Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ipatasertib dihydrochloride (GDC-0068 dihydrochloride) 是ATP 竞争性的pan-Akt 选择性抑制剂,抑制Akt1,Akt2,Akt3,IC50分别为 5,18,8 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 358 | 现货 | ||
2 mg | ¥ 513 | 现货 | ||
5 mg | ¥ 888 | 现货 | ||
10 mg | ¥ 1,290 | 现货 | ||
25 mg | ¥ 2,290 | 现货 | ||
50 mg | ¥ 3,550 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 995 | 现货 |
产品描述 | Ipatasertib dihydrochloride (GDC-0068 dihydrochloride) is a highly selective and ATP-competitive inhibitor of pan-Akt (IC50s: 5, 18 and 8 nM for Akt1, Akt2 and Akt3, respectively). |
靶点活性 | Akt3:8 nM, PKA:3100 nM, Akt2:18 nM, Akt1:5 nM |
体外活性 | Ipatasertib displays more than 600 and more than 100-fold selectivity for Akt1 in IC50 against the closely related kinases PKA and p70S6K, respectively. Ipatasertib inhibits only 3 other kinases by more than 70% at 1 μM concentration (PRKG1α, PRKG1β, and p70S6K) when tested at 1 μM in a panel of 230 protein kinases, which includes 36 human AGC family members. IC50s measured for these 3 kinases are 98, 69, and 860 nM, respectively. The relationship between pharmacokinetics (PK) and pharmacodynamics (PD) of Ipatasertib is investigated in 3 xenograft models that showed a dose-dependent response to drug treatment: MCF7-neo/HER2, TOV-21G.x1, and LNCaP. The mean cell viability IC50 of Ipatasertib in these 3 cell lines is 2.56, 0.44, and 0.11 μM, respectively. Ipatasertib shows a more than 100-fold selectivity for Akt1 over the next most potently inhibited non-Akt kinase, p70S6K, in the screening kinase panel with the exception of PKG1 (relative to which Ipatasertib is >10-fold more selective for Akt1) [2]. |
体内活性 | Ipatasertib is typically efficacious in xenograft models in which Akt is activated because of genetic alterations including PTEN loss, PIK3CA mutations/amplification, or HER2 overexpression. The combination of Ipatasertib with RP-56976 or NSC 241240 is tolerated with less than 5% body weight loss when compared with treatment with each chemotherapeutic agent alone. The daily dosing of Ipatasertib in combination with RP-56976 induces tumor regression and stasis in the PC-3 and MCF7-neo/HER2 xenograft models, at doses where every single agent is ineffective or only causes modest tumor growth delay, when tested in vivo. Similarly, enhanced TGI is observed in the OVCAR3 ovarian cancer xenograft model when Ipatasertib is combined with NSC 241240 [2]. |
别名 | GDC-0068 dihydrochloride, RG-7440 dihydrochloride |
分子量 | 530.92 |
分子式 | C24H34Cl3N5O2 |
CAS No. | 1396257-94-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 125 mg/mL (235.44 mM), Sonication is recommended.
H2O: 41 mg/mL (77.22 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / H2O | 1 mM | 1.8835 mL | 9.4176 mL | 18.8352 mL | 47.0881 mL |
5 mM | 0.3767 mL | 1.8835 mL | 3.767 mL | 9.4176 mL | |
10 mM | 0.1884 mL | 0.9418 mL | 1.8835 mL | 4.7088 mL | |
20 mM | 0.0942 mL | 0.4709 mL | 0.9418 mL | 2.3544 mL | |
50 mM | 0.0377 mL | 0.1884 mL | 0.3767 mL | 0.9418 mL | |
DMSO | 100 mM | 0.0188 mL | 0.0942 mL | 0.1884 mL | 0.4709 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Ipatasertib dihydrochloride 1396257-94-5 Cytoskeletal Signaling PI3K/Akt/mTOR signaling Tyrosine Kinase/Adaptors Akt PKA RG 7440 Inhibitor PKB GDC 0068 Dihydrochloride Ipatasertib Dihydrochloride RG-7440 GDC 0068 RG7440 Dihydrochloride inhibit GDC-0068 Dihydrochloride RG-7440 Dihydrochloride GDC-0068 Ipatasertib RG7440 GDC-0068 dihydrochloride RG-7440 dihydrochloride Protein kinase B GDC0068 Dihydrochloride RG 7440 Dihydrochloride GDC0068 inhibitor