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Ipatasertib dihydrochloride (GDC-0068 (dihydrochloride)) Sale

(Synonyms: (2S)-2-(4-氯苯基)-1-[4-[(5R,7R)-6,7-二氢-7-羟基-5-甲基-5H-环戊并嘧啶-4-基]-1-哌嗪基]-3-[(1-甲基乙基)氨基]-1-丙酮二盐酸盐,GDC-0068 dihydrochloride; RG-7440 dihydrochloride) 目录号 : GC32794

A pan-Akt inhibitor

Ipatasertib dihydrochloride (GDC-0068 (dihydrochloride)) Chemical Structure

Cas No.:1396257-94-5

规格 价格 库存 购买数量
2mg
¥585.00
现货
5mg
¥990.00
现货
10mM (in 1mL Water)
¥1,440.00
现货
50mg
¥3,870.00
现货
100mg
¥5,400.00
现货

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Sample solution is provided at 25 µL, 10mM.

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Quality Control & SDS

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实验参考方法

Cell experiment:

The 384-well plates are seeded with 2,000 cells per well in a volume of 54 μL per well followed by incubation at 37°C under 5% CO2 overnight (~16 hours). Compounds (e.g., Ipatasertib) are diluted in DMSO to generate the desired stock concentrations then added in a volume of 6 μL per well. All treatments are tested in quadruplicates. After 4 days incubation, relative numbers of viable cells are estimated using CellTiter-Glo and total luminescence is measured on a Wallac Multilabel Reader. The concentration of drug resulting in IC50 is calculated from a 4-parameter curve analysis (XLfit) and is determined from a minimum of 3 experiments. For cell lines that failed to achieve an IC50, the highest concentration tested (10 μM) is listed[2].

Animal experiment:

Mice[2] In vivo efficacy is evaluated in multiple tumor cell line- and patient-derived xenograft models. Cells or tumor fragments are implanted subcutaneously into the flank of immunocompromised mice. Female or male nude (nu/nu) or severe combined immunodeficient mice (SCID)/beige mice are used. For the MCF7-neo/HER2 model, 17β-estradiol pellets (0.36 mg/pellet, 60-day release) are implanted into the dorsal shoulder before cell inoculation. The LuCaP35V patient-derived primary tumors are obtained; male mice are castrated before implantation of tumor fragments. After implantation of tumor cells or fragments into mice, tumors are monitored until they reached mean tumor volumes of 180 to 350 mm3 and distributed into groups of 8 to 10 animals/group. Ipatasertib is formulated in 0.5% methylcellulose/0.2% Tween-80 (MCT) and administered daily (QD), via oral (per os; PO) gavage. Docetaxel is formulated in 3% EtOH/97% saline and dosed intravenously (IV) every week (QW) at 2.5 or 7.5 mg/kg. Carboplatin is formulated in saline and dosed intraperitoneally (IP) weekly at 50 mg/kg.

References:

[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.

产品描述

GDC-0068 is a selective, ATP-competitive, pan-Akt inhibitor that targets Akt1, 2, and 3 with IC50 values of 5, 18, and 8 nM, respectively in cell-free assays.1 It is 620-fold selective for Akt over protein kinase A and has been shown to block Akt signaling selectively in cultured tumor cell lines characterized by activated Akt, halting cell cycle progression and reducing cell viability.1 In multiple tumor xenograft models, oral administration of GDC-0068 at 100 mg/kg/day can lead to delayed tumor growth and regression.1

1.Lin, J., Sampath, D., Nannini, M.A., et al.Targeting activated Akt with GDC-0068, a novel selective Akt inhibitor that is efficacious in multiple tumor modelsClin. Cancer Res.19(7)1760-1772(2016)

Chemical Properties

Cas No. 1396257-94-5 SDF
别名 (2S)-2-(4-氯苯基)-1-[4-[(5R,7R)-6,7-二氢-7-羟基-5-甲基-5H-环戊并嘧啶-4-基]-1-哌嗪基]-3-[(1-甲基乙基)氨基]-1-丙酮二盐酸盐,GDC-0068 dihydrochloride; RG-7440 dihydrochloride
Canonical SMILES ClC1=CC=C([C@@H](CNC(C)C)C(N2CCN(C3=C([C@H](C)C[C@H]4O)C4=NC=N3)CC2)=O)C=C1.[H]Cl.[H]Cl
分子式 C24H34Cl3N5O2 分子量 530.92
溶解度 DMSO : 125 mg/mL (235.44 mM);Water : ≥ 41 mg/mL (77.22 mM) 储存条件 Store at -20°C, sealed storage, away from moisture
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 1.8835 mL 9.4176 mL 18.8352 mL
5 mM 0.3767 mL 1.8835 mL 3.767 mL
10 mM 0.1884 mL 0.9418 mL 1.8835 mL
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