2. Protein Tyrosine Kinase/RTK
  3. c-Fms
  4. PXB17

PXB17 可以通过阻断 PI3K/ AKT/mTORC1 信号的激活抑制 CSF1R (IC50 = 1.7 nM)， 口服有效，明显抑制 CRC 的生长，提高 PD-1 mAb 的疗效并且减少 CRC 的肿瘤复发。

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PXB17 Chemical Structure

PXB17 Chemical Structure

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PXB17 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

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].

体外研究
(In Vitro)

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.

PXB17 相关抗体:

Real Time qPCR[1]

Cell Line: BMDMs
Concentration: 10, 30, 100nM
Incubation Time: 24 h
Result: PXB17 shifted macrophages from an M2-like to an M1-like phenotype, indicated by changes in marker gene expression. The ability of PXB17 to reprogram macrophages suggests a role in enhancing anti-tumor immunity by converting immunosuppressive M2 macrophages into pro-inflammatory M1 macrophages, which are more capable of attacking tumor cells.

Immunofluorescence[1]

Cell Line: BMDMs
Concentration: 10, 30,100 nM
Incubation Time: 4 h
Result: PXB17 significantly inhibited CSF1R phosphorylation across all tested concentrations.
体内研究
(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: mice were inoculated with MC-38 cell [1]
Dosage: 10,20 mg/kg; daily
Administration: p.o.
Result: PXB17 significantly inhibited tumor growth and showed stronger anti-tumor effects at a dose of 20 mg/kg compared with PLX3397 (HY-16749). Meanwhile, tumor cell apoptosis was significantly increased in the PXB17-treated group, reprogramming of M2-type to M1-type macrophages, and enhanced activation and infiltration of CD8+ T cells.
Animal Model: mice were inoculated with CT-26 cell [1]
Dosage: 5, 10,20 mg/kg
Administration: p.o.
Result: PXB17 significantly inhibited CT-26 tumor growth at all doses. tumor tissues showed an increased proportion of M1-type macrophages, while decreasing the proportion of M2-type macrophages and enhancing CD8+ cell responses.
分子量

545.63

Formula

C29H35N7O4
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

PXB17 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PXB17PXB 17PXB-17c-FmsCSF-1 receptorcolony stimulating factor 1 receptorCSF-1RCSF1RColorectal cancerTumor associated macrophagesTumor immune microenvironmentCSF1R inhibitorAnti-PD-1 therapyCholesterol biosynthesisInhibitorinhibitorinhibit

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