):8110-27. 2. Lin J, et al. Targeting activated Akt with GDC-0068, a novel selective Akt inhibitor that is efficacious in multiple tumor models. Clin Cancer Res. 2013 Apr 1;19(7):1760-72.

溶解性：

DMSO : 220 mg/mL (480.35 mM; Need ultrasonic) H2O : 3.57 mg/mL (7.79 mM; ultrasonic and warming and heat to 60°C)

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.183 ml	10.917 ml	21.834 ml
5 mM	0.437 ml	2.183 ml	4.367 ml
10 mM	0.218 ml	1.092 ml	2.183 ml
50 mM	0.044 ml	0.218 ml	0.437 ml