| Bioactivity | Ipatasertib (GDC-0068) tosylate is an orally active, highly selective and ATP-competitive pan-Akt inhibitor with IC50 values of 5, 18, 8 nM for Akt1/2/3, respectively. Ipatasertib tosylate synchronously activates FoxO3a and NF-κB through inhibition of Akt leading to p53-independent activation of PUMA. Ipatasertib tosylate also induces apoptosis in cancer cells and inhibits tumor growth in xenograft mouse models[1][2]. |
| Invitro | Ipatasertib tosylate (10 µM; 12, 24 h) 在细胞实验中，通过非 p53 依赖性的 PUMA 激活抑制结肠癌细胞增殖[1]。Ipatasertib tosylate (1, 5, 10, 20 μM; 24 h/10 μM; 3, 6, 12, 24 h) 在 HCT116 细胞中，以时间和浓度依赖的方式上调 PUMA 的表达[1]。Ipatasertib tosylate 在野生型、p53−/− 型, 以及 DLD1 (p53 突变) 型 HCT116 细胞中增加 PUMA 的 mRNA 水平[1]。Ipatasertib tosylate (10 µM; 24 h) 通过 PUMA/Bax 途径诱导 HCT116 细胞凋亡[1]。Cell Viability Assay:[1] MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Ipatasertib tosylate 相关抗体: Cell Viability Assay[1] Cell Line: |
| In Vivo | Ipatasertib tosylate (30 mg/kg; p.o.; single daily for 15 consecutive days) 在野生型和 PUMA−/− 型 HCT116 异种移植小鼠模型中显示出 PUMA 依赖性抗肿瘤活性[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
| CAS | 1491138-24-9 |
| Formula | C31H40ClN5O5S |
| Molar Mass | 630.20 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Sun L, et al. Ipatasertib, a novel Akt inhibitor, induces transcription factor FoxO3a and NF-κB directly regulates PUMA-dependent apoptosis. Cell Death Dis. 2018 Sep 5;9(9):911. |
Ipatasertib tosylate
CAS: 1491138-24-9 F: C31H40ClN5O5S W: 630.20
Ipatasertib (GDC-0068) tosylate is an orally active, highly selective and ATP-competitive pan-Akt inhibitor with IC50 va
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