2. Protein Tyrosine Kinase/RTK Apoptosis
  3. c-Fms Apoptosis
  4. CSF1R-IN-22

CSF1R-IN-22 (Compound C19) 是口服有效的 CSF-1R 选择性的抑制剂 (IC50 <6 nM)。通过促进 M2 型巨噬细胞分泌 CXCL9，提高 CD8+ T 细胞的浸润，增强 anti-PD-1 抗肿瘤免疫反应，诱导细胞凋亡。CSF1R-IN-22 可以有效地将 M2 型的肿瘤相关巨噬细胞重编程为 M1 表型，并通过诱导 CD8+ T 细胞募集到肿瘤中并减少免疫抑制性 Tregs/MDSCs 的浸润来重塑肿瘤相关巨噬细胞。

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CSF1R-IN-22 Chemical Structure

CSF1R-IN-22 Chemical Structure

CAS No. : 2760585-35-9

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CSF1R-IN-22 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

体外研究
(In Vitro)

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.

CSF1R-IN-22 相关抗体:

Western Blot Analysis[1]

Cell Line: BMDMs cells
Concentration: 10, 30, 100 nM
Incubation Time: 1 h
Result: Dose-dependently inhibited the phosphorylation of CSF-1R and its downstream signaling mediators AKT and mTORC1.

Apoptosis Analysis[1]

Cell Line: MC-38, CT-26 cells
Concentration: 10, 30, 100 nM
Incubation Time: 20 h
Result: Processed M2 macrophage supernatant significantly increased the apoptosis rate of MC-38 and CT-26 cells, with an increase of approximately 60% in the 100 nM concentration group.
体内研究
(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 Dose (mg/kg) AUC0-t (ng·h/mL) t1/2 (h) Cl (L/h/kg) Vss (L/kg) Cmax (ng/mL) F (%)
i.v. 1 9126.62 1.34 0.10 0.34 / /
p.o. 10 85 939.36 2.41 0.12 / 10 867.65 94.2

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 mice bearing subcutaneous MC-38 tumors [1]
Dosage: 5,10,20 mg/kg
Administration: p.o.; once daily for 14 days
Result: Inhibited tumor growth, tumor mass was significantly lower than that of the control group, and induced apoptosis. In the high-dose group, tumor volume inhibition (TGI) was 65% and 30-day survival in mice was 70%.
Increased mRNA levels of M1 macrophage markers (Nos2, Tnf, Il6, Il1) and decreased expression of M2 macrophage markers (Arg1, Chil3l, Rentla, Mrc1).
(10 mg/kg and 20 mg/kg) Significantly increased the proportion of CD3+ CD8+ T cells. Dose-dependently reduced the proportion of immunosuppressive Treg cells and myeloid-derived suppressor cells (MDSCs) in tumor tissues.
Animal Model: C57BL/6 mice bearing subcutaneous MC-38 tumors or MC-38-luc [1]
Dosage: 20 mg/kg; 100 μg/mouse PD-1
Administration: p.o.; once daily for 14 days
Result: Significantly lower tumor bioluminescence intensity in the combination dose group than in the PD-1 antibody alone or C19 alone dose groups in both models.
The combination dose group significantly increased the proportion of CD3+ CD8+ T cells and CTLs in the tumor tissue while significantly decreasing the proportion of immunosuppressive Treg cells in the MC-38 tumor model. A significant increase in the infiltration of CD8+ T cells and CTLs correlated with a significant increase in the mRNA expression of Cxcl9.
Co-administered mice had 100% survival at 70 days, and 70% overcame tumor recurrence within 91 days after reinoculation with MC-38 tumor cells.
A significant reduction in apoptosis and a significant reduction in the proportion of CD3+ CD8+ T cells following the use of CXCL9-neutralizing antibody.
分子量

392.41

Formula

C20H20N6O3
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

CSF1R-IN-22 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

CSF1R-IN-222760585-35-9c-FmsApoptosisCSF-1 receptorcolony stimulating factor 1 receptorCSF-1RCSF1RCXCL9 SecretionM2 Macrophage ReprogrammingT Cell InfiltrationAnti-Tumor Immune ResponseCancerImmune ModulationInhibitorinhibitorinhibit

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