| Bioactivity | KTC1101 is an orally active pan-PI3K inhibitor. KTC1101 can inhibit the PI3K signaling pathway, reduce downstream AKT and mTOR phosphorylation, and reduces the expression of Ki67. The anti-tumor effect of KTC1101 has a dual mechanism of action: directly inhibiting tumor cell growth and dynamically enhancing immune response[1]. |
| Invitro | KTC1101 (0.1-50000 nM, 48 h) 以剂量依赖性方式诱导所有测试细胞系 (PC3，TMD8，HSC2，HSC4 和 CAL33 细胞) 的细胞周期停滞在 G1 期，具有抗增殖活性，IC50 范围在20 nM-130 nM之间，但没有显著的促进凋亡作用[1]。KTC1101 (0.1-1000 nM, 1 h) 在 Adapta 激酶检测试验中，对所有 PI3K 亚型都表现出显著的抑制活性。KTC1101 对 PI3Kα，PI3Kβ，PI3Kδ 和 PI3Kγ 的 IC50 值分别为 3.72 nM，36.29 nM，1.22 nM 和 17.09 nM[1]。KTC1101 (0-125 nM, 48 h) 在 WB 实验中表现出对 PI3K 信号通路的有效抑制，PI3K 下游效应物 AKT 和 mTOR 磷酸化降低[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> KTC1101 相关抗体: Cell Viability Assay[1] Cell Line: |
| In Vivo | KTC1101 (每日口服 0-125 mg/kg，连续 14 天) 可以使人肿瘤异种移植小鼠的肿瘤生长停滞，并且没有复发迹象[1]。肿瘤异种移植小鼠模型的药代动力学分析[1]Route |
| CAS | 2764833-47-6 |
| Formula | C21H26F2N8O3 |
| Molar Mass | 476.48 |
| 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]. Peng X, et al. A novel pan-PI3K inhibitor KTC1101 synergizes with anti-PD-1 therapy by targeting tumor suppression and immune activation. Mol Cancer. 2024 Mar 14;23(1):54. |
KTC1101
CAS: 2764833-47-6 F: C21H26F2N8O3 W: 476.48
KTC1101 is an orally active pan-PI3K inhibitor. KTC1101 can inhibit the PI3K signaling pathway, reduce downstream AKT an
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