| Bioactivity | PXB17 can inhibit CSF1R (IC50 = 1.7 nM) by blocking the activation of PI3K/ AKT/mTORC1 signaling. PXB17 is orally effective. PXB17 significantly inhibits the growth of CRC, improves PD-1 mAb efficacy and reduces tumor recurrence in CRC[1]. |
| Invitro | PXB17 (30 - 3000 nM; 4 h) 剂量依赖性地提高了 CSF1R 的稳定性[1]。PXB17 (30, 100 nM; 24 h) 抑制胆固醇的生物合成，并通过阻断 PI3K-AKT-mTORC1 信号转导来促使 M2 表型转化为 M1 表型，从而阻止 CRC 的发展[1]。PXB17 (10, 30, 100nM; 72 h) 提高了 CD8+T 细胞中的 CD69 的表达。 通过提高抗肿瘤的免疫力来阻止 CRC 细胞的生长[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> PXB17 相关抗体: Real Time qPCR[1] Cell Line: |
| In Vivo | PXB17 (10, 20 mg/kg; p.o.; 每天) 有效地抑制了接种 MC-38 细胞的 C57BL/6 小鼠的肿瘤生长[1]。PXB17 (10, 20 mg/kg ;p.o.; 每天) 在接种 MC-38 细胞的 C57BL/6， BALB/c 小鼠上发现, 可以通过直接抑制 CSF1R 和调节胆固醇生物合成途径来影响肿瘤细胞的生存和增殖，而且通过改变巨噬细胞的表型从而重塑肿瘤微环境[1]。PXB17 (20 mg/kg ;p.o.; 每天) 和 PD-1 mAb 同时使用提高了 CT-26(MSS)， MC-38(MSI-H) 小鼠抗肿瘤效果并且减少复发[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
| Formula | C29H35N7O4 |
| Molar Mass | 545.63 |
| 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]. Qi L et al. CSF1R inhibition reprograms tumor-associated macrophages to potentiate anti-PD-1 therapy efficacy against colorectal cancer Pharmacological Research 202 (2024) 107126. |