Ipatasertib NEW
| Price | $39 | $55 | $80 |
| Package | 2mg | 5mg | 10mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-01 |
Product Details
| Product Name: Ipatasertib | CAS No.: 1001264-89-6 |
| Purity: 99.21% | Supply Ability: 10g |
| Release date: 2024/11/01 |
Product Introduction
Bioactivity
| 名稱 | Ipatasertib |
| 描述 | Ipatasertib (GDC-0068) is a selective, ATP-competitive pan-Akt inhibitor that inhibits Akt1 (IC50:5 nM), Akt2 (IC50:18 nM), and Akt3 (IC50:8 nM). Ipatasertib (GDC-0068) can lead to p53-independent PUMA activation by inhibiting Akt, thereby activating FoxO3a and NF-κB simultaneously, directly binding to the PUMA promoter, upregulating PUMA transcription and Bax-mediated intrinsic mitochondrial apoptosis. |
| 細(xì)胞實(shí)驗(yàn) | GDC-0068 is prepared in DMSO and stored, and then diluted with appropriate medium before use[2]. 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., GDC-0068) 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]. |
| 激酶實(shí)驗(yàn) | Kinase Assay: The fluorescence polarization assay for ATP competitive inhibition is done as follows: mPI3Kα dilution solution (90 nM) is prepared in fresh assay buffer (50 mM Hepes pH 7.4, 150 mM NaCl, 5 mM DTT, 0.05% CHAPS) and kept on ice. The enzyme reaction contains 0.5 nM mouse PI3Kα (p110α/p85α complex purified from insect cells), 30 μM PIP2, PF-04691502 (0, 1, 4, and 8 nM), 5 mM MgCl2, and 2-fold serial dilutions of ATP (0–800 μM). Final dimethyl sulfoxide is 2.5%. The reaction is initiated by the addition of ATP and terminated after 30 minutes with 10 mM EDTA. In a detection plate, 15 uL of detector/probe mixture containing 480 nM GST-Grp1PH domain and 12 nM TAMRA tagged fluorescent PIP3 in assay buffer is mixed with 15 uL of kinase reaction mixture. The plate is shaken for 3 minutes, and incubated for 35 to 40 minutes before reading on an LJL Analyst HT. |
| 體外活性 | METHODS: At 0, 3, 6, 12, and 24 hours after HCT116 cells were treated with Ipatasertib (GDC-0068) (1-20 μM), cell viability was detected in HCT116 by CCK-8 to study how ipatasertib affects tumor progression. RESULTS HCT116 cell viability decreased significantly with increasing dose or time, and Ipatasertib (GDC-0068) could inhibit cell proliferation in a dose- and time-dependent manner. [1] METHODS: HCT116 cells were treated with ipatasertib (GDC-0068) (10 μM), and the expression of p53 or PUMA in HCT116 WT and p53?/? was analyzed by Western blotting; ipatasertib (GDC-0068)-induced PUMA mRNA in WT, p53?/?HCT116 and DLD1 was analyzed by real-time qPCR and normalized to the housekeeping gene β-actin. RESULTS Ipatasertib (GDC-0068) treatment increased the expression level of PUMA with increasing doses; this upregulation was observed in WT (HCT116, RKO), p53 mutants (DLD1, HT29), and p53; Ipatasertib (GDC-0068) can lead to p53-independent transcriptional activation of PUMA and inhibit cell proliferation. [1] |
| 體內(nèi)活性 | METHODS: Nude mice were subcutaneously injected with HCT116 WT or PUMA?/?, and model mice were treated with Ipatasertib (GDC-0068) (30 mg/kg, oral, 15 days). Representative tumors at the end of the experiment, tumor weights, and c tumor volumes at specified time points after treatment were calculated to investigate whether PUMA-mediated apoptosis is essential for the anti-tumor activity of ipatasertib. RESULTS Ipatasertib (GDC-0068) significantly inhibited the growth of WT tumors; immunohistochemical staining showed that the expression of P-Akt was reduced in both WT and PUMA; Ki67 was significantly reduced in WT tumors, but there was no significant change in PUMA; C-Caspase3 was significantly increased in WT tumors and slightly increased in PUMA; Ipatasertib (GDC-0068) has a PUMA-dependent anti-tumor effect in colon cancer. [1] |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 85 mg/mL (185.6 mM) Ethanol : 85 mg/mL (185.6 mM) H2O : < 1 mg/mL (insoluble or slightly soluble) |
| 關(guān)鍵字 | Protein kinase B | RG-7440 | Ipatasertib | Inhibitor | Akt | PKB | GDC 0068 | inhibit | GDC0068 | RG 7440 |
| 相關(guān)產(chǎn)品 | Ethyl gallate | Oridonin | Capivasertib | SKLB-163 | Scutellarin | Artemisinin | Honokiol | 2,3-Butanediol | MK-2206 dihydrochloride | AKT Kinase Inhibitor |
| 相關(guān)庫(kù) | 高選擇性抑制劑庫(kù) | 經(jīng)典已知活性庫(kù) | 激酶抑制劑庫(kù) | 抗癌臨床化合物庫(kù) | 藥物功能重定位化合物庫(kù) | 抑制劑庫(kù) | 抗衰老化合物庫(kù) | 已知活性化合物庫(kù) | 抗癌藥物庫(kù) | 抗癌活性化合物庫(kù) |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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