| Bioactivity | CSF1R-IN-22 (Compound C19) is an orally effective CSF-1R selective inhibitor (IC50<6 nM). CSF1R-IN-22 enhances the secretion of CXCL9 from M2 macrophages, increases CD8+ T cell infiltration. CSF1R-IN-22 boosts anti-tumor immune responses of anti-PD-1, and induces apoptosis in tumor cells. CSF1R-IN-22 can effectively reprogram M2-like TAMs (tumor-associated macrophages) to the M1 phenotype and reshape the TME by inducing the recruitment of CD8+ T cells into tumors and reducing the infiltration of immunosuppressive Tregs and MDSCs[1]. |
| Invitro | CSF1R-IN-22 (0-2500 nM; 1 h) 显著抑制 BMDMs 细胞中的 CSF-1R 信号通路的激活[1]。CSF1R-IN-22 (30-100 nM; 24 h) 能够有效地将 BMDMs 细胞和 HMDMs 细胞中的 M2 型巨噬细胞重新编程为 M1 型巨噬细胞[1]。CSF1R-IN-22 (10-100 nM; 20 h) 处理的 M2 型巨噬细胞上清液显著抑制了 MC-38 和 CT-26 细胞的活力[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> CSF1R-IN-22 相关抗体: Western Blot Analysis[1] Cell Line: |
| In Vivo | CSF1R-IN-22 (5-20 mg/kg; p.o.; 每天一次，持续 14 天) 在携带 MC-38 皮下肿瘤的 C57BL/6 小鼠中展示了显著的抗肿瘤活性，增强了细胞毒性 T 淋巴细胞 (CTLs) 的活性，高剂量组表现出优于 PLX3397 (HY-16749) 的效果[1]。CSF1R-IN-22 (20 mg/kg; p.o.; 每天一次，持续 14 天) 和 100 μg/mouse PD-1 抗体联合使用时，显示出更强的抗肿瘤效果。CXCL9 的表达与生存率显著正相关[1]。SD 大鼠中的药代动力学分析[1] Route |
| CAS | 2760585-35-9 |
| Formula | C20H20N6O3 |
| Molar Mass | 392.41 |
| 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]. Lv Q, et al. Discovery of a Novel CSF-1R Inhibitor with Highly Improved Pharmacokinetic Profiles and Superior Efficacy in Colorectal Cancer Immunotherapy. J Med Chem. 2024 Apr 25;67(8):6854-6879. |